DGIdb - ADRA2B Gene Record

CLONIDINE ADRA2B

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Specific Action of the Ligand Partial agonist

Endogenous Drug? False

Direct Interaction? True

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

OLANZAPINE ADRA2B

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Trial Name OREX-003, olanzapine plus zonisamide SR

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

Trial Name ALKS 3831

Publications:

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

TIZANIDINE ADRA2B

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.

PHENOXYBENZAMINE ADRA2B

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Direct Interaction? True

Endogenous Drug? False

Specific Action of the Ligand Antagonist

Publications:

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

TOLAZOLINE ADRA2B

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.

ROXINDOLE ADRA2B

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Endogenous Drug? False

Specific Action of the Ligand Antagonist

Publications:

HYDROXYAMPHETAMINE HYDROBROMIDE ADRA2B

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Mechanism of Interaction Adrenergic receptor agonist

Direct Interaction yes

Publications:

ZOTEPINE ADRA2B

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Specific Action of the Ligand Antagonist

Endogenous Drug? False

Direct Interaction? False

Publications:

TETRAHYDROZOLINE HYDROCHLORIDE ADRA2B

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Mechanism of Interaction Adrenergic receptor alpha agonist

Direct Interaction yes

Publications:

CLONIDINE HYDROCHLORIDE ADRA2B

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Mechanism of Interaction Adrenergic receptor alpha-2 agonist

Direct Interaction yes

Publications:

LOFEXIDINE ADRA2B

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Details of the Assay for Interaction Calculated from [3H]RS-79948-197 radioligand competition binding to membrane preparations from CHO cells expressing human α2B-AR.

Specific Action of the Ligand Agonist

Endogenous Drug? False

Publications:

ERGOLOID MESYLATES ADRA2B

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Adrenergic receptor alpha antagonist

Publications:

DEXMEDETOMIDINE HYDROCHLORIDE ADRA2B

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Adrenergic receptor alpha-2 agonist

Publications:

MIRTAZAPINE ADRA2B

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Direct Interaction? True

Endogenous Drug? False

Specific Action of the Ligand Antagonist

Publications:

FADOLMIDINE HYDROCHLORIDE ADRA2B

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Mechanism of Interaction Adrenergic receptor alpha-2 agonist

Direct Interaction yes

Publications:

METHYLDOPATE HYDROCHLORIDE ADRA2B

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Mechanism of Interaction Adrenergic receptor alpha-2 agonist

Direct Interaction yes

Publications:

EPINEPHRINE BITARTRATE ADRA2B

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Adrenergic receptor agonist

Publications:

LABETALOL HYDROCHLORIDE ADRA2B

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Mechanism of Interaction Adrenergic receptor antagonist

Direct Interaction yes

Publications:

PHENTOLAMINE ADRA2B

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Specific Action of the Ligand Antagonist

Endogenous Drug? False

Publications:

RAUWOLFIA SERPENTINA ADRA2B

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Adrenergic receptor alpha antagonist

Publications:

XYLAZINE ADRA2B

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Specific Action of the Ligand Partial agonist

Endogenous Drug? False

Publications:

CHLORPROMAZINE ADRA2B

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Specific Action of the Ligand Antagonist

Endogenous Drug? False

Publications:

PHENTOLAMINE MESYLATE ADRA2B

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Mechanism of Interaction Adrenergic receptor alpha antagonist

Direct Interaction yes

Publications:

NAPHAZOLINE HYDROCHLORIDE ADRA2B

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Mechanism of Interaction Adrenergic receptor alpha agonist

Direct Interaction yes

Publications:

APRACLONIDINE HYDROCHLORIDE ADRA2B

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Mechanism of Interaction Adrenergic receptor alpha-2 agonist

Direct Interaction yes

Publications:

OXYMETAZOLINE HYDROCHLORIDE ADRA2B

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Mechanism of Interaction Adrenergic receptor alpha agonist

Direct Interaction yes

Publications:

GUANABENZ ACETATE ADRA2B

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Adrenergic receptor alpha-2 agonist

Publications:

MEPHENTERMINE SULFATE ADRA2B

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Mechanism of Interaction Adrenergic receptor agonist

