DGIdb - ADRA1A Gene Record

ADRA1A 148 Druggable GenomeDrug Resistance

Alternate Names:

148
ADRENOCEPTOR ALPHA 1A
ADRA1A
ADRA1C
ADRA1L1
ALPHA1AAR
104221
277
ENSG00000120907
OTTHUMG00000099459
P35348
ADA1A_HUMAN
22
NP_000671
NM_000680
α<sub>1A</sub>-adrenoceptor
BE0004888
Alpha-adrenergic receptor 1a
Alpha-1D adrenoceptor
Alpha-1D adrenoreceptor
Alpha-1D adrenergic receptor
Alpha-1A adrenergic receptor
ADRA1D
Alpha-1A adrenoceptor
Alpha-1A adrenoreceptor
Alpha-1C adrenergic receptor
Alpha-adrenergic receptor 1c
ALPHA-1A ADRENERGIC RECEPTOR (ALPHA 1A-ADRENOCEPTOR) (ALPHA 1A- ADRENORECEPTOR) (ALPHA-1C ADRENERGIC RECEPTOR) (ALPHA ADRENERGIC RECEPTOR 1C). [SOURCE:UNIPROT/SWISSPROT;ACC:P35348]
BE0000501
BE0004863
TTDC00292
ALPHA ADRENERGIC RECEPTOR 1C
ALPHA 1A-ADRENORECEPTOR
ALPHA 1A-ADRENOCEPTOR
PA34
Adrenergic receptor alpha-1A
T92609

Gene Info:

GuideToPharmacology Gene Category Name	Adrenoceptors
GuideToPharmacology Gene Category ID	4
GuideToPharmacology Gene Type	gpcr
Interpro Acc	IPR000276
Interpro Short Name	7TM_GPCR_Rhodpsn
Human Readable Name	G PROTEIN COUPLED RECEPTOR
Uniprot Evidence	1: Evidence at protein level
Interpro Name	GPCR, rhodopsin-like, 7TM
Uniprot Status	Swiss-Prot
Interpro Type	Family
Human Readable Name	DRUGGABLE GENOME
Target Class	Receptors
Target Subclass	GPCR
Target Subclass	Rhodopsin
Target Main Class	Receptors
Transmembrane Helix Count	7
Gene Biotype	PROTEIN_CODING

(13 More Sources)

Gene Categories: Category Details

CELL SURFACE
DRUG RESISTANCE
G PROTEIN COUPLED RECEPTOR
PHOSPHOLIPASE
DRUGGABLE GENOME

Publications:

