DGIdb - ADRA2C Gene Record

OLANZAPINE ADRA2C

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Trial Name olanzapine,Zyprexa, Zypadhera, Zyprexa Relprevv

Novel drug target Established target

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

Publications:

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

TIZANIDINE ADRA2C

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Trial Name NVD-422, tizanidine oral spray

Novel drug target Established target

Trial Name tizanidine hydrochloride,Zanaflex

Publications:

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.

OXYMETAZOLINE ADRA2C

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Direct Interaction? False

Endogenous Drug? False

Specific Action of the Ligand Partial agonist

Publications:

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

TOLAZOLINE ADRA2C

Interaction Types & Directionality:

binder

antagonist (inhibitory)

Interaction Info:

Details of the Assay for Interaction Inhibition of agonist-stimulated [35S]GTPγS binding

Specific Action of the Ligand Antagonist

Endogenous Drug? False

Publications:

Trendelenburg et al., 1997, Presynaptic alpha 2A/D-autoreceptors in the brain cortex of Cercopithecus aethiops., Naunyn Schmiedebergs Arch. Pharmacol.

MIRTAZAPINE ADRA2C

Interaction Types & Directionality:

binder

antagonist (inhibitory)

Interaction Info:

Mechanism of Interaction Adrenergic receptor alpha-2 antagonist

Direct Interaction yes

Specific Action of the Ligand Antagonist

Publications:

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

Fernández et al., 2005, Discovery of new tetracyclic tetrahydrofuran derivatives as potential broad-spectrum psychotropic agents., J. Med. Chem.

CLONIDINE ADRA2C

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Mechanism of Interaction Adrenergic receptor alpha-2 agonist

Direct Interaction yes

Specific Action of the Ligand Partial agonist

Publications:

Yang YY et al., 2010, Association of the G-protein and α2-adrenergic receptor gene and plasma norepinephrine level with clonidine improvement of the effects of diuretics in patients with cirrhosis with refractory ascites: a randomised clinical trial., Gut

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

LURASIDONE ADRA2C

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Trial Name lurasidone, SM-13496,Latuda

Novel drug target Established target

Specific Action of the Ligand Antagonist

Publications:

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

RAUWOLSCINE ADRA2C

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Specific Action of the Ligand Antagonist

Endogenous Drug? False

Publications:

DEXMEDETOMIDINE HYDROCHLORIDE ADRA2C

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Adrenergic receptor alpha-2 agonist

Publications:

NOREPINEPHRINE BITARTRATE ADRA2C

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Mechanism of Interaction Adrenergic receptor agonist

Direct Interaction yes

Publications:

CHLORPROMAZINE ADRA2C

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Endogenous Drug? False

Specific Action of the Ligand Antagonist

Publications:

RAUWOLFIA SERPENTINA ADRA2C

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Adrenergic receptor alpha antagonist

Publications:

LOFEXIDINE ADRA2C

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Novel drug target Established target

Trial Name lofexidine,BritLofex

Details of the Assay for Interaction Calculated from [3H]RS-79948-197 radioligand competition binding to membrane preparations from CHO cells expressing human α2C-AR.

Publications:

ILOPERIDONE ADRA2C

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Trial Name iloperidone,Fanapt, Fiapta, Zomaril

Novel drug target Established target

Publications:

HYDROXYAMPHETAMINE HYDROBROMIDE ADRA2C

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Mechanism of Interaction Adrenergic receptor agonist

Direct Interaction yes

Publications:

NAPHAZOLINE HYDROCHLORIDE ADRA2C

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Mechanism of Interaction Adrenergic receptor alpha agonist

Direct Interaction yes

Publications:

SPIROXATRINE ADRA2C

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Direct Interaction? False

Endogenous Drug? False

Specific Action of the Ligand Antagonist

Publications:

TIZANIDINE HYDROCHLORIDE ADRA2C

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Adrenergic receptor alpha-2 agonist

Publications:

CLONIDINE HYDROCHLORIDE ADRA2C

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Mechanism of Interaction Adrenergic receptor alpha-2 agonist

Direct Interaction yes

Publications:

APRACLONIDINE ADRA2C

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Direct Interaction? True

Endogenous Drug? False

Specific Action of the Ligand Agonist

Publications:

ALSEROXYLON ADRA2C

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Mechanism of Interaction Adrenergic receptor alpha antagonist

Direct Interaction yes

Publications:

GUANFACINE HYDROCHLORIDE ADRA2C

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Mechanism of Interaction Adrenergic receptor alpha-2 agonist

Direct Interaction yes

Publications:

XYLAZINE ADRA2C

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Specific Action of the Ligand Partial agonist

Endogenous Drug? False

Publications:

TERGURIDE ADRA2C

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Specific Action of the Ligand Antagonist

Endogenous Drug? False

Publications:

METHYLDOPATE HYDROCHLORIDE ADRA2C

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Mechanism of Interaction Adrenergic receptor alpha-2 agonist

Direct Interaction yes

Publications:

PHENOXYBENZAMINE HYDROCHLORIDE ADRA2C

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Mechanism of Interaction Adrenergic receptor alpha antagonist

Direct Interaction yes

Publications:

OXYMETAZOLINE HYDROCHLORIDE ADRA2C

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Mechanism of Interaction Adrenergic receptor alpha agonist

Direct Interaction yes

Publications:

PHENTOLAMINE ADRA2C

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Specific Action of the Ligand Antagonist

Endogenous Drug? False

Publications:

MEPHENTERMINE SULFATE ADRA2C

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Mechanism of Interaction Adrenergic receptor agonist

Direct Interaction yes

Publications:

METHYLDOPA ADRA2C

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Mechanism of Interaction Adrenergic receptor alpha-2 agonist

Direct Interaction yes

Publications:

LEVONORDEFRIN ADRA2C

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Mechanism of Interaction Adrenergic receptor alpha-2 agonist

Direct Interaction yes

Publications:

chembl:CHEMBL362051 ADRA2C

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Specific Action of the Ligand Antagonist

Endogenous Drug? False

Publications:

GUANFACINE ADRA2C

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Specific Action of the Ligand Partial agonist

Endogenous Drug? False

Direct Interaction? True

Publications:

PRAZOSIN ADRA2C

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Specific Action of the Ligand Antagonist

Endogenous Drug? False

Publications:

DEXMEDETOMIDINE ADRA2C

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Specific Action of the Ligand Full agonist

Endogenous Drug? False

Direct Interaction? True

Publications:

FADOLMIDINE HYDROCHLORIDE ADRA2C

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Mechanism of Interaction Adrenergic receptor alpha-2 agonist

Direct Interaction yes

Publications:

LABETALOL HYDROCHLORIDE ADRA2C

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Mechanism of Interaction Adrenergic receptor antagonist

Direct Interaction yes

Publications:

BRIMONIDINE TARTRATE ADRA2C

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Mechanism of Interaction Adrenergic receptor alpha-2 agonist

Direct Interaction yes

Publications:

GUANABENZ ACETATE ADRA2C

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Adrenergic receptor alpha-2 agonist

Publications:

GUANABENZ ADRA2C

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Direct Interaction? True

Endogenous Drug? False

Specific Action of the Ligand Agonist

Publications:

ROXINDOLE ADRA2C

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Endogenous Drug? False

Specific Action of the Ligand Antagonist

Publications:

ESMIRTAZAPINE MALEATE ADRA2C

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Mechanism of Interaction Adrenergic receptor alpha-2 antagonist

Direct Interaction yes

Publications:

ERGOLOID MESYLATES ADRA2C

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Mechanism of Interaction Adrenergic receptor alpha antagonist

Direct Interaction yes

Publications:

PHENTOLAMINE MESYLATE ADRA2C

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Mechanism of Interaction Adrenergic receptor alpha antagonist

Direct Interaction yes

Publications:

PIRIBEDIL ADRA2C

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Specific Action of the Ligand Antagonist

Endogenous Drug? False

Publications:

APRACLONIDINE HYDROCHLORIDE ADRA2C

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Mechanism of Interaction Adrenergic receptor alpha-2 agonist