Direct Interaction yes

Publications:

ALSEROXYLON ADRA2B

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Mechanism of Interaction Adrenergic receptor alpha antagonist

Direct Interaction yes

Publications:

LEVONORDEFRIN ADRA2B

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Mechanism of Interaction Adrenergic receptor alpha-2 agonist

Direct Interaction yes

Publications:

SPIROXATRINE ADRA2B

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Specific Action of the Ligand Antagonist

Endogenous Drug? False

Publications:

DEXMEDETOMIDINE ADRA2B

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Specific Action of the Ligand Full agonist

Endogenous Drug? False

Direct Interaction? True

Publications:

TIZANIDINE HYDROCHLORIDE ADRA2B

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Mechanism of Interaction Adrenergic receptor alpha-2 agonist

Direct Interaction yes

Publications:

TOLAZOLINE HYDROCHLORIDE ADRA2B

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Mechanism of Interaction Adrenergic receptor alpha antagonist

Direct Interaction yes

Publications:

BRIMONIDINE TARTRATE ADRA2B

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Mechanism of Interaction Adrenergic receptor alpha-2 agonist

Direct Interaction yes

Publications:

DIPIVEFRIN HYDROCHLORIDE ADRA2B

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Mechanism of Interaction Adrenergic receptor agonist

Direct Interaction yes

Publications:

METHYLDOPA ADRA2B

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Mechanism of Interaction Adrenergic receptor alpha-2 agonist

Direct Interaction yes

Publications:

PHENOXYBENZAMINE HYDROCHLORIDE ADRA2B

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Mechanism of Interaction Adrenergic receptor alpha antagonist

Direct Interaction yes

Publications:

GUANFACINE HYDROCHLORIDE ADRA2B

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Mechanism of Interaction Adrenergic receptor alpha-2 agonist

Direct Interaction yes

Publications:

RAUWOLSCINE ADRA2B

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Specific Action of the Ligand Antagonist

Endogenous Drug? False

Publications:

NOREPINEPHRINE BITARTRATE ADRA2B

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Mechanism of Interaction Adrenergic receptor agonist

Direct Interaction yes

Publications:

ESMIRTAZAPINE MALEATE ADRA2B

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Mechanism of Interaction Adrenergic receptor alpha-2 antagonist

Direct Interaction yes

Publications:

chembl:CHEMBL362051 ADRA2B

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Specific Action of the Ligand Antagonist

Endogenous Drug? False

Publications:

TERGURIDE ADRA2B

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Specific Action of the Ligand Antagonist

Endogenous Drug? False

Publications:

GUANFACINE ADRA2B

Interaction Types & Directionality:

agonist (activating)

binder

Interaction Info:

Direct Interaction? True

Endogenous Drug? False

Specific Action of the Ligand Full agonist

Publications:

Uhlén et al., 1991, Delineation of rat kidney alpha 2A- and alpha 2B-adrenoceptors with [3H]RX821002 radioligand binding: computer modelling reveals that guanfacine is an alpha 2A-selective compound., Eur. J. Pharmacol.

OXYMETAZOLINE ADRA2B

Interaction Types & Directionality:

binder

agonist (activating)

Interaction Info:

Specific Action of the Ligand Partial agonist

Endogenous Drug? False

Publications:

Uhlén et al., 1991, Delineation of rat kidney alpha 2A- and alpha 2B-adrenoceptors with [3H]RX821002 radioligand binding: computer modelling reveals that guanfacine is an alpha 2A-selective compound., Eur. J. Pharmacol.

Gaulton et al., 2012, ChEMBL: a large-scale bioactivity database for drug discovery., Nucleic Acids Res.

NOREPINEPHRINE ADRA2B

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Trial Name -

Novel drug target Established target

Publications:

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

Vizi et al., 2001, Evidence for presynaptic cannabinoid CB(1) receptor-mediated inhibition of noradrenaline release in the guinea pig lung., Eur. J. Pharmacol.

Gobbi et al., 1990, The modulation of [3H]noradrenaline and [3H]serotonin release from rat brain synaptosomes is not mediated by the alpha 2B-adrenoceptor subtype., Naunyn Schmiedebergs Arch. Pharmacol.