Shahid et al., 2009, Asenapine: a novel psychopharmacologic agent with a unique human receptor signature., J. Psychopharmacol. (Oxford)
González-Espinosa et al., 2001, Molecular cloning and functional expression of the guinea pig alpha(1a)-adrenoceptor., Eur. J. Pharmacol.
Yang et al., 1996, (+/-)-tamsulosin, an alpha 1A-adrenoceptor antagonist, inhibits the positive inotropic effect but not the accumulation of inositol phosphates in rabbit heart., Eur. J. Pharmacol.
Shibata et al., 2001, [Excitatory effect of noradrenaline on rat airway parasympathetic ganglion neurons]., Fukuoka Igaku Zasshi
Furukawa et al., 1995, Alpha 1A-adrenoceptor-mediated contractile responses of the human vas deferens., Br. J. Pharmacol.
Deplanne et al., 1996, Functional characterization of alpha-1-adrenoceptor subtypes in the prostatic urethra and trigone of male rabbit., J. Pharmacol. Exp. Ther.
Nasrallah, 2008, Atypical antipsychotic-induced metabolic side effects: insights from receptor-binding profiles., Mol. Psychiatry
Nourian et al., 2008, Orthostatic hypotensive effect of antipsychotic drugs in Wistar rats by in vivo and in vitro studies of alpha1-adrenoceptor function., Psychopharmacology (Berl.)
Eltze, 1996, In functional experiments, risperidone is selective, not for the B, but for the A subtype of alpha 1-adrenoceptors., Eur. J. Pharmacol.
Keks et al., 1999, Risperidone (Risperdal): clinical experience with a new antipsychosis drug., Expert Opin Investig Drugs
Fenton et al., 2005, Risperidone: a review of its use in the treatment of bipolar mania., CNS Drugs
Richelson et al., 2000, Binding of antipsychotic drugs to human brain receptors focus on newer generation compounds., Life Sci.
Sleight et al., 1993, Binding of antipsychotic drugs at alpha 1A- and alpha 1B-adrenoceptors: risperidone is selective for the alpha 1B-adrenoceptors., Eur. J. Pharmacol.
Corena-McLeod M, 2015, Comparative Pharmacology of Risperidone and Paliperidone., Drugs R D
Moya-Huff et al., 1987, Adrenergic receptor subtype activation by (+)-, (-)- and (+/-)-norephedrine in the pithed rat., J. Pharm. Pharmacol.
Buckner et al., 2002, ABT-866, a novel alpha(1A)-adrenoceptor agonist with antagonist properties at the alpha(1B)- and alpha(1D)-adrenoceptor subtypes., Eur. J. Pharmacol.
Altenbach et al., 2004, Synthesis and structure-activity studies on N-[5-(1H-imidazol-4-yl)-5,6,7,8-tetrahydro-1-naphthalenyl]methanesulfonamide, an imidazole-containing alpha(1A)-adrenoceptor agonist., J. Med. Chem.
Imming et al., 2006, Drugs, their targets and the nature and number of drug targets., Nat Rev Drug Discov
Wellman et al., Effects of the alpha 1a-adrenoceptor antagonist RS-17053 on phenylpropanolamine-induced anorexia in rats., Pharmacol. Biochem. Behav.
Martínez-Salas et al., 2007, Alpha1A-adrenoceptors predominate in the control of blood pressure in mouse mesenteric vascular bed., Auton Autacoid Pharmacol
Tomiyama et al., 2007, Expressions and mechanical functions of alpha1-adrenoceptor subtypes in hamster ureter., Eur. J. Pharmacol.
Huerta-Bahena et al., 1983, Trifluoperazine and chlorpromazine antagonize alpha 1- but not alpha2- adrenergic effects., Mol. Pharmacol.
Cahir et al., 2005, Antipsychotics lack alpha 1A/B adrenoceptor subtype selectivity in the rat., Eur Neuropsychopharmacol
Michel et al., 1996, Drugs for treatment of benign prostatic hyperplasia: affinity comparison at cloned alpha 1-adrenoceptor subtypes and in human prostate., J Auton Pharmacol
Lee et al., 1997, Clinical comparison of selective and non-selective alpha 1A-adrenoreceptor antagonists in benign prostatic hyperplasia: studies on tamsulosin in a fixed dose and terazosin in increasing doses., Br J Urol
Na et al., 1998, Clinical comparison of selective and non-selective alpha 1A-adrenoceptor antagonists for bladder outlet obstruction associated with benign prostatic hyperplasia: studies on tamsulosin and terazosin in Chinese patients. The Chinese Tamsulosin Study Group., J Med
Roehrborn et al., 2004, Alpha1-adrenergic receptors and their inhibitors in lower urinary tract symptoms and benign prostatic hyperplasia., J. Urol.
Chapple, 1998, Medical therapy and quality of life., Eur. Urol.
Chen et al., 2002, TTD: Therapeutic Target Database., Nucleic Acids Res.
Millan MJ et al., 2000, S18616, a highly potent, spiroimidazoline agonist at alpha(2)-adrenoceptors: I. Receptor profile, antinociceptive and hypothermic actions in comparison with dexmedetomidine and clonidine., J Pharmacol Exp Ther
Saeed et al., Alpha-adrenoceptor blockade by phentolamine causes beta-adrenergic vasodilation by increased catecholamine release due to presynaptic alpha-blockade., J. Cardiovasc. Pharmacol.
Giussani et al., 1995, Alpha 1- and alpha 2-adrenoreceptor actions of phentolamine and prazosin on breathing movements in fetal sheep in utero., J. Physiol. (Lond.)
Bylund, 1992, Subtypes of alpha 1- and alpha 2-adrenergic receptors., FASEB J.
Kawasaki et al., 2008, False negative apraclonidine test in two patients with Horner syndrome., Klin Monbl Augenheilkd
Sueke et al., 2010, Using apraclonidine in diagnosing Horner syndrome in children., Am. J. Ophthalmol.
Mirzai et al., 2006, Congenital Horner's syndrome and the usefulness of the apraclonidine test in its diagnosis., Indian J Ophthalmol
Moodley et al., 2007, Apraclonidine in the diagnosis of Horner's syndrome., S. Afr. Med. J.
Chen et al., 2006, Efficacy of apraclonidine 0.5% in the diagnosis of Horner syndrome in pediatric patients under low or high illumination., Am. J. Ophthalmol.
Freedman et al., 2005, Topical apraclonidine in the diagnosis of suspected Horner syndrome., J Neuroophthalmol
Watts et al., 2007, Adverse effects of apraclonidine used in the diagnosis of Horner syndrome in infants., J AAPOS
Lepor et al., 2010, Silodosin for the treatment of benign prostatic hyperplasia: pharmacology and cardiovascular tolerability., Pharmacotherapy
Cusack et al., 1994, Binding of antidepressants to human brain receptors: focus on newer generation compounds., Psychopharmacology (Berl.)
Taylor et al., 1995, Pharmacology and neurochemistry of nefazodone, a novel antidepressant drug., J Clin Psychiatry
Hietala et al., 2001, Sertindole is a serotonin 5-HT2c inverse agonist and decreases agonist but not antagonist binding to 5-HT2c receptors after chronic treatment., Psychopharmacology (Berl.)
Lindström et al., 2006, Sertindole: efficacy and safety in schizophrenia., Expert Opin Pharmacother
Millan et al., 2000, Mirtazapine enhances frontocortical dopaminergic and corticolimbic adrenergic, but not serotonergic, transmission by blockade of alpha2-adrenergic and serotonin2C receptors: a comparison with citalopram., Eur. J. Neurosci.
de Boer et al., 1988, Neurochemical and autonomic pharmacological profiles of the 6-aza-analogue of mianserin, Org 3770 and its enantiomers., Neuropharmacology
Wikström et al., 2002, Synthesis and pharmacological testing of 1,2,3,4,10,14b-hexahydro-6-methoxy-2-methyldibenzo[c,f]pyrazino[1,2-a]azepin and its enantiomers in comparison with the two antidepressants mianserin and mirtazapine., J. Med. Chem.
Fernández et al., 2005, Discovery of new tetracyclic tetrahydrofuran derivatives as potential broad-spectrum psychotropic agents., J. Med. Chem.
Nutt D, 1997, Mirtazapine: pharmacology in relation to adverse effects., Acta Psychiatr Scand Suppl
Senard et al., 2001, Orthostatic hypotension in patients with Parkinson's disease: pathophysiology and management., Drugs Aging
Lachnit et al., 1997, Pharmacological characterization of an alpha 1A-adrenoceptor mediating contractile responses to noradrenaline in isolated caudal artery of rat., Br. J. Pharmacol.
Du et al., 2010, Modeling the interactions between alpha(1)-adrenergic receptors and their antagonists., Curr Comput Aided Drug Des
Burt et al., 1996, The role of diacylglycerol and activation of protein kinase C in alpha 1A-adrenoceptor-mediated contraction to noradrenaline of rat isolated epididymal vas deferens., Br. J. Pharmacol.
Bishop, 2007, Recent advances in the discovery of alpha1-adrenoceptor agonists., Curr Top Med Chem
Morris et al., 2004, Cellular trafficking of human alpha1a-adrenergic receptors is continuous and primarily agonist-independent., Mol. Pharmacol.
Suzuki et al., 2000, Effect of JTH-601, a novel alpha(1)-adrenoceptor antagonist, on prostate function in dogs., Eur. J. Pharmacol.
Chang et al., 2003, Stimulatory effect of cinnamic acid analogues on alpha1A-adrenoceptors in-vitro., J. Pharm. Pharmacol.
Zacharia et al., 2004, Alpha1-adrenoceptor subtypes involved in vasoconstrictor responses to exogenous and neurally released noradrenaline in rat femoral resistance arteries., Br. J. Pharmacol.
Andersohn et al., 2010, Priapism associated with antipsychotics: role of alpha1 adrenoceptor affinity., J Clin Psychopharmacol
Bymaster et al., 1999, Antagonism by olanzapine of dopamine D1, serotonin2, muscarinic, histamine H1 and alpha 1-adrenergic receptors in vitro., Schizophr. Res.
Brafford MV et al., 2014, Olanzapine: an antiemetic option for chemotherapy-induced nausea and vomiting., J Adv Pract Oncol
Jensen et al., 2010, Functional alpha-1B adrenergic receptors on human epicardial coronary artery endothelial cells., Naunyn Schmiedebergs Arch. Pharmacol.
Sanbe et al., 2007, Alpha1-adrenoceptors are required for normal male sexual function., Br. J. Pharmacol.
Overington et al., 2006, How many drug targets are there?, Nat Rev Drug Discov
Martin et al., 1995, Renal vasodilatation by dopexamine and fenoldopam due to alpha 1-adrenoceptor blockade., Br. J. Pharmacol.
Ahlquist, 1976, Present state of alpha- and beta-adrenergic drugs I. The adrenergic receptor., Am. Heart J.
Mohta et al., 2010, Comparison of phenylephrine hydrochloride and mephentermine sulphate for prevention of post spinal hypotension., Anaesthesia
Alvarez-Guerra et al., 1999, Selective blockade by nicergoline of vascular responses elicited by stimulation of alpha 1A-adrenoceptor subtype in the rat., Fundam Clin Pharmacol
Hrometz et al., 1999, Expression of multiple alpha1-adrenoceptors on vascular smooth muscle: correlation with the regulation of contraction., J. Pharmacol. Exp. Ther.
Bogacka, 1999, [Decongestants in treatment of nasal obstruction]., Otolaryngol Pol
Leonardi, 2005, Emerging drugs for ocular allergy., Expert Opin Emerg Drugs
Ogidigben et al., 2001, Naphazoline-induced suppression of aqueous humor pressure and flow: involvement of central and peripheral alpha(2)/I(1) receptors., Exp. Eye Res.
Piletz et al., 1996, Comparison of ligand binding affinities at human I1-imidazoline binding sites and the high affinity state of alpha-2 adrenoceptor subtypes., J. Pharmacol. Exp. Ther.
Kai, 1999, [Effects of topical alpha 1- and beta 2-adrenoceptor stimulants on nasal nitric oxide level]., Nippon Jibiinkoka Gakkai Kaiho
Southard BT et al., 2020, Promethazine,
Tatsuta et al., 1998, Alpha1-adrenoceptor stimulation enhances experimental gastric carcinogenesis induced by N-methyl-N'-nitro-N-nitrosoguanidine in Wistar rats., Int. J. Cancer
Dale et al., 2007, Dronedarone: an amiodarone analog for the treatment of atrial fibrillation and atrial flutter., Ann Pharmacother
Heijman J et al., 2013, Pleiotropic effects of antiarrhythmic agents: dronedarone in the treatment of atrial fibrillation., Clin Med Insights Cardiol
Wellington et al., 2001, Cetirizine/pseudoephedrine., Drugs
Johnson DA et al., 1993, The pharmacology of alpha-adrenergic decongestants., Pharmacotherapy
Nakamura et al., 1999, Tamsulosin: assessment of affinityof (3)H-P razosin binding to two alpha-1- adrenoceptor subtypes in the canine aorta., Pharmacology
Rosendorff, 1993, Beta-blocking agents with vasodilator activity., J Hypertens Suppl
Bernstein et al., 1989, Partial attenuation of hemodynamic responses to rapid sequence induction and intubation with labetalol., J Clin Anesth
Shiraishi et al., 1992, Alpha 1-adrenoceptor blocking activities of bevantolol hydrochloride(NC-1400) and labetalol in rat isolated thoracic aorta--do they distinguish between subtypes?, Gen. Pharmacol.
Sassard et al., 1983, [Comparative effects of an alpha 1 and beta 1-2 blocker (labetalol) and a beta-1 blocker (atenolol) in the hypertensive patient]., J Pharmacol
van Zwieten, 1993, An overview of the pharmacodynamic properties and therapeutic potential of combined alpha- and beta-adrenoceptor antagonists., Drugs
Pedersen et al., 2007, The vasodilatory beta-blockers., Curr. Hypertens. Rep.
Eltze, 1997, Affinity of the miotic drug, dapiprazole, at alpha 1-adrenoceptor subtypes A, B and D., J. Pharm. Pharmacol.
Abrams et al., 1997, A dose-ranging study of the efficacy and safety of tamsulosin, the first prostate-selective alpha 1A-adrenoceptor antagonist, in patients with benign prostatic obstruction (symptomatic benign prostatic hyperplasia)., Br J Urol
Michel et al., 2004, Efficacy and safety of tamsulosin in the treatment of urological diseases., Expert Opin Pharmacother
Chen et al., 2009, Blockade of alpha 1A-adrenoceptor: a novel possible strategy for male contraception., Med. Hypotheses
Schulman et al., 1996, Tamsulosin, the first prostate-selective alpha 1A-adrenoceptor antagonist. Analysis of a multinational, multicentre, open-label study assessing the long-term efficacy and safety in patients with benign prostatic obstruction (symptomatic BPH). European Tamsulosin Study Group., Eur. Urol.
Chapple et al., 1996, Tamsulosin, the first prostate-selective alpha 1A-adrenoceptor antagonist. A meta-analysis of two randomized, placebo-controlled, multicentre studies in patients with benign prostatic obstruction (symptomatic BPH). European Tamsulosin Study Group., Eur. Urol.
Richelson et al., 1984, Antagonism by antidepressants of neurotransmitter receptors of normal human brain in vitro., J. Pharmacol. Exp. Ther.
Buckley et al., 1998, Can the fatal toxicity of antidepressant drugs be predicted with pharmacological and toxicological data?, Drug Saf
Fabre et al., [Mechanisms of action of antidepressants: new data from Escitalopram]., Encephale
Bareggi et al., 2007, The use of escitalopram beyond major depression: pharmacological aspects, efficacy and tolerability in anxiety disorders., Expert Opin Drug Metab Toxicol
Sanchez C et al., 2014, A comparative review of escitalopram, paroxetine, and sertraline: Are they all alike?, Int Clin Psychopharmacol
Zupkó et al., 2003, Alpha-adrenergic blockade: a possible mechanism of tocolytic action of certain benzodiazepines in a postpartum rat model in vivo., Life Sci.
Spencer RC et al., 2015, The cognition-enhancing effects of psychostimulants involve direct action in the prefrontal cortex., Biol Psychiatry
Bèïque et al., 1998, Are the new selective alpha-blockers better than non-selective alpha-blockers for benign prostatic hyperplasia?, Can Fam Physician
Elhilali, 2006, Alfuzosin: an alpha1-receptor blocker for the treatment of lower urinary tract symptoms associated with benign prostatic hyperplasia., Expert Opin Pharmacother
Faure et al., 1994, Identification of alpha 1-adrenoceptor subtypes present in the human prostate., Life Sci.
Roehrborn, 2001, Alfuzosin: overview of pharmacokinetics, safety, and efficacy of a clinically uroselective alpha-blocker., Urology
McVary, 2006, BPH: epidemiology and comorbidities., Am J Manag Care
Martin et al., 1997, Comparative alpha-1 adrenoceptor subtype selectivity and functional uroselectivity of alpha-1 adrenoceptor antagonists., J. Pharmacol. Exp. Ther.
Andersson et al., 1997, Prostatic alpha 1-adrenoceptors and uroselectivity., Prostate
Kenny et al., 1996, Evaluation of the pharmacological selectivity profile of alpha 1 adrenoceptor antagonists at prostatic alpha 1 adrenoceptors: binding, functional and in vivo studies., Br. J. Pharmacol.
Lee, 2003, Alfuzosin hydrochloride for the treatment of benign prostatic hyperplasia., Am J Health Syst Pharm
Lowe, 2004, Role of the newer alpha, -adrenergic-receptor antagonists in the treatment of benign prostatic hyperplasia-related lower urinary tract symptoms., Clin Ther
Greco et al., 2008, The role of combination medical therapy in benign prostatic hyperplasia., Int. J. Impot. Res.
Shannon et al., 2006, Effect of alpha1-adrenergic receptors in cardiac pathophysiology., Am. Heart J.
Martin, 1999, Preclinical pharmacology of alpha1-adrenoceptor antagonists., Eur. Urol.
Yono et al., 2004, Doxazosin-induced up-regulation of alpha 1A-adrenoceptor mRNA in the rat lower urinary tract., Can. J. Physiol. Pharmacol.
Bae et al., 2005, The effects of alpha-adrenoceptor antagonists on the urethral perfusion pressure of the female rat., BJU Int.
Ishizuka et al., 1997, Stimulation of bladder activity by volume, L-dopa and capsaicin in normal conscious rats--effects of spinal alpha 1-adrenoceptor blockade., Naunyn Schmiedebergs Arch. Pharmacol.
Schwinn DA et al., 2008, Alpha1-adrenoceptor subtypes and lower urinary tract symptoms., Int J Urol
Nojimoto et al., The tricyclic antidepressants amitriptyline, nortriptyline and imipramine are weak antagonists of human and rat alpha1B-adrenoceptors., Neuropharmacology
O'Connell TD et al., 2013, Cardiac alpha1-adrenergic receptors: novel aspects of expression, signaling mechanisms, physiologic function, and clinical importance., Pharmacol Rev
Jensen BC et al., 2009, {alpha}1-Adrenergic receptor subtypes in nonfailing and failing human myocardium., Circ Heart Fail
Shekim WO et al., 1994, Platelet alpha 2-adrenergic receptor binding and the effects of d-amphetamine in boys with attention deficit hyperactivity disorder., Neuropsychobiology
Nakamura S et al., 1982, Changes in noradrenergic terminal excitability induced by amphetamine and their relation to impulse traffic., Neuroscience
Parker et al., 1988, Comparative effects of amphetamine, phenylethylamine and related drugs on dopamine efflux, dopamine uptake and mazindol binding., J. Pharmacol. Exp. Ther.
Valdivia et al., 2004, Pharmacological analysis of the mechanisms involved in the tachycardic and vasopressor responses to the antimigraine agent, isometheptene, in pithed rats., Life Sci.
Taniguchi et al., 1996, NS-49, an alpha 1A-adrenoceptor agonist, selectively increases intraurethral pressure in dogs., Eur. J. Pharmacol.
Ashford JW, 2019, Treatment of Alzheimer's Disease: Trazodone, Sleep, Serotonin, Norepinephrine, and Future Directions., J Alzheimers Dis
Spiller et al., 2008, Prolonged cardiovascular effects after unintentional ingestion of tetrahydrozoline., Clin Toxicol (Phila)
Suzuki et al., 1990, Two pharmacologically distinct alpha 1-adrenoceptor subtypes in the contraction of rabbit aorta: each subtype couples with a different Ca2+ signalling mechanism and plays a different physiological role., Mol. Pharmacol.
Sallés et al., 1996, Sustained increase in rat myocardial alpha 1A-adrenoceptors induced by 6-hydroxydopamine treatment involves a decelerated receptor turnover., Naunyn Schmiedebergs Arch. Pharmacol.
Michel et al., 1994, Functional studies on alpha 1-adrenoceptor subtypes mediating inotropic effects in rat right ventricle., Br. J. Pharmacol.
Stam et al., 1999, Analysis of alpha 1L-adrenoceptor pharmacology in rat small mesenteric artery., Br. J. Pharmacol.
Yu et al., 2003, Functional characterization of alpha-adrenoceptors mediating pupillary dilation in rats., Eur. J. Pharmacol.
Berman et al., 2000, The Protein Data Bank., Nucleic Acids Res.
Ma et al., 2007, Pharmacological effects of ephedrine alkaloids on human alpha(1)- and alpha(2)-adrenergic receptor subtypes., J. Pharmacol. Exp. Ther.
Wellman et al., 2003, Noradrenergic modulation of ephedrine-induced hypophagia., Synapse
Statler AK et al., 2020, Ephedrine,
Scatton et al., 2001, The preclinical pharmacologic profile of tiapride., Eur. Psychiatry
Lam, 2000, Clinical pharmacology of dopamine agonists., Pharmacotherapy
Gibson A et al., 1979, The effects of bromocriptine on pre-synaptic and post-synaptic alpha-adrenoceptors in the mouse vas deferens., J Pharm Pharmacol
Cohen, Risperidone., Pharmacotherapy
Megens et al., 1994, Survey on the pharmacodynamics of the new antipsychotic risperidone., Psychopharmacology (Berl.)
Ferry DG et al., 1986, Interaction between antidepressants and alpha 1-adrenergic receptor antagonists on the binding to alpha 1-acid glycoprotein., J Pharm Sci
Fujinaga et al., 1994, Receptor subtype and intracellular signal transduction pathway associated with situs inversus induced by alpha 1 adrenergic stimulation in rat embryos., Dev. Biol.
Zhang Y et al., 2009, Arg347Cys polymorphism of alpha1A-adrenoceptor gene is associated with blood pressure response to nifedipine GITS in Chinese hypertensive patients., J Hum Genet
Leung JY et al., 2012, Cardiovascular side-effects of antipsychotic drugs: the role of the autonomic nervous system., Pharmacol Ther
Kim DH et al., 2009, Building a better antipsychotic: receptor targets for the treatment of multiple symptom dimensions of schizophrenia., Neurotherapeutics
Görnemann et al., 2008, Pharmacological properties of a wide array of ergolines at functional alpha(1)-adrenoceptor subtypes., Naunyn Schmiedebergs Arch. Pharmacol.
Dupont et al., 1996, Epinastine (WAL 801CL) modulates the noncholinergic contraction in guinea-pig airways in vitro by a prejunctional 5-HT1-like receptor., Eur. Respir. J.
POWE CE et al., 1962, Propiomazine hydrochloride in obstetrical analgesia. A controlled study of 520 patients., JAMA
Stahl, 2008, Selective histamine H1 antagonism: novel hypnotic and pharmacologic actions challenge classical notions of antihistamines., CNS Spectr
Green et al., 2004, Focus on levomepromazine., Curr Med Res Opin
Dahl et al., 1986, Phenothiazine drugs and metabolites: molecular conformation and dopaminergic, alpha adrenergic and muscarinic cholinergic receptor binding., Biochem. Pharmacol.
Rothman et al., 2006, Therapeutic potential of monoamine transporter substrates., Curr Top Med Chem
Bray, 2005, Drug Insight: appetite suppressants., Nat Clin Pract Gastroenterol Hepatol
Bray, 2000, A concise review on the therapeutics of obesity., Nutrition
Teskin et al., 2006, Comparative effects of tolazoline and nitroprusside on human isolated radial artery., Ann. Thorac. Surg.
Song et al., 1998, [Effects of some mexiletine derivatives on alpha 1-adrenoceptors]., Yao Xue Xue Bao
Khalifa, 2003, Zuclopenthixol facilitates memory retrieval in rats: possible involvement of noradrenergic and serotonergic mechanisms., Pharmacol. Biochem. Behav.
Satoh et al., 1994, Alpha 1-adrenoceptor subtypes mediating the regulation and modulation of Ca2+ sensitization in rabbit thoracic aorta., Eur. J. Pharmacol.
Hoang et al., 1996, Characterization of alpha-adrenoceptor activity in the preterm piglet mesentery., J. Pediatr. Surg.
Sattar et al., 1994, Evidence for an alpha 1-adrenoceptor subtype mediating adrenergic vasoconstriction in Wistar normotensive and stroke-prone spontaneously hypertensive rat kidney., J. Cardiovasc. Pharmacol.
Piascik et al., 1991, Evidence for a complex interaction between the subtypes of the alpha 1-adrenoceptor., Eur. J. Pharmacol.
Haenisch et al., 2010, Alpha-adrenoceptor agonistic activity of oxymetazoline and xylometazoline., Fundam Clin Pharmacol
de Bartolomeis A et al., 2015, Update on the Mechanism of Action of Aripiprazole: Translational Insights into Antipsychotic Strategies Beyond Dopamine Receptor Antagonism., CNS Drugs
Foglar R et al., 1995, Use of recombinant alpha 1-adrenoceptors to characterize subtype selectivity of drugs for the treatment of prostatic hypertrophy., Eur J Pharmacol
Forray C et al., 1994, The alpha 1-adrenergic receptor that mediates smooth muscle contraction in human prostate has the pharmacological properties of the cloned human alpha 1c subtype., Mol Pharmacol
Berger et al., 1996, Trimipramine: a challenge to current concepts on antidepressives., Eur Arch Psychiatry Clin Neurosci
Millan et al., 2002, Differential actions of antiparkinson agents at multiple classes of monoaminergic receptor. I. A multivariate analysis of the binding profiles of 14 drugs at 21 native and cloned human receptor subtypes., J. Pharmacol. Exp. Ther.
Wei et al., 1990, [Comparison of the affinities of amoxapine and loxapine for various receptors in rat brain and the receptor down-regulation after chronic administration]., Yao Xue Xue Bao
George et al., 2013, Newer antipsychotics and upcoming molecules for schizophrenia., Eur. J. Clin. Pharmacol.
Zhu et al., 2010, Update of TTD: Therapeutic Target Database., Nucleic Acids Res.
Gibson et al., 1988, Agonist profile of ergometrine (ergonovine) on a population of postsynaptic alpha-adrenoceptors., J. Pharm. Pharmacol.
Ruffolo et al., 1982, Receptor interactions of imidazolines. IX. Cirazoline is an alpha-1 adrenergic agonist and an alpha-2 adrenergic antagonist., J. Pharmacol. Exp. Ther.
Horie et al., 1995, Selectivity of the imidazoline alpha-adrenoceptor agonists (oxymetazoline and cirazoline) for human cloned alpha 1-adrenoceptor subtypes., Br. J. Pharmacol.
Reisine et al., 1980, Effects of combined administration of amphetamine and iprindole on brain adrenergic receptors., Brain Res.
Leibowitz, 1970, Reciprocal hunger-regulating circuits involving alpha- and beta-adrenergic receptors located, respectively, in the ventromedial and lateral hypothalamus., Proc. Natl. Acad. Sci. U.S.A.
Shayegan DK et al., 2004, Atypical antipsychotics: matching receptor profile to individual patient's clinical profile., CNS Spectr
Li X et al., 2000, Novel arylpiperazines as selective alpha1-adrenergic receptor antagonists., Bioorg Med Chem Lett
Thayer et al., 1985, Effects of dihydropyridine calcium channel blocking drugs on rat brain muscarinic and alpha-adrenergic receptors., Biochem. Pharmacol.
Miyoshi K et al., 1996, Regional vascular effects of MPC-1304, a novel dihydropyridine derivative, in conscious normotensive and spontaneously hypertensive rats., J Pharmacol Exp Ther
Mylecharane EJ, 1991, 5-HT2 receptor antagonists and migraine therapy., J Neurol
Ruffolo RR Jr et al., 1981, Alpha and beta adrenergic effects of the stereoisomers of dobutamine., J Pharmacol Exp Ther
Kishi T et al., 2013, Efficacy and tolerability of perospirone in schizophrenia: a systematic review and meta-analysis of randomized controlled trials., CNS Drugs
Howland RH, 2015, Buspirone: Back to the Future., J Psychosoc Nurs Ment Health Serv
Isah AO et al., 1991, Clinical pharmacology of prochlorperazine in healthy young males., Br J Clin Pharmacol
Huang YT et al., 2001, Hemodynamic effects of synephrine treatment in portal hypertensive rats., Jpn J Pharmacol
Schotte et al., 1996, Risperidone compared with new and reference antipsychotic drugs: in vitro and in vivo receptor binding., Psychopharmacology (Berl.)
Kroeze et al., 2003, H1-histamine receptor affinity predicts short-term weight gain for typical and atypical antipsychotic drugs., Neuropsychopharmacology
Kvernmo et al., 2008, Receptor-binding and pharmacokinetic properties of dopaminergic agonists., Curr Top Med Chem
Shill HA et al., 2009, Update on ropinirole in the treatment of Parkinson's disease., Neuropsychiatr Dis Treat
Coppi G, 1992, [Dihydroergocristine. A review of pharmacology and toxicology]., Arzneimittelforschung
Shibata K et al., 1998, Effects of quinidine and verapamil on human cardiovascular alpha1-adrenoceptors., Circulation
Thomas DR et al., 1987, Biochemical effects of the antidepressant paroxetine, a specific 5-hydroxytryptamine uptake inhibitor., Psychopharmacology (Berl)
Abelaira HM et al., 2012, Lamotrigine treatment reverses depressive-like behavior and alters BDNF levels in the brains of maternally deprived adult rats., Pharmacol Biochem Behav
Wand M et al., 1980, Thymoxamine hydrochloride: an alpha-adrenergic blocker., Surv Ophthalmol
Rayner-Hartley E et al., 2016, Ranolazine: A Contemporary Review., J Am Heart Assoc
Virsolvy A et al., 2015, Antagonism of Nav channels and α1-adrenergic receptors contributes to vascular smooth muscle effects of ranolazine., Sci Rep
Zhao G et al., 2011, Antiadrenergic and hemodynamic effects of ranolazine in conscious dogs., J Cardiovasc Pharmacol
Jarema M et al., 2011, [Trazodon--the antidepressant: mechanism of action and its position in the treatment of depression]., Psychiatr Pol
Takayanagi I et al., 1991, Differences in alpha 1-adrenoceptor mechanisms for phenylephrine and tizanidine in rabbit thoracic aorta and common iliac artery., Can J Physiol Pharmacol
Takayanagi I et al., 1984, Actions of tizanidine on alpha 1-and alpha 2-adrenoceptors in the peripheral tissues., Gen Pharmacol