Direct Interaction yes

Publications:

EPINEPHRINE BITARTRATE ADRA2C

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Mechanism of Interaction Adrenergic receptor agonist

Direct Interaction yes

Publications:

TETRAHYDROZOLINE HYDROCHLORIDE ADRA2C

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Mechanism of Interaction Adrenergic receptor alpha agonist

Direct Interaction yes

Publications:

TOLAZOLINE HYDROCHLORIDE ADRA2C

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Mechanism of Interaction Adrenergic receptor alpha antagonist

Direct Interaction yes

Publications:

DIPIVEFRIN HYDROCHLORIDE ADRA2C

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Mechanism of Interaction Adrenergic receptor agonist

Direct Interaction yes

Publications:

ZIPRASIDONE ADRA2C

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Publications:

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

PERGOLIDE ADRA2C

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Specific Action of the Ligand Partial agonist

Endogenous Drug? False

Publications:

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

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

NOREPINEPHRINE ADRA2C

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Trial Name -

Novel drug target Established target

Publications:

Rump et al., 1995, Alpha 2C-adrenoceptor-modulated release of noradrenaline in human right atrium., Br. J. Pharmacol.

Nash, 1990, Alpha-adrenergic blockers: mechanism of action, blood pressure control, and effects of lipoprotein metabolism., Clin Cardiol

Bruck et al., 2007, Presynaptic alpha-2C adrenoceptor-mediated control of noradrenaline release in humans: genotype- or age-dependent?, Clin. Pharmacol. Ther.

YOHIMBINE ADRA2C

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Specific Action of the Ligand Antagonist

Endogenous Drug? False

Direct Interaction? True

Publications:

Cleary et al., 2002, Investigation of neurotransmission in vas deferens from alpha(2A/D)-adrenoceptor knockout mice., Br. J. Pharmacol.

Rizzo et al., 2001, Postjunctional alpha(2C)-adrenoceptor contractility in human saphenous vein., Eur. J. Pharmacol.

Kalkman et al., 2003, alpha2C-Adrenoceptor blockade by clozapine and other antipsychotic drugs., Eur. J. Pharmacol.

ASENAPINE ADRA2C

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)

QUETIAPINE ADRA2C

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

Uys MM et al., 2017, Therapeutic Potential of Selectively Targeting the α2C-Adrenoceptor in Cognition, Depression, and Schizophrenia-New Developments and Future Perspective., Front Psychiatry

XYLOMETAZOLINE ADRA2C

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Publications:

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

EPINEPHRINE ADRA2C

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Adrenergic receptor agonist

Publications:

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

BRIMONIDINE ADRA2C

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Specific Action of the Ligand Partial agonist

Endogenous Drug? False

Direct Interaction? True

Publications:

Prinster et al., 2006, Alpha2C-adrenergic receptors exhibit enhanced surface expression and signaling upon association with beta2-adrenergic receptors., J. Pharmacol. Exp. Ther.

Zhang et al., 2003, The alpha2C-adrenoceptor modulates GABA release in mouse striatum., Brain Res. Mol. Brain Res.

Orito et al., 2001, alpha(2)-adrenoceptor antagonist properties of OPC-28326, a novel selective peripheral vasodilator., Br. J. Pharmacol.

FENOLDOPAM ADRA2C

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

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

METHAMPHETAMINE ADRA2C

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Trial Name low dose intravenous methamphetamine

Novel drug target Established target

Publications:

Jeng et al., 1998, Methamphetamine modulates GABA-induced electrophysiological depression by alternating noradrenergic actions in cerebellar Purkinje neurons., Psychopharmacology (Berl.)

Sulzer et al., 2005, Mechanisms of neurotransmitter release by amphetamines: a review., Prog. Neurobiol.

CABERGOLINE ADRA2C

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Endogenous Drug? False

Specific Action of the Ligand Antagonist

Publications:

Newman-Tancredi et al., 2002, Differential actions of antiparkinson agents at multiple classes of monoaminergic receptor. II. Agonist and antagonist properties at subtypes of dopamine D(2)-like receptor and alpha(1)/alpha(2)-adrenoceptor., J. Pharmacol. Exp. Ther.

