DGIdb - ADRA2B Gene Record

ADRA2B 151 Druggable Genome

Alternate Names:

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
PA36
Adrenergic receptor alpha-2B
T41580

Gene Info:

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
Target Class	Receptors
Gene Biotype	PROTEIN_CODING

(9 More Sources)

Gene Categories: Category Details

CELL SURFACE
G PROTEIN COUPLED RECEPTOR
DRUGGABLE GENOME

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.
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
Nasrallah, 2008, Atypical antipsychotic-induced metabolic side effects: insights from receptor-binding profiles., Mol. Psychiatry
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.
Rudling et al., 2000, A comparison of agonist-specific coupling of cloned human alpha(2)-adrenoceptor subtypes., Br. J. Pharmacol.
Gilsbach et al., 2008, Presynaptic metabotropic receptors for acetylcholine and adrenaline/noradrenaline., Handb Exp 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
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.
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.
Shahid et al., 2009, Asenapine: a novel psychopharmacologic agent with a unique human receptor signature., J. Psychopharmacol. (Oxford)
Ariëns EJ et al., 1983, Physiological and pharmacological aspects of adrenergic receptor classification., Biochem Pharmacol
Bylund et al., 1988, Alpha-2A and alpha-2B adrenergic receptor subtypes: antagonist binding in tissues and cell lines containing only one subtype., J. Pharmacol. Exp. Ther.
Bylund DB, 1985, Heterogeneity of alpha-2 adrenergic receptors., Pharmacol Biochem Behav
Adams HR, 1983, Pharmacologic problems in circulation research: alpha adrenergic blocking drugs., Circ Shock
Yasuda G et al., 1991, Characterization of prazosin-sensitive alpha 2 B-adrenoceptors expressed by cultured rat IMCD cells., Am J Physiol
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
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
Lam, 2000, Clinical pharmacology of dopamine agonists., Pharmacotherapy
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.
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
Freitag et al., 1996, Adrenoceptor- and cholinoceptor-mediated mechanisms in the regulation of 5-hydroxytryptamine release from isolated tracheae of newborn rabbits., Br. J. Pharmacol.
Millan et al., 2000, Agonist and antagonist actions of yohimbine as compared to fluparoxan at alpha(2)-adrenergic receptors (AR)s, serotonin (5-HT)(1A), 5-HT(1B), 5-HT(1D) and dopamine D(2) and D(3) receptors. Significance for the modulation of frontocortical monoaminergic transmission and depressive states., Synapse
Alonso et al., 2007, Yohimbine prevents morphine-induced changes of glial fibrillary acidic protein in brainstem and alpha2-adrenoceptor gene expression in hippocampus., Neurosci. Lett.
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
Haenisch et al., 2010, Alpha-adrenoceptor agonistic activity of oxymetazoline and xylometazoline., Fundam Clin Pharmacol
Frang et al., 2001, Phenoxybenzamine binding reveals the helical orientation of the third transmembrane domain of adrenergic receptors., J. Biol. Chem.
Koshimizu et al., 2004, Carvedilol selectively inhibits oscillatory intracellular calcium changes evoked by human alpha1D- and alpha1B-adrenergic receptors., Cardiovasc. Res.
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
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.
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.
Liu et al., 1991, Adrenergic mechanism in circadian elevation of intraocular pressure in rabbits., Invest. Ophthalmol. Vis. Sci.
Giovannoni et al., 2009, Alpha2-agonists as analgesic agents., Med Res Rev
Davis, 2010, Recent advances in the treatment of pain., F1000 Med Rep
Jeng et al., 1998, Methamphetamine modulates GABA-induced electrophysiological depression by alternating noradrenergic actions in cerebellar Purkinje neurons., Psychopharmacology (Berl.)
Suttajit S et al., 2014, Quetiapine for acute bipolar depression: a systematic review and meta-analysis., Drug Des Devel Ther
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
Trendelenburg et al., 1997, Presynaptic alpha 2A/D-autoreceptors in the brain cortex of Cercopithecus aethiops., Naunyn Schmiedebergs Arch. Pharmacol.
Martin et al., 1995, Renal vasodilatation by dopexamine and fenoldopam due to alpha 1-adrenoceptor blockade., Br. J. Pharmacol.
Berger et al., 1996, Trimipramine: a challenge to current concepts on antidepressives., Eur Arch Psychiatry Clin Neurosci
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.
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
Mylecharane EJ, 1991, 5-HT2 receptor antagonists and migraine therapy., J Neurol
Kroeze et al., 2003, H1-histamine receptor affinity predicts short-term weight gain for typical and atypical antipsychotic drugs., Neuropsychopharmacology
Nawarskas JJ et al., 2017, Celiprolol: A Unique Selective Adrenoceptor Modulator., Cardiol Rev