PHENYLEPHRINE ADRA1A

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Specific Action of the Ligand Full agonist

Endogenous Drug? False

Direct Interaction? True

Publications:

Martínez-Salas et al., 2007, Alpha1A-adrenoceptors predominate in the control of blood pressure in mouse mesenteric vascular bed., Auton Autacoid Pharmacol

Tomiyama et al., 2007, Expressions and mechanical functions of alpha1-adrenoceptor subtypes in hamster ureter., Eur. J. Pharmacol.

PHENTOLAMINE ADRA1A

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Trial Name aviptadil,Invicorp

Novel drug target Established target

Specific Action of the Ligand Antagonist

Publications:

Saeed et al., Alpha-adrenoceptor blockade by phentolamine causes beta-adrenergic vasodilation by increased catecholamine release due to presynaptic alpha-blockade., J. Cardiovasc. Pharmacol.

Giussani et al., 1995, Alpha 1- and alpha 2-adrenoreceptor actions of phentolamine and prazosin on breathing movements in fetal sheep in utero., J. Physiol. (Lond.)

Bylund, 1992, Subtypes of alpha 1- and alpha 2-adrenergic receptors., FASEB J.

SILODOSIN ADRA1A

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Mechanism of Interaction Alpha-1a adrenergic receptor antagonist

Direct Interaction yes

Novel drug target Established target

Publications:

Lepor et al., 2010, Silodosin for the treatment of benign prostatic hyperplasia: pharmacology and cardiovascular tolerability., Pharmacotherapy

OLANZAPINE ADRA1A

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Trial Name ALKS 3831

Trial Name OREX-003, olanzapine plus zonisamide SR

Trial Name Olanzapine/fluoxetine combination,Symbyax (Zyprexa/Prozac)

Publications:

Nasrallah, 2008, Atypical antipsychotic-induced metabolic side effects: insights from receptor-binding profiles., Mol. Psychiatry

Bymaster et al., 1999, Antagonism by olanzapine of dopamine D1, serotonin2, muscarinic, histamine H1 and alpha 1-adrenergic receptors in vitro., Schizophr. Res.

Brafford MV et al., 2014, Olanzapine: an antiemetic option for chemotherapy-induced nausea and vomiting., J Adv Pract Oncol

PHENYLEPHRINE BITARTRATE ADRA1A

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Mechanism of Interaction Adrenergic receptor alpha-1 agonist

Direct Interaction yes

Publications:
PHENTOLAMINE MESYLATE ADRA1A

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Mechanism of Interaction Adrenergic receptor alpha antagonist

Direct Interaction yes

Publications:
TERAZOSIN HYDROCHLORIDE HYDRATE ADRA1A

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Adrenergic receptor alpha-1 antagonist

Publications:
NAPHAZOLINE HYDROCHLORIDE ADRA1A

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Adrenergic receptor alpha agonist

Publications:
MEPHENTERMINE SULFATE ADRA1A

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Mechanism of Interaction Adrenergic receptor agonist

Direct Interaction yes

Publications:
HYDROXYAMPHETAMINE HYDROBROMIDE ADRA1A

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Adrenergic receptor agonist

Publications:
MIDODRINE HYDROCHLORIDE ADRA1A

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Adrenergic receptor alpha-1 agonist

Publications:
METARAMINOL BITARTRATE ADRA1A

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Mechanism of Interaction Adrenergic receptor alpha-1 agonist

Direct Interaction yes

Publications:
TAMSULOSIN HYDROCHLORIDE ADRA1A

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Mechanism of Interaction Adrenergic receptor alpha-1 antagonist

Direct Interaction yes

Publications:
TERGURIDE ADRA1A

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Specific Action of the Ligand Antagonist

Endogenous Drug? False

Publications:
TRIMIPRAMINE MALEATE ADRA1A

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Adrenergic receptor alpha-1 antagonist

Publications:
RAUWOLFIA SERPENTINA ADRA1A

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Mechanism of Interaction Adrenergic receptor alpha antagonist

Direct Interaction yes

Publications:
KETANSERIN ADRA1A

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Specific Action of the Ligand Antagonist

Endogenous Drug? False

Publications:
PRAZOSIN HYDROCHLORIDE ADRA1A

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Adrenergic receptor alpha-1 antagonist

Publications:
NOREPINEPHRINE BITARTRATE ADRA1A

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Mechanism of Interaction Adrenergic receptor agonist

Direct Interaction yes

Publications:
chembl:CHEMBL56331 ADRA1A

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Direct Interaction? False

Endogenous Drug? False

Specific Action of the Ligand Antagonist

Publications:
METHOXAMINE HYDROCHLORIDE ADRA1A

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Mechanism of Interaction Adrenergic receptor alpha-1 agonist

Direct Interaction yes

Publications:
PIRIBEDIL ADRA1A

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Specific Action of the Ligand Antagonist

Endogenous Drug? False

Publications:
RITANSERIN ADRA1A

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Specific Action of the Ligand Antagonist