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

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

PALIPERIDONE ADRA2C

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Publications:

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

CARVEDILOL ADRA2C

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Publications:

Koshimizu et al., 2004, Carvedilol selectively inhibits oscillatory intracellular calcium changes evoked by human alpha1D- and alpha1B-adrenergic receptors., Cardiovasc. Res.

RISPERIDONE ADRA2C

Interaction Types & Directionality:

agonist (activating)

antagonist (inhibitory)

Interaction Info:

Publications:

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

Fenton et al., 2005, Risperidone: a review of its use in the treatment of bipolar mania., CNS Drugs

Corena-McLeod M, 2015, Comparative Pharmacology of Risperidone and Paliperidone., Drugs R D

DRONEDARONE ADRA2C

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

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

APOMORPHINE ADRA2C

Interaction Types & Directionality:

antagonist (inhibitory)

agonist (activating)

Interaction Info:

Endogenous Drug? False

Specific Action of the Ligand Antagonist

Publications:

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

LEVOMEPROMAZINE ADRA2C

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Publications:

Tsukamoto et al., 1984, Interaction of neuroleptics and antidepressants with rat brain alpha 2-receptors: a possible relationship between alpha 2-receptor antagonism and antidepressant action., Biol. Psychiatry

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.

DOXEPIN ADRA2C

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.)

BROMOCRIPTINE ADRA2C

Interaction Types & Directionality:

antagonist (inhibitory)

agonist (activating)

Interaction Info:

Specific Action of the Ligand Antagonist

Endogenous Drug? False

Publications:

de Leeuw van Weenen et al., 2010, The dopamine receptor D2 agonist bromocriptine inhibits glucose-stimulated insulin secretion by direct activation of the alpha2-adrenergic receptors in beta cells., Biochem. Pharmacol.

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

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

EPHEDRA ADRA2C

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Publications:

Kobayashi et al., 2003, The sympathomimetic actions of l-ephedrine and d-pseudoephedrine: direct receptor activation or norepinephrine release?, Anesth. Analg.

Sulzer et al., 2005, Mechanisms of neurotransmitter release by amphetamines: a review., Prog. Neurobiol.

Rothman et al., 2003, In vitro characterization of ephedrine-related stereoisomers at biogenic amine transporters and the receptorome reveals selective actions as norepinephrine transporter substrates., J. Pharmacol. Exp. Ther.

LISURIDE ADRA2C

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Specific Action of the Ligand Antagonist

Endogenous Drug? False

Publications:

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

DROXIDOPA ADRA2C

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Mechanism of Interaction Adrenergic receptor agonist

Direct Interaction yes

Publications:

Giovannoni et al., 2009, Alpha2-agonists as analgesic agents., Med Res Rev

Rump et al., 1995, Alpha 2C-adrenoceptor-modulated release of noradrenaline in human right atrium., Br. J. Pharmacol.

Davis, 2010, Recent advances in the treatment of pain., F1000 Med Rep

ARIPIPRAZOLE ADRA2C

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

PHENOXYBENZAMINE ADRA2C

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Publications:

Frang et al., 2001, Phenoxybenzamine binding reveals the helical orientation of the third transmembrane domain of adrenergic receptors., J. Biol. Chem.

CLOZAPINE ADRA2C

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Publications:

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

BREXPIPRAZOLE ADRA2C

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Publications:

Oosterhof et al., 2014, Acute effects of brexpiprazole on serotonin, dopamine, and norepinephrine systems: an in vivo electrophysiologic characterization., J. Pharmacol. Exp. Ther.