BRIMONIDINE ADRA2B

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Specific Action of the Ligand Partial agonist

Endogenous Drug? False

Direct Interaction? True

Publications:

Bohmann et al., 1993, Methoxamine inhibits noradrenaline release through activation of alpha 1- and alpha 2-adrenoceptors in rat isolated kidney: involvement of purines and prostaglandins., Naunyn Schmiedebergs Arch. Pharmacol.

Trendelenburg et al., 2003, All three alpha2-adrenoceptor types serve as autoreceptors in postganglionic sympathetic neurons., Naunyn Schmiedebergs Arch. Pharmacol.

ASENAPINE ADRA2B

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Novel drug target Established target

Trial Name Asenapine

Publications:

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

EPINEPHRINE ADRA2B

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Trial Name transdermal lidocaine/epinephrine patch,Lidosite

Novel drug target Established target

Mechanism of Interaction Adrenergic receptor agonist

Publications:

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

Gobbi et al., 1990, The modulation of [3H]noradrenaline and [3H]serotonin release from rat brain synaptosomes is not mediated by the alpha 2B-adrenoceptor subtype., Naunyn Schmiedebergs Arch. Pharmacol.

Rudling et al., 2000, A comparison of agonist-specific coupling of cloned human alpha(2)-adrenoceptor subtypes., Br. J. Pharmacol.

PRAZOSIN ADRA2B

Interaction Types & Directionality:

antagonist (inhibitory)

binder

Interaction Info:

Specific Action of the Ligand Antagonist

Endogenous Drug? False

Publications:

Uhlén et al., 1991, Delineation of rat kidney alpha 2A- and alpha 2B-adrenoceptors with [3H]RX821002 radioligand binding: computer modelling reveals that guanfacine is an alpha 2A-selective compound., Eur. J. Pharmacol.

Adams HR, 1983, Pharmacologic problems in circulation research: alpha adrenergic blocking drugs., Circ Shock

Bylund DB, 1985, Heterogeneity of alpha-2 adrenergic receptors., Pharmacol Biochem Behav

RISPERIDONE ADRA2B

Interaction Types & Directionality:

antagonist (inhibitory)

agonist (activating)

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

CABERGOLINE ADRA2B

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Specific Action of the Ligand Antagonist

Endogenous Drug? False

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.

Sharif et al., 2009, Cabergoline: Pharmacology, ocular hypotensive studies in multiple species, and aqueous humor dynamic modulation in the Cynomolgus monkey eyes., Exp. Eye Res.

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

BROMOCRIPTINE ADRA2B

Interaction Types & Directionality:

antagonist (inhibitory)

agonist (activating)

Interaction Info:

Endogenous Drug? False

Specific Action of the Ligand Antagonist

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

ERGOTAMINE ADRA2B

Interaction Types & Directionality:

partial agonist (activating)

agonist (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

YOHIMBINE ADRA2B

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Direct Interaction? True

Endogenous Drug? False

Specific Action of the Ligand Antagonist

Publications:

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

Gyires et al., 2000, Functional evidence that gastroprotection can be induced by activation of central alpha(2B)-adrenoceptor subtypes in the rat., Eur. J. Pharmacol.

Takada et al., 2002, Meperidine exerts agonist activity at the alpha(2B)-adrenoceptor subtype., Anesthesiology

ARIPIPRAZOLE ADRA2B

Interaction Types & Directionality:

antagonist (inhibitory)

ligand

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

XYLOMETAZOLINE ADRA2B

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Publications:

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

APOMORPHINE ADRA2B

Interaction Types & Directionality:

agonist (activating)

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

LISURIDE ADRA2B

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

CLOZAPINE ADRA2B

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Publications:

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

CARVEDILOL ADRA2B

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.

ETOMIDATE ADRA2B

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Novel drug target Established target

Trial Name -

Publications:

Creagh et al., 2010, Alpha-2B adrenergic receptor mediated hemodynamic profile of etomidate., P R Health Sci J

Paris et al., 2003, Activation of alpha 2B-adrenoceptors mediates the cardiovascular effects of etomidate., Anesthesiology

ZIPRASIDONE ADRA2B

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Publications:

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

LEVOMEPROMAZINE ADRA2B

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.