Endogenous Drug? False

Publications:
DIPIVEFRIN HYDROCHLORIDE ADRA1A

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Mechanism of Interaction Adrenergic receptor agonist

Direct Interaction yes

Publications:
ALFUZOSIN HYDROCHLORIDE ADRA1A

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Mechanism of Interaction Adrenergic receptor alpha-1 agonist

Direct Interaction yes

Publications:
ERGOLOID MESYLATES ADRA1A

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Mechanism of Interaction Adrenergic receptor alpha antagonist

Direct Interaction yes

Publications:
EPINEPHRINE BITARTRATE ADRA1A

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Adrenergic receptor agonist

Publications:
LABETALOL HYDROCHLORIDE ADRA1A

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Mechanism of Interaction Adrenergic receptor antagonist

Direct Interaction yes

Publications:
SPIPERONE ADRA1A

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Specific Action of the Ligand Antagonist

Endogenous Drug? False

Publications:
MIANSERIN ADRA1A

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Specific Action of the Ligand Antagonist

Endogenous Drug? False

Publications:
PHENYLEPHRINE HYDROCHLORIDE ADRA1A

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Mechanism of Interaction Adrenergic receptor alpha-1 agonist

Direct Interaction yes

Publications:
PHENOXYBENZAMINE HYDROCHLORIDE ADRA1A

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Mechanism of Interaction Adrenergic receptor alpha antagonist

Direct Interaction yes

Publications:
UPIDOSIN ADRA1A

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Endogenous Drug? False

Specific Action of the Ligand Antagonist

Publications:
ALSEROXYLON ADRA1A

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Mechanism of Interaction Adrenergic receptor alpha antagonist

Direct Interaction yes

Publications:
DOXAZOSIN MESYLATE ADRA1A

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Mechanism of Interaction Adrenergic receptor alpha-1 antagonist

Direct Interaction yes

Publications:
TOLAZOLINE HYDROCHLORIDE ADRA1A

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Adrenergic receptor alpha antagonist

Publications:
DABUZALGRON ADRA1A

Interaction Types & Directionality:

agonist (activating)

partial agonist (activating)

Interaction Info:

Specific Action of the Ligand Agonist

Endogenous Drug? False

Direct Interaction yes

Publications:
CARVEDILOL PHOSPHATE ADRA1A

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Mechanism of Interaction Adrenergic receptor alpha-1 antagonist

Direct Interaction yes

Publications:
A-123189 ADRA1A

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Specific Action of the Ligand Antagonist

Endogenous Drug? False

Publications:
DAPIPRAZOLE HYDROCHLORIDE ADRA1A

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Mechanism of Interaction Alpha-1a adrenergic receptor antagonist

Direct Interaction yes

Publications:
ROXINDOLE ADRA1A

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Specific Action of the Ligand Antagonist

Endogenous Drug? False

Publications:
chembl:CHEMBL88272 ADRA1A

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Specific Action of the Ligand Antagonist

Endogenous Drug? False

Direct Interaction? False

Publications:
SPIROXATRINE ADRA1A

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Specific Action of the Ligand Antagonist

Endogenous Drug? False

Publications:
TEDATIOXETINE ADRA1A

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Alpha-1a adrenergic receptor antagonist

Trial Name Lu AA24530

Publications:
PHENYLPROPANOLAMINE HYDROCHLORIDE ADRA1A

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Mechanism of Interaction Alpha-1a adrenergic receptor agonist

Direct Interaction yes

Publications:
BMY-7378 ADRA1A

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Specific Action of the Ligand Antagonist

Endogenous Drug? False

Publications:
A-119637 ADRA1A

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Specific Action of the Ligand Antagonist

Endogenous Drug? False

Publications:
PHENYLPROPANOLAMINE POLISTIREX ADRA1A

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Mechanism of Interaction Alpha-1a adrenergic receptor agonist

Direct Interaction yes

Publications:
CYPROHEPTADINE ADRA1A

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Specific Action of the Ligand Antagonist

Endogenous Drug? False

Publications:
NS-49 ADRA1A

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Specific Action of the Ligand Partial agonist

Endogenous Drug? False

Publications:
OXYMETAZOLINE HYDROCHLORIDE ADRA1A

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Mechanism of Interaction Adrenergic receptor alpha agonist

Direct Interaction yes

Publications:
LISURIDE ADRA1A

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Specific Action of the Ligand Antagonist

Endogenous Drug? False

Publications:
ASENAPINE ADRA1A

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Trial Name Asenapine

Novel drug target Established target

Publications:

Shahid et al., 2009, Asenapine: a novel psychopharmacologic agent with a unique human receptor signature., J. Psychopharmacol. (Oxford)

OXYMETAZOLINE ADRA1A

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Specific Action of the Ligand Full agonist

Endogenous Drug? False

Direct Interaction? True

Publications:

González-Espinosa et al., 2001, Molecular cloning and functional expression of the guinea pig alpha(1a)-adrenoceptor., Eur. J. Pharmacol.

Yang et al., 1996, (+/-)-tamsulosin, an alpha 1A-adrenoceptor antagonist, inhibits the positive inotropic effect but not the accumulation of inositol phosphates in rabbit heart., Eur. J. Pharmacol.

Shibata et al., 2001, [Excitatory effect of noradrenaline on rat airway parasympathetic ganglion neurons]., Fukuoka Igaku Zasshi

CLOZAPINE ADRA1A

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Specific Action of the Ligand Antagonist

Endogenous Drug? False

Publications:

Nasrallah, 2008, Atypical antipsychotic-induced metabolic side effects: insights from receptor-binding profiles., Mol. Psychiatry

RISPERIDONE ADRA1A

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Specific Action of the Ligand Antagonist

Endogenous Drug? False

Publications:

Nourian et al., 2008, Orthostatic hypotensive effect of antipsychotic drugs in Wistar rats by in vivo and in vitro studies of alpha1-adrenoceptor function., Psychopharmacology (Berl.)

Eltze, 1996, In functional experiments, risperidone is selective, not for the B, but for the A subtype of alpha 1-adrenoceptors., Eur. J. Pharmacol.

Keks et al., 1999, Risperidone (Risperdal): clinical experience with a new antipsychosis drug., Expert Opin Investig Drugs

PHENYLPROPANOLAMINE ADRA1A

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Novel drug target Established target

Trial Name -

Publications:

Moya-Huff et al., 1987, Adrenergic receptor subtype activation by (+)-, (-)- and (+/-)-norephedrine in the pithed rat., J. Pharm. Pharmacol.

Buckner et al., 2002, ABT-866, a novel alpha(1A)-adrenoceptor agonist with antagonist properties at the alpha(1B)- and alpha(1D)-adrenoceptor subtypes., Eur. J. Pharmacol.

Altenbach et al., 2004, Synthesis and structure-activity studies on N-[5-(1H-imidazol-4-yl)-5,6,7,8-tetrahydro-1-naphthalenyl]methanesulfonamide, an imidazole-containing alpha(1A)-adrenoceptor agonist., J. Med. Chem.

CHLORPROMAZINE ADRA1A

Interaction Types & Directionality:

antagonist (inhibitory)

inhibitor (inhibitory)

Interaction Info:

Publications:

Huerta-Bahena et al., 1983, Trifluoperazine and chlorpromazine antagonize alpha 1- but not alpha2- adrenergic effects., Mol. Pharmacol.

Cahir et al., 2005, Antipsychotics lack alpha 1A/B adrenoceptor subtype selectivity in the rat., Eur Neuropsychopharmacol

TERAZOSIN ADRA1A

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Trial Name -

Novel drug target Established target

Specific Action of the Ligand Antagonist

Publications:

Michel et al., 1996, Drugs for treatment of benign prostatic hyperplasia: affinity comparison at cloned alpha 1-adrenoceptor subtypes and in human prostate., J Auton Pharmacol

Lee et al., 1997, Clinical comparison of selective and non-selective alpha 1A-adrenoreceptor antagonists in benign prostatic hyperplasia: studies on tamsulosin in a fixed dose and terazosin in increasing doses., Br J Urol

Na et al., 1998, Clinical comparison of selective and non-selective alpha 1A-adrenoceptor antagonists for bladder outlet obstruction associated with benign prostatic hyperplasia: studies on tamsulosin and terazosin in Chinese patients. The Chinese Tamsulosin Study Group., J Med

CLONIDINE ADRA1A

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Publications:

Millan MJ et al., 2000, S18616, a highly potent, spiroimidazoline agonist at alpha(2)-adrenoceptors: I. Receptor profile, antinociceptive and hypothermic actions in comparison with dexmedetomidine and clonidine., J Pharmacol Exp Ther

APRACLONIDINE ADRA1A

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Publications:

Kawasaki et al., 2008, False negative apraclonidine test in two patients with Horner syndrome., Klin Monbl Augenheilkd

Sueke et al., 2010, Using apraclonidine in diagnosing Horner syndrome in children., Am. J. Ophthalmol.

Mirzai et al., 2006, Congenital Horner's syndrome and the usefulness of the apraclonidine test in its diagnosis., Indian J Ophthalmol

NEFAZODONE ADRA1A

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Novel drug target Established target

Trial Name -

Publications:

Cusack et al., 1994, Binding of antidepressants to human brain receptors: focus on newer generation compounds., Psychopharmacology (Berl.)

Taylor et al., 1995, Pharmacology and neurochemistry of nefazodone, a novel antidepressant drug., J Clin Psychiatry

MIRTAZAPINE ADRA1A

Interaction Types & Directionality:

binder

antagonist (inhibitory)

Interaction Info:

Publications:

Millan et al., 2000, Mirtazapine enhances frontocortical dopaminergic and corticolimbic adrenergic, but not serotonergic, transmission by blockade of alpha2-adrenergic and serotonin2C receptors: a comparison with citalopram., Eur. J. Neurosci.

de Boer et al., 1988, Neurochemical and autonomic pharmacological profiles of the 6-aza-analogue of mianserin, Org 3770 and its enantiomers., Neuropharmacology

Wikström et al., 2002, Synthesis and pharmacological testing of 1,2,3,4,10,14b-hexahydro-6-methoxy-2-methyldibenzo[c,f]pyrazino[1,2-a]azepin and its enantiomers in comparison with the two antidepressants mianserin and mirtazapine., J. Med. Chem.

DROXIDOPA ADRA1A

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Adrenergic receptor agonist

Publications:

Senard et al., 2001, Orthostatic hypotension in patients with Parkinson's disease: pathophysiology and management., Drugs Aging

Lachnit et al., 1997, Pharmacological characterization of an alpha 1A-adrenoceptor mediating contractile responses to noradrenaline in isolated caudal artery of rat., Br. J. Pharmacol.

Du et al., 2010, Modeling the interactions between alpha(1)-adrenergic receptors and their antagonists., Curr Comput Aided Drug Des

PRAZOSIN ADRA1A

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Trial Name -

Novel drug target Established target

Specific Action of the Ligand Inverse agonist

Publications:

Cusack et al., 1994, Binding of antidepressants to human brain receptors: focus on newer generation compounds., Psychopharmacology (Berl.)

Morris et al., 2004, Cellular trafficking of human alpha1a-adrenergic receptors is continuous and primarily agonist-independent., Mol. Pharmacol.

Suzuki et al., 2000, Effect of JTH-601, a novel alpha(1)-adrenoceptor antagonist, on prostate function in dogs., Eur. J. Pharmacol.

ZIPRASIDONE ADRA1A

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Publications:

Andersohn et al., 2010, Priapism associated with antipsychotics: role of alpha1 adrenoceptor affinity., J Clin Psychopharmacol

Nasrallah, 2008, Atypical antipsychotic-induced metabolic side effects: insights from receptor-binding profiles., Mol. Psychiatry

EPINEPHRINE ADRA1A

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Mechanism of Interaction Adrenergic receptor agonist

Direct Interaction yes

Trial Name transdermal lidocaine/epinephrine patch,Lidosite

Publications:

Jensen et al., 2010, Functional alpha-1B adrenergic receptors on human epicardial coronary artery endothelial cells., Naunyn Schmiedebergs Arch. Pharmacol.

Sanbe et al., 2007, Alpha1-adrenoceptors are required for normal male sexual function., Br. J. Pharmacol.

Tomiyama et al., 2007, Expressions and mechanical functions of alpha1-adrenoceptor subtypes in hamster ureter., Eur. J. Pharmacol.

NOREPINEPHRINE ADRA1A

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Trial Name -

Novel drug target Established target

Publications:

Bishop, 2007, Recent advances in the discovery of alpha1-adrenoceptor agonists., Curr Top Med Chem

Lachnit et al., 1997, Pharmacological characterization of an alpha 1A-adrenoceptor mediating contractile responses to noradrenaline in isolated caudal artery of rat., Br. J. Pharmacol.

Burt et al., 1996, The role of diacylglycerol and activation of protein kinase C in alpha 1A-adrenoceptor-mediated contraction to noradrenaline of rat isolated epididymal vas deferens., Br. J. Pharmacol.