AGMATINE ADRA2C

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Publications:

Li et al., 1994, Agmatine: an endogenous clonidine-displacing substance in the brain., Science

ROPINIROLE ADRA2C

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Publications:

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

PIZOTYLINE ADRA2C

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Publications:

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

CELIPROLOL ADRA2C

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Publications:

Nawarskas JJ et al., 2017, Celiprolol: A Unique Selective Adrenoceptor Modulator., Cardiol Rev

LOXAPINE ADRA2C

Interaction Types & Directionality:

binder

Interaction Info:

Publications:

MIANSERIN ADRA2C

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Publications:

RACEPINEPHRINE ADRA2C

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Publications:

SENREBOTASE ADRA2C

Interaction Types & Directionality:

n/a

Interaction Info:

Novel drug target Established target

Trial Name AGN-214868

Publications:

FIPAMEZOLE ADRA2C

Interaction Types & Directionality:

n/a

Interaction Info:

Trial Name fipamezole, JP-1730

Novel drug target Established target

Publications:

BETHANIDINE ADRA2C

Interaction Types & Directionality:

n/a

Interaction Info:

Trial Name -

Novel drug target Established target

Publications:

DEBRISOQUIN ADRA2C

Interaction Types & Directionality:

n/a

Interaction Info:

Trial Name -

Novel drug target Established target

Publications:

BUCINDOLOL ADRA2C

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:

O'Connor CM et al., 2012, Combinatorial pharmacogenetic interactions of bucindolol and β1, α2C adrenergic receptor polymorphisms., PLoS One

PRAMIPEXOLE ADRA2C

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:

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

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

ERGOTAMINE ADRA2C

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:

Villamil-Hernández MT et al., 2013, Pharmacological identification of α1- and α2-adrenoceptor subtypes involved in the vasopressor responses induced by ergotamine in pithed rats., Eur J Pharmacol

HALOPERIDOL ADRA2C

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

GuideToPharmacology Gene Category Name	Adrenoceptors
GuideToPharmacology Gene Category ID	4
GuideToPharmacology Gene Type	gpcr
Target Class	Receptors
Target Subclass	GPCR
Target Subclass	Rhodopsin
Target Class	Transporters
Human Readable Name	G PROTEIN COUPLED RECEPTOR
Transmembrane Helix Count	7
Target Main Class	Receptors
Human Readable Name	DRUGGABLE GENOME
Uniprot Evidence	2: Evidence at transcript level
Interpro Name	GPCR, rhodopsin-like, 7TM
Interpro Acc	IPR000276
Uniprot Status	Swiss-Prot
Interpro Type	Family
Interpro Short Name	7TM_GPCR_Rhodpsn
Gene Biotype	PROTEIN_CODING

Trial Name	olanzapine,Zyprexa, Zypadhera, Zyprexa Relprevv
Novel drug target	Established target
Trial Name	Olanzapine/fluoxetine combination,Symbyax (Zyprexa/Prozac)

Trial Name	NVD-422, tizanidine oral spray
Novel drug target	Established target
Trial Name	tizanidine hydrochloride,Zanaflex

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

Details of the Assay for Interaction	Inhibition of agonist-stimulated [<sup>35</sup>S]GTPγS binding
Specific Action of the Ligand	Antagonist
Endogenous Drug?	False

Mechanism of Interaction	Adrenergic receptor alpha-2 antagonist
Direct Interaction	yes
Specific Action of the Ligand	Antagonist

Mechanism of Interaction	Adrenergic receptor alpha-2 agonist
Direct Interaction	yes
Specific Action of the Ligand	Partial agonist

Trial Name	lurasidone, SM-13496,Latuda
Novel drug target	Established target
Specific Action of the Ligand	Antagonist

Mechanism of Interaction	Adrenergic receptor agonist
Direct Interaction	yes

Direct Interaction	yes
Mechanism of Interaction	Adrenergic receptor alpha antagonist

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

152
ADRENOCEPTOR ALPHA 2C
ADRA2C
ADRA2L2
ADRA2RL2
ADRARL2
ALPHA2CAR
104250
283
ENSG00000184160
OTTHUMG00000159830
P18825
ADA2C_HUMAN
Alpha-2 adrenergic receptor subtype C4
Alpha-2CAR
Alpha-2C adrenoceptor
Alpha-2C adrenoreceptor
Alpha-2C adrenergic receptor
27
NM_000683
α<sub>2C</sub>-adrenoceptor
NP_000674
BE0000342
PA37
Adrenergic receptor alpha-2C
T01777