EPHEDRA ADRA2B

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.

APRACLONIDINE ADRA2B

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Publications:

Liu et al., 1991, Adrenergic mechanism in circadian elevation of intraocular pressure in rabbits., Invest. Ophthalmol. Vis. Sci.

DOXEPIN ADRA2B

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.)

DROXIDOPA ADRA2B

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

Gilsbach et al., 2008, Presynaptic metabotropic receptors for acetylcholine and adrenaline/noradrenaline., Handb Exp Pharmacol

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

METHAMPHETAMINE ADRA2B

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.

QUETIAPINE ADRA2B

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

Jensen et al., 2008, N-desalkylquetiapine, a potent norepinephrine reuptake inhibitor and partial 5-HT1A agonist, as a putative mediator of quetiapine's antidepressant activity., Neuropsychopharmacology

PALIPERIDONE ADRA2B

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.

ROPINIROLE ADRA2B

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Publications:

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

FENOLDOPAM ADRA2B

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.

PERGOLIDE ADRA2B

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

GUANABENZ ADRA2B

Interaction Types & Directionality:

binder

agonist (activating)

Interaction Info:

Specific Action of the Ligand Agonist

Endogenous Drug? False

Direct Interaction? True

Publications:

Uhlén et al., 1991, Delineation of rat kidney alpha 2A- and alpha 2B-adrenoceptors with [3H]RX821002 radioligand binding: computer modelling reveals that guanfacine is an alpha 2A-selective compound., Eur. J. Pharmacol.

ROTIGOTINE ADRA2B

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Publications:

Scheller et al., 2009, The in vitro receptor profile of rotigotine: a new agent for the treatment of Parkinson's disease., Naunyn Schmiedebergs Arch. Pharmacol.

DRONEDARONE ADRA2B

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

PIZOTYLINE ADRA2B

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Publications:

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

CELIPROLOL ADRA2B

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Publications:

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

MIANSERIN ADRA2B

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Publications:

LOXAPINE ADRA2B

Interaction Types & Directionality:

binder

Interaction Info:

Publications:

RACEPINEPHRINE ADRA2B

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Publications:

DEBRISOQUIN ADRA2B

Interaction Types & Directionality:

n/a

Interaction Info:

Trial Name -

Novel drug target Established target

Publications:

SENREBOTASE ADRA2B

Interaction Types & Directionality:

n/a

Interaction Info:

Trial Name AGN-214868

Novel drug target Established target

Publications:

FIPAMEZOLE ADRA2B

Interaction Types & Directionality:

n/a

Interaction Info:

Novel drug target Established target

Trial Name fipamezole, JP-1730

Publications:

BETHANIDINE ADRA2B

Interaction Types & Directionality:

n/a

Interaction Info:

Trial Name -

Novel drug target Established target

Publications:

PRAMIPEXOLE ADRA2B

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

TRIMIPRAMINE ADRA2B

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:

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

HALOPERIDOL ADRA2B

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

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

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

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

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

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 agonist
Direct Interaction	yes

Mechanism of Interaction	Adrenergic receptor alpha agonist
Direct Interaction	yes

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

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>2B</sub>-AR.
Specific Action of the Ligand	Agonist
Endogenous Drug?	False

Direct Interaction	yes
Mechanism of Interaction	Adrenergic receptor alpha antagonist

Mechanism of Interaction	Adrenergic receptor antagonist
Direct Interaction	yes

151
ADRENOCEPTOR ALPHA 2B
ADRA2B
ADRA2L1
ADRA2RL1
ADRARL1
ALPHA2BAR
FAME2
alpha-2BAR
104260
282
ENSG00000274286
OTTHUMG00000188276
ENSG00000181210
ALPHA-2B ADRENERGIC RECEPTOR (ALPHA-2B ADRENOCEPTOR) (ALPHA-2B ADRENORECEPTOR) (SUBTYPE C2). [SOURCE:UNIPROT/SWISSPROT;ACC:P18089]
BE0000572
P18089
ADA2B_HUMAN
ENSG00000222040
ALPHA-2B ADRENERGIC RECEPTOR
Alpha-2B adrenoceptor
Alpha-2B adrenoreceptor
Alpha-2 adrenergic receptor subtype C2
26
α<sub>2B</sub>-adrenoceptor
NP_000673
NM_000682
TTDC00293
SUBTYPE C2
PA36
Adrenergic receptor alpha-2B
T41580