DESIPRAMINE ADRA1A

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Publications:

Cusack et al., 1994, Binding of antidepressants to human brain receptors: focus on newer generation compounds., Psychopharmacology (Berl.)
FENOLDOPAM ADRA1A

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Publications:

Martin et al., 1995, Renal vasodilatation by dopexamine and fenoldopam due to alpha 1-adrenoceptor blockade., Br. J. Pharmacol.

MEPHENTERMINE ADRA1A

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Novel drug target Established target

Trial Name -

Publications:

Ahlquist, 1976, Present state of alpha- and beta-adrenergic drugs I. The adrenergic receptor., Am. Heart J.

Mohta et al., 2010, Comparison of phenylephrine hydrochloride and mephentermine sulphate for prevention of post spinal hypotension., Anaesthesia

NICERGOLINE ADRA1A

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Novel drug target Established target

Trial Name -

Publications:

Alvarez-Guerra et al., 1999, Selective blockade by nicergoline of vascular responses elicited by stimulation of alpha 1A-adrenoceptor subtype in the rat., Fundam Clin Pharmacol

NAPHAZOLINE ADRA1A

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Publications:

Hrometz et al., 1999, Expression of multiple alpha1-adrenoceptors on vascular smooth muscle: correlation with the regulation of contraction., J. Pharmacol. Exp. Ther.

Bogacka, 1999, [Decongestants in treatment of nasal obstruction]., Otolaryngol Pol

Leonardi, 2005, Emerging drugs for ocular allergy., Expert Opin Emerg Drugs

PROMETHAZINE ADRA1A

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Publications:

Imming et al., 2006, Drugs, their targets and the nature and number of drug targets., Nat Rev Drug Discov

Overington et al., 2006, How many drug targets are there?, Nat Rev Drug Discov

Southard BT et al., 2020, Promethazine,

METARAMINOL ADRA1A

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Trial Name -

Novel drug target Established target

Publications:

Tatsuta et al., 1998, Alpha1-adrenoceptor stimulation enhances experimental gastric carcinogenesis induced by N-methyl-N'-nitro-N-nitrosoguanidine in Wistar rats., Int. J. Cancer

Imming et al., 2006, Drugs, their targets and the nature and number of drug targets., Nat Rev Drug Discov

Overington et al., 2006, How many drug targets are there?, Nat Rev Drug Discov

DRONEDARONE ADRA1A

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Trial Name -

Novel drug target Established target

Publications:

Dale et al., 2007, Dronedarone: an amiodarone analog for the treatment of atrial fibrillation and atrial flutter., Ann Pharmacother

Heijman J et al., 2013, Pleiotropic effects of antiarrhythmic agents: dronedarone in the treatment of atrial fibrillation., Clin Med Insights Cardiol

PSEUDOEPHEDRINE ADRA1A

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Trial Name fexofenadine + ps/

Novel drug target Established target

Publications:

Wellington et al., 2001, Cetirizine/pseudoephedrine., Drugs

Imming et al., 2006, Drugs, their targets and the nature and number of drug targets., Nat Rev Drug Discov

Overington et al., 2006, How many drug targets are there?, Nat Rev Drug Discov

LABETALOL ADRA1A

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Trial Name -

Novel drug target Established target

Publications:

Nakamura et al., 1999, Tamsulosin: assessment of affinityof (3)H-P razosin binding to two alpha-1- adrenoceptor subtypes in the canine aorta., Pharmacology

Rosendorff, 1993, Beta-blocking agents with vasodilator activity., J Hypertens Suppl

Bernstein et al., 1989, Partial attenuation of hemodynamic responses to rapid sequence induction and intubation with labetalol., J Clin Anesth

DAPIPRAZOLE ADRA1A

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Trial Name -

Novel drug target Established target

Publications:

Imming et al., 2006, Drugs, their targets and the nature and number of drug targets., Nat Rev Drug Discov

Overington et al., 2006, How many drug targets are there?, Nat Rev Drug Discov

Eltze, 1997, Affinity of the miotic drug, dapiprazole, at alpha 1-adrenoceptor subtypes A, B and D., J. Pharm. Pharmacol.

TAMSULOSIN ADRA1A

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Trial Name dutasteride + tamsulosin,Jalyn

Novel drug target Established target

Trial Name tamsulosin, YM-617,Harnal, Flomax

Publications:

Abrams et al., 1997, A dose-ranging study of the efficacy and safety of tamsulosin, the first prostate-selective alpha 1A-adrenoceptor antagonist, in patients with benign prostatic obstruction (symptomatic benign prostatic hyperplasia)., Br J Urol

Lee et al., 1997, Clinical comparison of selective and non-selective alpha 1A-adrenoreceptor antagonists in benign prostatic hyperplasia: studies on tamsulosin in a fixed dose and terazosin in increasing doses., Br J Urol

Michel et al., 2004, Efficacy and safety of tamsulosin in the treatment of urological diseases., Expert Opin Pharmacother

MAPROTILINE ADRA1A

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Publications:

Richelson et al., 1984, Antagonism by antidepressants of neurotransmitter receptors of normal human brain in vitro., J. Pharmacol. Exp. Ther.

Buckley et al., 1998, Can the fatal toxicity of antidepressant drugs be predicted with pharmacological and toxicological data?, Drug Saf

ESCITALOPRAM ADRA1A

Interaction Types & Directionality:

antagonist (inhibitory)

inhibitor (inhibitory)

Interaction Info:

Publications:

Fabre et al., [Mechanisms of action of antidepressants: new data from Escitalopram]., Encephale

Bareggi et al., 2007, The use of escitalopram beyond major depression: pharmacological aspects, efficacy and tolerability in anxiety disorders., Expert Opin Drug Metab Toxicol

Sanchez C et al., 2014, A comparative review of escitalopram, paroxetine, and sertraline: Are they all alike?, Int Clin Psychopharmacol

DROPERIDOL ADRA1A

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Publications:

Zupkó et al., 2003, Alpha-adrenergic blockade: a possible mechanism of tocolytic action of certain benzodiazepines in a postpartum rat model in vivo., Life Sci.

BENZPHETAMINE ADRA1A

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Trial Name -

Novel drug target Established target

Publications:

Imming et al., 2006, Drugs, their targets and the nature and number of drug targets., Nat Rev Drug Discov

Overington et al., 2006, How many drug targets are there?, Nat Rev Drug Discov

Spencer RC et al., 2015, The cognition-enhancing effects of psychostimulants involve direct action in the prefrontal cortex., Biol Psychiatry

ALFUZOSIN ADRA1A

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Trial Name alfuzosin,UroXatral

Novel drug target Established target

Specific Action of the Ligand Antagonist

Publications:

Bèïque et al., 1998, Are the new selective alpha-blockers better than non-selective alpha-blockers for benign prostatic hyperplasia?, Can Fam Physician

Elhilali, 2006, Alfuzosin: an alpha1-receptor blocker for the treatment of lower urinary tract symptoms associated with benign prostatic hyperplasia., Expert Opin Pharmacother

Faure et al., 1994, Identification of alpha 1-adrenoceptor subtypes present in the human prostate., Life Sci.

DOXAZOSIN ADRA1A

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Specific Action of the Ligand Antagonist

Endogenous Drug? False

Direct Interaction? True

Publications:

Michel et al., 1996, Drugs for treatment of benign prostatic hyperplasia: affinity comparison at cloned alpha 1-adrenoceptor subtypes and in human prostate., J Auton Pharmacol

Greco et al., 2008, The role of combination medical therapy in benign prostatic hyperplasia., Int. J. Impot. Res.

Shannon et al., 2006, Effect of alpha1-adrenergic receptors in cardiac pathophysiology., Am. Heart J.

IMIPRAMINE ADRA1A

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Publications:

Cusack et al., 1994, Binding of antidepressants to human brain receptors: focus on newer generation compounds., Psychopharmacology (Berl.)

Nojimoto et al., The tricyclic antidepressants amitriptyline, nortriptyline and imipramine are weak antagonists of human and rat alpha1B-adrenoceptors., Neuropharmacology

BEVANTOLOL ADRA1A

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Publications:

Shiraishi et al., 1992, Alpha 1-adrenoceptor blocking activities of bevantolol hydrochloride(NC-1400) and labetalol in rat isolated thoracic aorta--do they distinguish between subtypes?, Gen. Pharmacol.

THIORIDAZINE ADRA1A

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Trial Name -

Novel drug target Established target

Publications:

Sleight et al., 1993, Binding of antipsychotic drugs at alpha 1A- and alpha 1B-adrenoceptors: risperidone is selective for the alpha 1B-adrenoceptors., Eur. J. Pharmacol.

Cahir et al., 2005, Antipsychotics lack alpha 1A/B adrenoceptor subtype selectivity in the rat., Eur Neuropsychopharmacol

CARVEDILOL ADRA1A

Interaction Types & Directionality:

antagonist (inhibitory)

potentiator

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Adrenergic receptor alpha-1 antagonist

Direct Interaction yes

Trial Name carvedilol, Coreg

Publications:

Imming et al., 2006, Drugs, their targets and the nature and number of drug targets., Nat Rev Drug Discov

Overington et al., 2006, How many drug targets are there?, Nat Rev Drug Discov

O'Connell TD et al., 2013, Cardiac alpha1-adrenergic receptors: novel aspects of expression, signaling mechanisms, physiologic function, and clinical importance., Pharmacol Rev

DEXTROAMPHETAMINE ADRA1A

Interaction Types & Directionality:

inhibitor (inhibitory)

inducer (activating)

Interaction Info:

Publications:

Imming et al., 2006, Drugs, their targets and the nature and number of drug targets., Nat Rev Drug Discov

Overington et al., 2006, How many drug targets are there?, Nat Rev Drug Discov

Shekim WO et al., 1994, Platelet alpha 2-adrenergic receptor binding and the effects of d-amphetamine in boys with attention deficit hyperactivity disorder., Neuropsychobiology

ISOMETHEPTENE ADRA1A

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Publications:

Parker et al., 1988, Comparative effects of amphetamine, phenylethylamine and related drugs on dopamine efflux, dopamine uptake and mazindol binding., J. Pharmacol. Exp. Ther.

Valdivia et al., 2004, Pharmacological analysis of the mechanisms involved in the tachycardic and vasopressor responses to the antimigraine agent, isometheptene, in pithed rats., Life Sci.

MIDODRINE ADRA1A

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Trial Name -

Novel drug target Established target

Publications:

Taniguchi et al., 1996, NS-49, an alpha 1A-adrenoceptor agonist, selectively increases intraurethral pressure in dogs., Eur. J. Pharmacol.

Buckner et al., 2002, ABT-866, a novel alpha(1A)-adrenoceptor agonist with antagonist properties at the alpha(1B)- and alpha(1D)-adrenoceptor subtypes., Eur. J. Pharmacol.

Altenbach et al., 2004, Synthesis and structure-activity studies on N-[5-(1H-imidazol-4-yl)-5,6,7,8-tetrahydro-1-naphthalenyl]methanesulfonamide, an imidazole-containing alpha(1A)-adrenoceptor agonist., J. Med. Chem.

AMITRIPTYLINE ADRA1A

Interaction Types & Directionality:

antagonist (inhibitory)

inhibitor (inhibitory)

Interaction Info:

Publications:

Cusack et al., 1994, Binding of antidepressants to human brain receptors: focus on newer generation compounds., Psychopharmacology (Berl.)

Nojimoto et al., The tricyclic antidepressants amitriptyline, nortriptyline and imipramine are weak antagonists of human and rat alpha1B-adrenoceptors., Neuropharmacology

TRAZODONE ADRA1A

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Publications:

Cusack et al., 1994, Binding of antidepressants to human brain receptors: focus on newer generation compounds., Psychopharmacology (Berl.)

Ashford JW, 2019, Treatment of Alzheimer's Disease: Trazodone, Sleep, Serotonin, Norepinephrine, and Future Directions., J Alzheimers Dis

THIOPROPERAZINE ADRA1A

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Publications:

Cahir et al., 2005, Antipsychotics lack alpha 1A/B adrenoceptor subtype selectivity in the rat., Eur Neuropsychopharmacol
TETRAHYDROZOLINE HYDROCHLORIDE ADRA1A

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Mechanism of Interaction Adrenergic receptor alpha agonist

Direct Interaction yes

Publications:

Spiller et al., 2008, Prolonged cardiovascular effects after unintentional ingestion of tetrahydrozoline., Clin Toxicol (Phila)

PHENOXYBENZAMINE ADRA1A

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Trial Name -

Novel drug target Established target

Publications:

Suzuki et al., 1990, Two pharmacologically distinct alpha 1-adrenoceptor subtypes in the contraction of rabbit aorta: each subtype couples with a different Ca2+ signalling mechanism and plays a different physiological role., Mol. Pharmacol.

Sallés et al., 1996, Sustained increase in rat myocardial alpha 1A-adrenoceptors induced by 6-hydroxydopamine treatment involves a decelerated receptor turnover., Naunyn Schmiedebergs Arch. Pharmacol.