KINASE
SERINE THREONINE KINASE
TYROSINE KINASE
G PROTEIN COUPLED RECEPTOR
DRUGGABLE GENOME

Mechanism of Interaction	Adrenergic receptor alpha agonist
Direct Interaction	yes

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

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

Mechanism of Interaction	Adrenergic receptor antagonist
Direct Interaction	yes

Trial Name	low dose intravenous methamphetamine
Novel drug target	Established target

Trial Name	fipamezole, JP-1730
Novel drug target	Established target

ADRA2C	Gene Symbol
ADA2C_HUMAN	Uniprot Id
ENSG00000184160	Ensembl Gene Id

ALPHA-2C ADRENERGIC RECEPTOR	Uniprot Protein Name
152	Entrez Gene Id
ADA2C_HUMAN	Uniprot Id

ADRA2C	DrugBank Gene Name
P18825	UniProt Accession
152	Entrez Gene Id

ADRA2RL2	GENE_SYMBOL
ADRA2C	GENE_SYMBOL
Alpha-2C adrenergic receptor	UNIPROT

ADRA2C Gene Record

ADRA2C 152 Druggable Genome

Alternate Names:

Gene Info:

Gene Categories: Category Details

Publications:

Interaction Types & Directionality: antagonist (inhibitory)

Interaction Info: Trial Name olanzapine,Zyprexa, Zypadhera, Zyprexa Relprevv Novel drug target Established target Trial Name Olanzapine/fluoxetine combination,Symbyax (Zyprexa/Prozac)

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

Interaction Types & Directionality: agonist (activating)

Interaction Info: Trial Name NVD-422, tizanidine oral spray Novel drug target Established target Trial Name tizanidine hydrochloride,Zanaflex

Publications: 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.

Interaction Types & Directionality: agonist (activating)

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

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

Interaction Types & Directionality: binder antagonist (inhibitory)

Interaction Info: Details of the Assay for Interaction Inhibition of agonist-stimulated [<sup>35</sup>S]GTP&gamma;S binding Specific Action of the Ligand Antagonist Endogenous Drug? False

Publications: Trendelenburg et al., 1997, Presynaptic alpha 2A/D-autoreceptors in the brain cortex of Cercopithecus aethiops., Naunyn Schmiedebergs Arch. Pharmacol.

Interaction Types & Directionality: binder antagonist (inhibitory)

Interaction Info: Mechanism of Interaction Adrenergic receptor alpha-2 antagonist Direct Interaction yes Specific Action of the Ligand Antagonist

Interaction Types & Directionality: agonist (activating)

Interaction Info: Mechanism of Interaction Adrenergic receptor alpha-2 agonist Direct Interaction yes Specific Action of the Ligand Partial agonist

Interaction Types & Directionality: antagonist (inhibitory)

Interaction Info: Trial Name lurasidone, SM-13496,Latuda Novel drug target Established target Specific Action of the Ligand Antagonist

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

Interaction Types & Directionality: antagonist (inhibitory)

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

Publications:

Interaction Types & Directionality: agonist (activating)

Interaction Info: Direct Interaction yes Mechanism of Interaction Adrenergic receptor alpha-2 agonist

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: Endogenous Drug? False Specific Action of the Ligand Antagonist

Publications:

Interaction Types & Directionality: antagonist (inhibitory)

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

Publications:

Interaction Types & Directionality: agonist (activating)

Interaction Info: Novel drug target Established target Trial Name lofexidine,BritLofex Details of the Assay for Interaction Calculated from [<sup>3</sup>H]RS-79948-197 radioligand competition binding to membrane preparations from CHO cells expressing human &alpha;<sub>2C</sub>-AR.