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

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

Mechanism of Interaction	Adrenergic receptor alpha-2 antagonist
Direct Interaction	yes

Trial Name	transdermal lidocaine/epinephrine patch,Lidosite
Novel drug target	Established target
Mechanism of Interaction	Adrenergic receptor agonist

Trial Name	low dose intravenous methamphetamine
Novel drug target	Established target

adrenoceptor alpha 2B	HUGO Gene Name
282	HUGO Gene ID
ADRA2B	Gene Symbol

ADA2B_HUMAN	Uniprot Id
ALPHA-2B ADRENERGIC RECEPTOR	Uniprot Protein Name
ADRA2B	Uniprot Gene Name

ENSG00000181210	Ensembl Gene Id
ALPHA-2B ADRENERGIC RECEPTOR (ALPHA-2B ADRENOCEPTOR) (ALPHA-2B ADRENORECEPTOR) (SUBTYPE C2). [SOURCE:UNIPROT/SWISSPROT;ACC:P18089]	Description
ADRA2B	Display Id

ADRA2B	DrugBank Gene Name
P18089	UniProt Accession
151	Entrez Gene Id

ADRA2RL1	GENE_SYMBOL
ADRA2B	GENE_SYMBOL
Alpha-2B adrenergic receptor	UNIPROT

α<sub>2B</sub>-adrenoceptor	GuideToPharmacology Name
P18089	UniProtKB ID

ADRA2B Gene Record

ADRA2B 151 Druggable Genome

Alternate Names:

Gene Info:

Gene Categories: Category Details

Publications:

Interaction Types & Directionality: agonist (activating)

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

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

Interaction Types & Directionality: antagonist (inhibitory)

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

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: antagonist (inhibitory)

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

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

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: antagonist (inhibitory)

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

Publications:

Interaction Types & Directionality: agonist (activating)

Interaction Info: Mechanism of Interaction Adrenergic receptor alpha agonist 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: 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>2B</sub>-AR. Specific Action of the Ligand Agonist Endogenous Drug? False

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

Publications:

Interaction Types & Directionality: antagonist (inhibitory)

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

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: Mechanism of Interaction Adrenergic receptor alpha-2 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: antagonist (inhibitory)

Interaction Info: Mechanism of Interaction Adrenergic receptor 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 antagonist

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: 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 agonist Direct Interaction yes

Publications:

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

Direct Interaction? True

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

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Trial Name OREX-003, olanzapine plus zonisamide SR

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

Trial Name ALKS 3831

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:

antagonist (inhibitory)

Interaction Info:

Direct Interaction? True

Endogenous Drug? False

Specific Action of the Ligand Antagonist

Publications:

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

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:

antagonist (inhibitory)

Interaction Info:

Endogenous Drug? False

Specific Action of the Ligand Antagonist

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Mechanism of Interaction Adrenergic receptor agonist

Direct Interaction yes

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Specific Action of the Ligand Antagonist

Endogenous Drug? False

Direct Interaction? False

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Mechanism of Interaction Adrenergic receptor alpha 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:

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>2B</sub>-AR.

Specific Action of the Ligand Agonist

Endogenous Drug? False

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Adrenergic receptor alpha antagonist

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Adrenergic receptor alpha-2 agonist

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Direct Interaction? True

Endogenous Drug? False

Specific Action of the Ligand Antagonist

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:

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:

Direct Interaction yes

Mechanism of Interaction Adrenergic receptor alpha antagonist

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:

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:

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 agonist

Direct Interaction yes

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:

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:

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

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:

Mechanism of Interaction Adrenergic receptor agonist

Direct Interaction yes