Michel et al., 1994, Functional studies on alpha 1-adrenoceptor subtypes mediating inotropic effects in rat right ventricle., Br. J. Pharmacol.

EPHEDRINE ADRA1A

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Trial Name -

Novel drug target Established target

Publications:

Berman et al., 2000, The Protein Data Bank., Nucleic Acids Res.

Ma et al., 2007, Pharmacological effects of ephedrine alkaloids on human alpha(1)- and alpha(2)-adrenergic receptor subtypes., J. Pharmacol. Exp. Ther.

Wellman et al., 2003, Noradrenergic modulation of ephedrine-induced hypophagia., Synapse

TIAPRIDE ADRA1A

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Publications:

Scatton et al., 2001, The preclinical pharmacologic profile of tiapride., Eur. Psychiatry

BROMOCRIPTINE ADRA1A

Interaction Types & Directionality:

agonist (activating)

antagonist (inhibitory)

Interaction Info:

Publications:

Lam, 2000, Clinical pharmacology of dopamine agonists., Pharmacotherapy

Gibson A et al., 1979, The effects of bromocriptine on pre-synaptic and post-synaptic alpha-adrenoceptors in the mouse vas deferens., J Pharm Pharmacol

PALIPERIDONE ADRA1A

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Publications:

Nourian et al., 2008, Orthostatic hypotensive effect of antipsychotic drugs in Wistar rats by in vivo and in vitro studies of alpha1-adrenoceptor function., Psychopharmacology (Berl.)

Eltze, 1996, In functional experiments, risperidone is selective, not for the B, but for the A subtype of alpha 1-adrenoceptors., Eur. J. Pharmacol.

Keks et al., 1999, Risperidone (Risperdal): clinical experience with a new antipsychosis drug., Expert Opin Investig Drugs

NORTRIPTYLINE ADRA1A

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Publications:

Cusack et al., 1994, Binding of antidepressants to human brain receptors: focus on newer generation compounds., Psychopharmacology (Berl.)

Nojimoto et al., The tricyclic antidepressants amitriptyline, nortriptyline and imipramine are weak antagonists of human and rat alpha1B-adrenoceptors., Neuropharmacology

Ferry DG et al., 1986, Interaction between antidepressants and alpha 1-adrenergic receptor antagonists on the binding to alpha 1-acid glycoprotein., J Pharm Sci

TRIFLUOPERAZINE ADRA1A

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Trial Name -

Novel drug target Established target

Publications:

Huerta-Bahena et al., 1983, Trifluoperazine and chlorpromazine antagonize alpha 1- but not alpha2- adrenergic effects., Mol. Pharmacol.

Imming et al., 2006, Drugs, their targets and the nature and number of drug targets., Nat Rev Drug Discov

Overington et al., 2006, How many drug targets are there?, Nat Rev Drug Discov

PROMAZINE ADRA1A

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Trial Name -

Novel drug target Established target

Publications:

Imming et al., 2006, Drugs, their targets and the nature and number of drug targets., Nat Rev Drug Discov

Overington et al., 2006, How many drug targets are there?, Nat Rev Drug Discov

Leung JY et al., 2012, Cardiovascular side-effects of antipsychotic drugs: the role of the autonomic nervous system., Pharmacol Ther

ERGOTAMINE ADRA1A

Interaction Types & Directionality:

partial agonist (activating)

Interaction Info:

Publications:

Görnemann et al., 2008, Pharmacological properties of a wide array of ergolines at functional alpha(1)-adrenoceptor subtypes., Naunyn Schmiedebergs Arch. Pharmacol.

Imming et al., 2006, Drugs, their targets and the nature and number of drug targets., Nat Rev Drug Discov

Overington et al., 2006, How many drug targets are there?, Nat Rev Drug Discov

PROPIOMAZINE ADRA1A

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Trial Name -

Novel drug target Established target

Publications:

Imming et al., 2006, Drugs, their targets and the nature and number of drug targets., Nat Rev Drug Discov

Overington et al., 2006, How many drug targets are there?, Nat Rev Drug Discov

POWE CE et al., 1962, Propiomazine hydrochloride in obstetrical analgesia. A controlled study of 520 patients., JAMA

DOXEPIN ADRA1A

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Publications:

Cusack et al., 1994, Binding of antidepressants to human brain receptors: focus on newer generation compounds., Psychopharmacology (Berl.)

Richelson et al., 1984, Antagonism by antidepressants of neurotransmitter receptors of normal human brain in vitro., J. Pharmacol. Exp. Ther.

Stahl, 2008, Selective histamine H1 antagonism: novel hypnotic and pharmacologic actions challenge classical notions of antihistamines., CNS Spectr

CITALOPRAM ADRA1A

Interaction Types & Directionality:

binder

Interaction Info:

Publications:

Bareggi et al., 2007, The use of escitalopram beyond major depression: pharmacological aspects, efficacy and tolerability in anxiety disorders., Expert Opin Drug Metab Toxicol

LEVOMEPROMAZINE ADRA1A

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Trial Name -

Novel drug target Established target

Publications:

Green et al., 2004, Focus on levomepromazine., Curr Med Res Opin

Dahl et al., 1986, Phenothiazine drugs and metabolites: molecular conformation and dopaminergic, alpha adrenergic and muscarinic cholinergic receptor binding., Biochem. Pharmacol.

PHENDIMETRAZINE ADRA1A

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Trial Name -

Novel drug target Established target

Publications:

Rothman et al., 2006, Therapeutic potential of monoamine transporter substrates., Curr Top Med Chem

Imming et al., 2006, Drugs, their targets and the nature and number of drug targets., Nat Rev Drug Discov

Overington et al., 2006, How many drug targets are there?, Nat Rev Drug Discov

TOLAZOLINE ADRA1A

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Trial Name -

Novel drug target Established target

Publications:

Teskin et al., 2006, Comparative effects of tolazoline and nitroprusside on human isolated radial artery., Ann. Thorac. Surg.

Imming et al., 2006, Drugs, their targets and the nature and number of drug targets., Nat Rev Drug Discov

Overington et al., 2006, How many drug targets are there?, Nat Rev Drug Discov

DIPIVEFRIN ADRA1A

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Publications:

Sanbe et al., 2007, Alpha1-adrenoceptors are required for normal male sexual function., Br. J. Pharmacol.

Tomiyama et al., 2007, Expressions and mechanical functions of alpha1-adrenoceptor subtypes in hamster ureter., Eur. J. Pharmacol.

PERGOLIDE ADRA1A

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Publications:

Lam, 2000, Clinical pharmacology of dopamine agonists., Pharmacotherapy
ZUCLOPENTHIXOL ADRA1A

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Publications:

Khalifa, 2003, Zuclopenthixol facilitates memory retrieval in rats: possible involvement of noradrenergic and serotonergic mechanisms., Pharmacol. Biochem. Behav.

METHOXAMINE ADRA1A

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Specific Action of the Ligand Full agonist

Endogenous Drug? False

Direct Interaction? True

Publications:

Suzuki et al., 1990, Two pharmacologically distinct alpha 1-adrenoceptor subtypes in the contraction of rabbit aorta: each subtype couples with a different Ca2+ signalling mechanism and plays a different physiological role., Mol. Pharmacol.

Satoh et al., 1994, Alpha 1-adrenoceptor subtypes mediating the regulation and modulation of Ca2+ sensitization in rabbit thoracic aorta., Eur. J. Pharmacol.

Hoang et al., 1996, Characterization of alpha-adrenoceptor activity in the preterm piglet mesentery., J. Pediatr. Surg.

XYLOMETAZOLINE ADRA1A

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Publications:

Yang et al., 1996, (+/-)-tamsulosin, an alpha 1A-adrenoceptor antagonist, inhibits the positive inotropic effect but not the accumulation of inositol phosphates in rabbit heart., Eur. J. Pharmacol.

Haenisch et al., 2010, Alpha-adrenoceptor agonistic activity of oxymetazoline and xylometazoline., Fundam Clin Pharmacol

ARIPIPRAZOLE ADRA1A

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Publications:

Nasrallah, 2008, Atypical antipsychotic-induced metabolic side effects: insights from receptor-binding profiles., Mol. Psychiatry

de Bartolomeis A et al., 2015, Update on the Mechanism of Action of Aripiprazole: Translational Insights into Antipsychotic Strategies Beyond Dopamine Receptor Antagonism., CNS Drugs

INDORAMIN ADRA1A

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Specific Action of the Ligand Antagonist

Endogenous Drug? False

Publications:

Foglar R et al., 1995, Use of recombinant alpha 1-adrenoceptors to characterize subtype selectivity of drugs for the treatment of prostatic hypertrophy., Eur J Pharmacol

Forray C et al., 1994, The alpha 1-adrenergic receptor that mediates smooth muscle contraction in human prostate has the pharmacological properties of the cloned human alpha 1c subtype., Mol Pharmacol

TRIMIPRAMINE ADRA1A

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Publications:

Berger et al., 1996, Trimipramine: a challenge to current concepts on antidepressives., Eur Arch Psychiatry Clin Neurosci

CABERGOLINE ADRA1A

Interaction Types & Directionality:

binder

antagonist (inhibitory)

Interaction Info:

Specific Action of the Ligand Antagonist

Endogenous Drug? False

Publications:

Millan et al., 2002, Differential actions of antiparkinson agents at multiple classes of monoaminergic receptor. I. A multivariate analysis of the binding profiles of 14 drugs at 21 native and cloned human receptor subtypes., J. Pharmacol. Exp. Ther.

AMOXAPINE ADRA1A

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Publications:

Buckley et al., 1998, Can the fatal toxicity of antidepressant drugs be predicted with pharmacological and toxicological data?, Drug Saf

Wei et al., 1990, [Comparison of the affinities of amoxapine and loxapine for various receptors in rat brain and the receptor down-regulation after chronic administration]., Yao Xue Xue Bao

Richelson et al., 1984, Antagonism by antidepressants of neurotransmitter receptors of normal human brain in vitro., J. Pharmacol. Exp. Ther.

ILOPERIDONE ADRA1A

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Trial Name iloperidone,Fanapt, Fiapta, Zomaril

Novel drug target Established target

Publications:

George et al., 2013, Newer antipsychotics and upcoming molecules for schizophrenia., Eur. J. Clin. Pharmacol.
ACEPROMAZINE ADRA1A

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Publications:

Cahir et al., 2005, Antipsychotics lack alpha 1A/B adrenoceptor subtype selectivity in the rat., Eur Neuropsychopharmacol

ERGONOVINE ADRA1A

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Publications:

Zhu et al., 2010, Update of TTD: Therapeutic Target Database., Nucleic Acids Res.

Gibson et al., 1988, Agonist profile of ergometrine (ergonovine) on a population of postsynaptic alpha-adrenoceptors., J. Pharm. Pharmacol.

CIRAZOLINE ADRA1A

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Publications:

Ruffolo et al., 1982, Receptor interactions of imidazolines. IX. Cirazoline is an alpha-1 adrenergic agonist and an alpha-2 adrenergic antagonist., J. Pharmacol. Exp. Ther.

Horie et al., 1995, Selectivity of the imidazoline alpha-adrenoceptor agonists (oxymetazoline and cirazoline) for human cloned alpha 1-adrenoceptor subtypes., Br. J. Pharmacol.

AMPHETAMINE ADRA1A

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Publications:

Reisine et al., 1980, Effects of combined administration of amphetamine and iprindole on brain adrenergic receptors., Brain Res.

Leibowitz, 1970, Reciprocal hunger-regulating circuits involving alpha- and beta-adrenergic receptors located, respectively, in the ventromedial and lateral hypothalamus., Proc. Natl. Acad. Sci. U.S.A.

QUETIAPINE ADRA1A

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Publications:

Richelson et al., 2000, Binding of antipsychotic drugs to human brain receptors focus on newer generation compounds., Life Sci.

Nasrallah, 2008, Atypical antipsychotic-induced metabolic side effects: insights from receptor-binding profiles., Mol. Psychiatry

Shayegan DK et al., 2004, Atypical antipsychotics: matching receptor profile to individual patient's clinical profile., CNS Spectr

FLUPENTIXOL ADRA1A

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Publications:

Imming et al., 2006, Drugs, their targets and the nature and number of drug targets., Nat Rev Drug Discov

Overington et al., 2006, How many drug targets are there?, Nat Rev Drug Discov

Li X et al., 2000, Novel arylpiperazines as selective alpha1-adrenergic receptor antagonists., Bioorg Med Chem Lett

NICARDIPINE ADRA1A

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Publications:

Thayer et al., 1985, Effects of dihydropyridine calcium channel blocking drugs on rat brain muscarinic and alpha-adrenergic receptors., Biochem. Pharmacol.
ARANIDIPINE ADRA1A

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Publications:

Miyoshi K et al., 1996, Regional vascular effects of MPC-1304, a novel dihydropyridine derivative, in conscious normotensive and spontaneously hypertensive rats., J Pharmacol Exp Ther
PIZOTYLINE ADRA1A

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Publications:

Mylecharane EJ, 1991, 5-HT2 receptor antagonists and migraine therapy., J Neurol
DOBUTAMINE ADRA1A

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Publications:

Ruffolo RR Jr et al., 1981, Alpha and beta adrenergic effects of the stereoisomers of dobutamine., J Pharmacol Exp Ther
PEROSPIRONE ADRA1A

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Publications:

Kishi T et al., 2013, Efficacy and tolerability of perospirone in schizophrenia: a systematic review and meta-analysis of randomized controlled trials., CNS Drugs
BUSPIRONE ADRA1A

Interaction Types & Directionality:

partial agonist (activating)

Interaction Info:

Publications:

Howland RH, 2015, Buspirone: Back to the Future., J Psychosoc Nurs Ment Health Serv
PROCHLORPERAZINE ADRA1A

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Publications:

Isah AO et al., 1991, Clinical pharmacology of prochlorperazine in healthy young males., Br J Clin Pharmacol
PIPAMPERONE ADRA1A

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Publications:

Schotte et al., 1996, Risperidone compared with new and reference antipsychotic drugs: in vitro and in vivo receptor binding., Psychopharmacology (Berl.)
ETOPERIDONE ADRA1A

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Publications:

Cusack et al., 1994, Binding of antidepressants to human brain receptors: focus on newer generation compounds., Psychopharmacology (Berl.)