Publications:

Interaction Types & Directionality: antagonist (inhibitory)

Interaction Info: Trial Name iloperidone,Fanapt, Fiapta, Zomaril Novel drug target Established target

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 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: Direct Interaction yes Mechanism of Interaction Adrenergic receptor alpha-2 agonist

Publications:

Interaction Types & Directionality: agonist (activating)

Interaction Info: Mechanism of Interaction Adrenergic receptor alpha-2 agonist Direct Interaction yes

Publications:

Interaction Types & Directionality: agonist (activating)

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

Publications:

Interaction Types & Directionality: antagonist (inhibitory)

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

Publications:

Interaction Types & Directionality: agonist (activating)

Interaction Info: Mechanism of Interaction Adrenergic receptor alpha-2 agonist Direct Interaction yes

Publications:

Interaction Types & Directionality: agonist (activating)

Interaction Info: Specific Action of the Ligand Partial agonist 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 alpha-2 agonist Direct Interaction yes

Publications:

Interaction Types & Directionality: antagonist (inhibitory)

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Trial Name olanzapine,Zyprexa, Zypadhera, Zyprexa Relprevv

Novel drug target Established target

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

Publications:

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

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Trial Name NVD-422, tizanidine oral spray

Novel drug target Established target

Trial Name tizanidine hydrochloride,Zanaflex

Publications:

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.

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Direct Interaction? False

Endogenous Drug? False

Specific Action of the Ligand Partial agonist

Publications:

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

Interaction Types & Directionality:

binder

antagonist (inhibitory)

Interaction Info:

Details of the Assay for Interaction Inhibition of agonist-stimulated [<sup>35</sup>S]GTPγS binding

Specific Action of the Ligand Antagonist

Endogenous Drug? False

Publications:

Trendelenburg et al., 1997, Presynaptic alpha 2A/D-autoreceptors in the brain cortex of Cercopithecus aethiops., Naunyn Schmiedebergs Arch. Pharmacol.

Interaction Types & Directionality:

binder

antagonist (inhibitory)

Interaction Info:

Mechanism of Interaction Adrenergic receptor alpha-2 antagonist

Direct Interaction yes

Specific Action of the Ligand Antagonist

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Mechanism of Interaction Adrenergic receptor alpha-2 agonist

Direct Interaction yes

Specific Action of the Ligand Partial agonist

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Trial Name lurasidone, SM-13496,Latuda

Novel drug target Established target

Specific Action of the Ligand Antagonist

Publications:

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

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Specific Action of the Ligand Antagonist

Endogenous Drug? False

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Adrenergic receptor alpha-2 agonist

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Mechanism of Interaction Adrenergic receptor agonist

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:

Direct Interaction yes

Mechanism of Interaction Adrenergic receptor alpha antagonist

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Novel drug target Established target

Trial Name lofexidine,BritLofex

Details of the Assay for Interaction Calculated from [<sup>3</sup>H]RS-79948-197 radioligand competition binding to membrane preparations from CHO cells expressing human α<sub>2C</sub>-AR.

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Trial Name iloperidone,Fanapt, Fiapta, Zomaril

Novel drug target Established target

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 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:

Direct Interaction yes

Mechanism of Interaction Adrenergic receptor alpha-2 agonist

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Mechanism of Interaction Adrenergic receptor alpha-2 agonist

Direct Interaction yes

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Direct Interaction? True

Endogenous Drug? False

Specific Action of the Ligand Agonist

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Mechanism of Interaction Adrenergic receptor alpha antagonist

Direct Interaction yes

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Mechanism of Interaction Adrenergic receptor alpha-2 agonist

Direct Interaction yes

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Specific Action of the Ligand Partial agonist

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-2 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:

Mechanism of Interaction Adrenergic receptor alpha agonist

Direct Interaction yes

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-2 agonist

Direct Interaction yes

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Mechanism of Interaction Adrenergic receptor alpha-2 agonist

Direct Interaction yes

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Specific Action of the Ligand Antagonist

Endogenous Drug? False

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Specific Action of the Ligand Partial agonist

Endogenous Drug? False

Direct Interaction? True

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Specific Action of the Ligand Antagonist

Endogenous Drug? False

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Specific Action of the Ligand Full agonist

Endogenous Drug? False

Direct Interaction? True

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Mechanism of Interaction Adrenergic receptor alpha-2 agonist

Direct Interaction yes

α<sub>2C</sub>-adrenoceptor	GuideToPharmacology Name
P18825	UniProtKB ID