ROPINIROLE ADRA1A

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Publications:

Kvernmo et al., 2008, Receptor-binding and pharmacokinetic properties of dopaminergic agonists., Curr Top Med Chem

Shill HA et al., 2009, Update on ropinirole in the treatment of Parkinson's disease., Neuropsychiatr Dis Treat

DIHYDROERGOCRISTINE ADRA1A

Interaction Types & Directionality:

antagonist (inhibitory)

agonist (activating)

Interaction Info:

Publications:

Coppi G, 1992, [Dihydroergocristine. A review of pharmacology and toxicology]., Arzneimittelforschung
QUINIDINE ADRA1A

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Publications:

Shibata K et al., 1998, Effects of quinidine and verapamil on human cardiovascular alpha1-adrenoceptors., Circulation
PAROXETINE ADRA1A

Interaction Types & Directionality:

binder

Interaction Info:

Publications:

Thomas DR et al., 1987, Biochemical effects of the antidepressant paroxetine, a specific 5-hydroxytryptamine uptake inhibitor., Psychopharmacology (Berl)
VERAPAMIL ADRA1A

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Publications:

Shibata K et al., 1998, Effects of quinidine and verapamil on human cardiovascular alpha1-adrenoceptors., Circulation
LAMOTRIGINE ADRA1A

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Publications:

Abelaira HM et al., 2012, Lamotrigine treatment reverses depressive-like behavior and alters BDNF levels in the brains of maternally deprived adult rats., Pharmacol Biochem Behav
MOXISYLYTE ADRA1A

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Publications:

Wand M et al., 1980, Thymoxamine hydrochloride: an alpha-adrenergic blocker., Surv Ophthalmol

RANOLAZINE ADRA1A

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Publications:

Rayner-Hartley E et al., 2016, Ranolazine: A Contemporary Review., J Am Heart Assoc

Virsolvy A et al., 2015, Antagonism of Nav channels and α1-adrenergic receptors contributes to vascular smooth muscle effects of ranolazine., Sci Rep

Zhao G et al., 2011, Antiadrenergic and hemodynamic effects of ranolazine in conscious dogs., J Cardiovasc Pharmacol

LORPIPRAZOLE ADRA1A

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Publications:

Jarema M et al., 2011, [Trazodon--the antidepressant: mechanism of action and its position in the treatment of depression]., Psychiatr Pol

TIZANIDINE ADRA1A

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Publications:

Takayanagi I et al., 1991, Differences in alpha 1-adrenoceptor mechanisms for phenylephrine and tizanidine in rabbit thoracic aorta and common iliac artery., Can J Physiol Pharmacol

Takayanagi I et al., 1984, Actions of tizanidine on alpha 1-and alpha 2-adrenoceptors in the peripheral tissues., Gen Pharmacol

NIGULDIPINE ADRA1A

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Publications:

Forray C et al., 1994, The alpha 1-adrenergic receptor that mediates smooth muscle contraction in human prostate has the pharmacological properties of the cloned human alpha 1c subtype., Mol Pharmacol

LOXAPINE ADRA1A

Interaction Types & Directionality:

binder

Interaction Info:

Publications:
RACEPINEPHRINE ADRA1A

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Publications:
PROPIVERINE ADRA1A

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Publications:
DOTHIEPIN ADRA1A

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Publications:
AROTINOLOL ADRA1A

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Publications:
LOFEXIDINE ADRA1A

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Publications:
LISDEXAMFETAMINE ADRA1A

Interaction Types & Directionality:

n/a

Interaction Info:

Trial Name -

Novel drug target Established target

Publications:
PERICIAZINE ADRA1A

Interaction Types & Directionality:

n/a

Interaction Info:

Trial Name -

Novel drug target Established target

Publications:
AMIODARONE ADRA1A

Interaction Types & Directionality:

n/a

Interaction Info:

Trial Name amiodarone HCl,Amio-Aqueous IV

Novel drug target Established target

Publications:
DEBRISOQUIN ADRA1A

Interaction Types & Directionality:

n/a

Interaction Info:

Novel drug target Established target

Trial Name -

Publications:
PARDOPRUNOX ADRA1A

Interaction Types & Directionality:

n/a

Interaction Info:

Trial Name pardoprunox, SLV 308

Novel drug target Established target

Publications:
SENREBOTASE ADRA1A

Interaction Types & Directionality:

n/a

Interaction Info:

Trial Name AGN-214868

Novel drug target Established target

Publications:
BETHANIDINE ADRA1A

Interaction Types & Directionality:

n/a

Interaction Info:

Trial Name -

Novel drug target Established target

Publications:

SERTINDOLE ADRA1A

Interaction Types & Directionality:

n/a

Interaction Info:

Novel drug target Established target

Trial Name Serdolect

Publications:

Hietala et al., 2001, Sertindole is a serotonin 5-HT2c inverse agonist and decreases agonist but not antagonist binding to 5-HT2c receptors after chronic treatment., Psychopharmacology (Berl.)

Lindström et al., 2006, Sertindole: efficacy and safety in schizophrenia., Expert Opin Pharmacother

NIFEDIPINE ADRA1A

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:

Zhang Y et al., 2009, Arg347Cys polymorphism of alpha1A-adrenoceptor gene is associated with blood pressure response to nifedipine GITS in Chinese hypertensive patients., J Hum Genet
EPINASTINE ADRA1A

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:

Dupont et al., 1996, Epinastine (WAL 801CL) modulates the noncholinergic contraction in guinea-pig airways in vitro by a prejunctional 5-HT1-like receptor., Eur. Respir. J.
OXEDRINE ADRA1A

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:

Huang YT et al., 2001, Hemodynamic effects of synephrine treatment in portal hypertensive rats., Jpn J Pharmacol
HALOPERIDOL ADRA1A

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:

Kroeze et al., 2003, H1-histamine receptor affinity predicts short-term weight gain for typical and atypical antipsychotic drugs., Neuropsychopharmacology
LEVONORDEFRIN ADRA1A

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:
ISOPROTERENOL ADRA1A

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:
PARA-METHOXYAMPHETAMINE ADRA1A

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:
chembl:CHEMBL180312 ADRA1A

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:
DOPAMINE ADRA1A

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:
MEDETOMIDINE ADRA1A

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:
NAFTOPIDIL ADRA1A

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:
chembl:CHEMBL96467 ADRA1A

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:
RWJ-68157 ADRA1A

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:
CORYNANTHEINE ADRA1A

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:
FLUANISONE ADRA1A

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:
METHAMPHETAMINE ADRA1A

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:
ISOCLOZAPINE ADRA1A

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:
chembl:CHEMBL49284 ADRA1A

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:
chembl:CHEMBL282214 ADRA1A

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:
chembl:CHEMBL242004 ADRA1A

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:
chembl:CHEMBL98241 ADRA1A

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:
L-765314 ADRA1A

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:
RWJ-69736 ADRA1A

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:
chembl:CHEMBL362863 ADRA1A

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:
chembl:CHEMBL22778 ADRA1A

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:
RWJ-38063 ADRA1A

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:
chembl:CHEMBL181071 ADRA1A

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:
chembl:CHEMBL318235 ADRA1A

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:
BESIPIRDINE ADRA1A

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:
OCAPERIDONE ADRA1A

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:

Ensembl: ENSG00000120907
- Version: 101_38
Alternate Names:

ADRA1A Ensembl Gene Name

Gene Info:

Gene Biotype PROTEIN_CODING

Publications:

RussLampel: ENSG00000120907

Version: 26-July-2011

Alternate Names:

ALPHA-1A ADRENERGIC RECEPTOR (ALPHA 1A-ADRENOCEPTOR) (ALPHA 1A- ADRENORECEPTOR) (ALPHA-1C ADRENERGIC RECEPTOR) (ALPHA ADRENERGIC RECEPTOR 1C). [SOURCE:UNIPROT/SWISSPROT;ACC:P35348] Description

ADRA1A Display Id

ENSG00000120907 Ensembl Gene Id

Gene Info:

Human Readable Name DRUGGABLE GENOME

Gene Categories:

DRUGGABLE GENOME

Publications:

TdgClinicalTrial: P35348
- Version: January-2014
Alternate Names:

ADRA1A Gene Symbol

Gene Info:

Target Class Receptors

Target Subclass GPCR

Target Subclass Rhodopsin

Publications:
GuideToPharmacologyGenes: 22
- Version: 4-March-2015
Alternate Names:

adrenoceptor alpha 1A HUGO Gene Name

277 HUGO Gene ID

ADRA1A Gene Symbol

Gene Info:

GuideToPharmacology Gene Category Name Adrenoceptors

GuideToPharmacology Gene Category ID 4

GuideToPharmacology Gene Type gpcr

Gene Categories:

G PROTEIN COUPLED RECEPTOR

Publications:
HopkinsGroom: P35348
- Version: 11-September-2012
Alternate Names:

ADRA1A Uniprot Gene Name

148 Entrez Gene Id

ENSG00000120907 Ensembl Gene Id

Gene Info:

Interpro Acc IPR000276

Interpro Short Name 7TM_GPCR_Rhodpsn

Human Readable Name G PROTEIN COUPLED RECEPTOR

Gene Categories:

G PROTEIN COUPLED RECEPTOR, DRUGGABLE GENOME

Publications:
TEND: P35348
- Version: 01-August-2011
Alternate Names:

ADRA1A Gene Symbol

ADA1A_HUMAN Uniprot Id

P35348 Uniprot Accession

Gene Info:

Transmembrane Helix Count 7

Target Subclass GPCR

Target Main Class Receptors

Publications:
PharmGKB: ADRA1A
- Version: 18-August-2020
Alternate Names:

PA34 PharmGKB ID

Gene Info:

Publications:

Zhang Y et al., 2009, Arg347Cys polymorphism of alpha1A-adrenoceptor gene is associated with blood pressure response to nifedipine GITS in Chinese hypertensive patients., J Hum Genet

DrugBank: BE0004888

Version: 5.1.7

Alternate Names:

ADRA1A DrugBank Gene Name

P35348 UniProt Accession

148 Entrez Gene Id

Gene Info:

Publications:

Reisine et al., 1980, Effects of combined administration of amphetamine and iprindole on brain adrenergic receptors., Brain Res.

Leibowitz, 1970, Reciprocal hunger-regulating circuits involving alpha- and beta-adrenergic receptors located, respectively, in the ventromedial and lateral hypothalamus., Proc. Natl. Acad. Sci. U.S.A.

Shill HA et al., 2009, Update on ropinirole in the treatment of Parkinson's disease., Neuropsychiatr Dis Treat

DrugBank: BE0000501

Version: 5.1.7

Alternate Names:

ADRA1A DrugBank Gene Name

P35348 UniProt Accession

148 Entrez Gene Id

Gene Info:

Publications:

Taniguchi et al., 1996, NS-49, an alpha 1A-adrenoceptor agonist, selectively increases intraurethral pressure in dogs., Eur. J. Pharmacol.

Altenbach et al., 2004, Synthesis and structure-activity studies on N-[5-(1H-imidazol-4-yl)-5,6,7,8-tetrahydro-1-naphthalenyl]methanesulfonamide, an imidazole-containing alpha(1A)-adrenoceptor agonist., J. Med. Chem.

Buckner et al., 2002, ABT-866, a novel alpha(1A)-adrenoceptor agonist with antagonist properties at the alpha(1B)- and alpha(1D)-adrenoceptor subtypes., Eur. J. Pharmacol.

DrugBank: BE0004863

Version: 5.1.7

Alternate Names:

ADRA1A DrugBank Gene Name

P35348 UniProt Accession

148 Entrez Gene Id

Gene Info:

Publications:

Nutt D, 1997, Mirtazapine: pharmacology in relation to adverse effects., Acta Psychiatr Scand Suppl

Huerta-Bahena et al., 1983, Trifluoperazine and chlorpromazine antagonize alpha 1- but not alpha2- adrenergic effects., Mol. Pharmacol.

Howland RH, 2015, Buspirone: Back to the Future., J Psychosoc Nurs Ment Health Serv

HingoraniCasas: ENSG00000120907
- Version: 31-May-2017
Alternate Names:

ENSG00000120907 Gene Symbol

ADRA1A Ensembl Id

Gene Info:

Gene Categories:

DRUGGABLE GENOME

Publications:
ChemblInteractions: ADRA1C
- Version: chembl_23
Alternate Names:

ADRA1C GENE_SYMBOL

ADRA1A GENE_SYMBOL

Alpha-1A adrenergic receptor UNIPROT

Gene Info:

Publications:
ChemblInteractions: ADRA1A
- Version: chembl_23
Alternate Names:

ADRA1A GENE_SYMBOL

ADRA1D GENE_SYMBOL

Alpha-1D adrenergic receptor UNIPROT

Gene Info:

Publications:
GuideToPharmacologyInteractions: ENSG00000120907
- Version: 20-July-2020
Alternate Names:

α<sub>1A</sub>-adrenoceptor GuideToPharmacology Name

P35348 UniProtKB ID

Gene Info:

Publications:
TTD: Adrenergic receptor alpha-1A
- Version: 2020.06.01
Alternate Names:

ADRA1A TTD Gene Abbreviation

T92609 TTD Target ID

Gene Info:

Publications:
GO: ADRA1A
- Version: 05-September-2020
Alternate Names:

ADRA1C GO Gene Synonym

Gene Info:

Gene Categories:

CELL SURFACE, DRUG RESISTANCE, G PROTEIN COUPLED RECEPTOR

Publications:
dGene: ADRA1A
- Version: 27-Jun-2013
Alternate Names:

148 Gene ID

ADRA1C dGene Synonym

ADRA1L1 dGene Synonym

Gene Info:

Gene Categories:

G PROTEIN COUPLED RECEPTOR

Publications:

Specific Action of the Ligand	Full agonist
Endogenous Drug?	False
Direct Interaction?	True

Trial Name	aviptadil,Invicorp
Novel drug target	Established target
Specific Action of the Ligand	Antagonist

Mechanism of Interaction	Alpha-1a adrenergic receptor antagonist
Direct Interaction	yes
Novel drug target	Established target

Trial Name	ALKS 3831
Trial Name	OREX-003, olanzapine plus zonisamide SR
Trial Name	Olanzapine/fluoxetine combination,Symbyax (Zyprexa/Prozac)

Mechanism of Interaction	Adrenergic receptor alpha-1 agonist
Direct Interaction	yes

Mechanism of Interaction	Adrenergic receptor alpha antagonist
Direct Interaction	yes

Direct Interaction	yes
Mechanism of Interaction	Adrenergic receptor alpha-1 antagonist

Direct Interaction	yes
Mechanism of Interaction	Adrenergic receptor alpha agonist

Mechanism of Interaction	Adrenergic receptor agonist
Direct Interaction	yes

Mechanism of Interaction	Adrenergic receptor antagonist
Direct Interaction	yes

Specific Action of the Ligand	Agonist
Endogenous Drug?	False
Direct Interaction	yes

Mechanism of Interaction	Alpha-1a adrenergic receptor agonist
Direct Interaction	yes

Specific Action of the Ligand	Partial agonist
Endogenous Drug?	False

Trial Name	fexofenadine + ps/
Novel drug target	Established target

Trial Name	dutasteride + tamsulosin,Jalyn
Novel drug target	Established target
Trial Name	tamsulosin, YM-617,Harnal, Flomax

Trial Name	alfuzosin,UroXatral
Novel drug target	Established target
Specific Action of the Ligand	Antagonist

Trial Name	iloperidone,Fanapt, Fiapta, Zomaril
Novel drug target	Established target

Trial Name	amiodarone HCl,Amio-Aqueous IV
Novel drug target	Established target

Trial Name	pardoprunox, SLV 308
Novel drug target	Established target

ALPHA-1A ADRENERGIC RECEPTOR (ALPHA 1A-ADRENOCEPTOR) (ALPHA 1A- ADRENORECEPTOR) (ALPHA-1C ADRENERGIC RECEPTOR) (ALPHA ADRENERGIC RECEPTOR 1C). [SOURCE:UNIPROT/SWISSPROT;ACC:P35348]	Description
ADRA1A	Display Id
ENSG00000120907	Ensembl Gene Id

ADRA1A Gene Record

ADRA1A 148 Druggable GenomeDrug Resistance

Alternate Names:

Gene Info:

Gene Categories: Category Details

Publications:

Interaction Types & Directionality: agonist (activating)

Interaction Info: Specific Action of the Ligand Full agonist Endogenous Drug? False Direct Interaction? True

Interaction Types & Directionality: antagonist (inhibitory)

Interaction Info: Trial Name aviptadil,Invicorp Novel drug target Established target Specific Action of the Ligand Antagonist

Interaction Types & Directionality: antagonist (inhibitory)

Interaction Info: Mechanism of Interaction Alpha-1a adrenergic receptor antagonist Direct Interaction yes Novel drug target Established target

Publications: Lepor et al., 2010, Silodosin for the treatment of benign prostatic hyperplasia: pharmacology and cardiovascular tolerability., Pharmacotherapy

Interaction Types & Directionality: antagonist (inhibitory)

Interaction Info: Trial Name ALKS 3831 Trial Name OREX-003, olanzapine plus zonisamide SR Trial Name Olanzapine/fluoxetine combination,Symbyax (Zyprexa/Prozac)

Interaction Types & Directionality: agonist (activating)

Interaction Info: Mechanism of Interaction Adrenergic receptor alpha-1 agonist Direct Interaction yes

Publications:

Interaction Types & Directionality: antagonist (inhibitory)

Interaction Info: Mechanism of Interaction Adrenergic receptor alpha antagonist Direct Interaction yes

Publications:

Interaction Types & Directionality: antagonist (inhibitory)

Interaction Info: Direct Interaction yes Mechanism of Interaction Adrenergic receptor alpha-1 antagonist

Publications:

Interaction Types & Directionality: agonist (activating)

Interaction Info: Direct Interaction yes Mechanism of Interaction Adrenergic receptor alpha agonist

Publications:

Interaction Types & Directionality: agonist (activating)

Interaction Info: Mechanism of Interaction Adrenergic receptor agonist Direct Interaction yes

Publications:

Interaction Types & Directionality: agonist (activating)

Interaction Info: Direct Interaction yes Mechanism of Interaction Adrenergic receptor agonist

Publications:

Interaction Types & Directionality: agonist (activating)

Interaction Info: Direct Interaction yes Mechanism of Interaction Adrenergic receptor alpha-1 agonist

Publications:

Interaction Types & Directionality: agonist (activating)

Interaction Info: Mechanism of Interaction Adrenergic receptor alpha-1 agonist Direct Interaction yes

Publications:

Interaction Types & Directionality: antagonist (inhibitory)

Interaction Info: Mechanism of Interaction Adrenergic receptor alpha-1 antagonist Direct Interaction yes

Publications:

Interaction Types & Directionality: antagonist (inhibitory)

Interaction Info: Specific Action of the Ligand Antagonist Endogenous Drug? False

Publications:

Interaction Types & Directionality: antagonist (inhibitory)

Interaction Info: Direct Interaction yes Mechanism of Interaction Adrenergic receptor alpha-1 antagonist

Publications:

Interaction Types & Directionality: antagonist (inhibitory)

Interaction Info: Mechanism of Interaction Adrenergic receptor alpha antagonist Direct Interaction yes

Publications:

Interaction Types & Directionality: antagonist (inhibitory)

Interaction Info: Specific Action of the Ligand Antagonist Endogenous Drug? False

Publications:

Interaction Types & Directionality: antagonist (inhibitory)

Interaction Info: Direct Interaction yes Mechanism of Interaction Adrenergic receptor alpha-1 antagonist

Publications:

Interaction Types & Directionality: agonist (activating)

Interaction Info: Mechanism of Interaction Adrenergic receptor agonist Direct Interaction yes

Publications:

Interaction Types & Directionality: antagonist (inhibitory)

Interaction Info: Direct Interaction? False Endogenous Drug? False Specific Action of the Ligand Antagonist

Publications:

Interaction Types & Directionality: agonist (activating)

Interaction Info: Mechanism of Interaction Adrenergic receptor alpha-1 agonist Direct Interaction yes

Publications:

Interaction Types & Directionality: antagonist (inhibitory)

Interaction Info: Specific Action of the Ligand Antagonist Endogenous Drug? False

Publications:

Interaction Types & Directionality: antagonist (inhibitory)

Interaction Info: Specific Action of the Ligand Antagonist Endogenous Drug? False

Publications:

Interaction Types & Directionality: agonist (activating)

Interaction Info: Mechanism of Interaction Adrenergic receptor agonist Direct Interaction yes

Publications:

Interaction Types & Directionality: agonist (activating)

Interaction Info: Mechanism of Interaction Adrenergic receptor alpha-1 agonist Direct Interaction yes

Publications:

Interaction Types & Directionality: antagonist (inhibitory)

Interaction Info: Mechanism of Interaction Adrenergic receptor alpha antagonist Direct Interaction yes

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Specific Action of the Ligand Full agonist

Endogenous Drug? False

Direct Interaction? True

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Trial Name aviptadil,Invicorp

Novel drug target Established target

Specific Action of the Ligand Antagonist

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Mechanism of Interaction Alpha-1a adrenergic receptor antagonist

Direct Interaction yes

Novel drug target Established target

Publications:

Lepor et al., 2010, Silodosin for the treatment of benign prostatic hyperplasia: pharmacology and cardiovascular tolerability., Pharmacotherapy

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Trial Name ALKS 3831

Trial Name OREX-003, olanzapine plus zonisamide SR

Trial Name Olanzapine/fluoxetine combination,Symbyax (Zyprexa/Prozac)

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Mechanism of Interaction Adrenergic receptor alpha-1 agonist

Direct Interaction yes

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Mechanism of Interaction Adrenergic receptor alpha antagonist

Direct Interaction yes

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Adrenergic receptor alpha-1 antagonist

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Adrenergic receptor alpha agonist

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Mechanism of Interaction Adrenergic receptor agonist

Direct Interaction yes

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Adrenergic receptor agonist

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Adrenergic receptor alpha-1 agonist

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Mechanism of Interaction Adrenergic receptor alpha-1 agonist

Direct Interaction yes

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Mechanism of Interaction Adrenergic receptor alpha-1 antagonist

Direct Interaction yes

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Specific Action of the Ligand Antagonist

Endogenous Drug? False

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Adrenergic receptor alpha-1 antagonist

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Mechanism of Interaction Adrenergic receptor alpha antagonist

Direct Interaction yes

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Specific Action of the Ligand Antagonist

Endogenous Drug? False

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Adrenergic receptor alpha-1 antagonist

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Mechanism of Interaction Adrenergic receptor agonist

Direct Interaction yes

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Direct Interaction? False

Endogenous Drug? False

Specific Action of the Ligand Antagonist

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Mechanism of Interaction Adrenergic receptor alpha-1 agonist

Direct Interaction yes

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Specific Action of the Ligand Antagonist

Endogenous Drug? False

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Specific Action of the Ligand Antagonist

Endogenous Drug? False

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Mechanism of Interaction Adrenergic receptor agonist

Direct Interaction yes

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Mechanism of Interaction Adrenergic receptor alpha-1 agonist

Direct Interaction yes

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Mechanism of Interaction Adrenergic receptor alpha antagonist

Direct Interaction yes

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Adrenergic receptor agonist

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Mechanism of Interaction Adrenergic receptor antagonist

Direct Interaction yes

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Specific Action of the Ligand Antagonist

Endogenous Drug? False

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Specific Action of the Ligand Antagonist

Endogenous Drug? False

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Mechanism of Interaction Adrenergic receptor alpha-1 agonist

Direct Interaction yes

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Mechanism of Interaction Adrenergic receptor alpha antagonist

Direct Interaction yes

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Endogenous Drug? False

Specific Action of the Ligand Antagonist

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Mechanism of Interaction Adrenergic receptor alpha antagonist

Direct Interaction yes

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Mechanism of Interaction Adrenergic receptor alpha-1 antagonist

Direct Interaction yes

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Adrenergic receptor alpha antagonist

adrenoceptor alpha 1A	HUGO Gene Name
277	HUGO Gene ID
ADRA1A	Gene Symbol

ADRA1A	Uniprot Gene Name
148	Entrez Gene Id
ENSG00000120907	Ensembl Gene Id

ADRA1A	DrugBank Gene Name
P35348	UniProt Accession
148	Entrez Gene Id

ADRA1C	GENE_SYMBOL
ADRA1A	GENE_SYMBOL
Alpha-1A adrenergic receptor	UNIPROT

α<sub>1A</sub>-adrenoceptor	GuideToPharmacology Name
P35348	UniProtKB ID