GUANABENZ ADRA2B

Interaction Score: 0.46

Interaction Types & Directionality:

binder

agonist (activating)

Interaction Info:

Specific Action of the Ligand Agonist

Endogenous Drug? False

Direct Interaction? True

PMIDs:
1666366

Sources:
DrugBank GuideToPharmacology
BRIMONIDINE ADRA2B

Interaction Score: 0.41

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Specific Action of the Ligand Partial agonist

Endogenous Drug? False

Direct Interaction? True

PMIDs:
8097565 14610637

Sources:
DrugBank TEND GuideToPharmacology PharmGKB
YOHIMBINE ADRA2B

Interaction Score: 0.36

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Direct Interaction? True

Endogenous Drug? False

Specific Action of the Ligand Antagonist

PMIDs:
12110610 10822066 12170055 8872361 10611634 17123717

Sources:
DrugBank TdgClinicalTrial TEND GuideToPharmacology PharmGKB
PRAZOSIN ADRA2B

Interaction Score: 0.33

Interaction Types & Directionality:

antagonist (inhibitory)

binder

Interaction Info:

Specific Action of the Ligand Antagonist

Endogenous Drug? False

PMIDs:
1666366 2835476 2989948 6133635 1719824

Sources:
DrugBank GuideToPharmacology
DROXIDOPA ADRA2B

Interaction Score: 0.31

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Mechanism of Interaction Adrenergic receptor agonist

Direct Interaction yes

PMIDs:
18680204 18064417 21173850

Sources:
DrugBank ChemblInteractions
APRACLONIDINE ADRA2B

Interaction Score: 0.31

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

PMIDs:
1676991

Sources:
DrugBank
CLONIDINE ADRA2B

Interaction Score: 0.28

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Specific Action of the Ligand Partial agonist

Endogenous Drug? False

Direct Interaction? True

PMIDs:
11082457

Sources:
DrugBank TdgClinicalTrial ChemblInteractions GuideToPharmacology PharmGKB
TOLAZOLINE ADRA2B

Interaction Score: 0.26

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

PMIDs:
9089664

Sources:
DrugBank GuideToPharmacology
GUANFACINE ADRA2B

Interaction Score: 0.26

Interaction Types & Directionality:

agonist (activating)

binder

Interaction Info:

Direct Interaction? True

Endogenous Drug? False

Specific Action of the Ligand Full agonist

PMIDs:
1666366

Sources:
DrugBank GuideToPharmacology
FENOLDOPAM ADRA2B

Interaction Score: 0.26

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

PMIDs:
17016423 17139284 7670737

Sources:
DrugBank TEND
NOREPINEPHRINE ADRA2B

Interaction Score: 0.25

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
1980236 11728431 1979424 11053214 18064417 17016423 17139284

Sources:
DrugBank TdgClinicalTrial TEND PharmGKB
CHEMBL362051 ADRA2B

Interaction Score: 0.21

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Specific Action of the Ligand Antagonist

Endogenous Drug? False

PMIDs:
None found

Sources:
GuideToPharmacology
BRIMONIDINE TARTRATE ADRA2B

Interaction Score: 0.21

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Mechanism of Interaction Adrenergic receptor alpha-2 agonist

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
TIZANIDINE HYDROCHLORIDE ADRA2B

Interaction Score: 0.21

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Mechanism of Interaction Adrenergic receptor alpha-2 agonist

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
APRACLONIDINE HYDROCHLORIDE ADRA2B

Interaction Score: 0.21

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Mechanism of Interaction Adrenergic receptor alpha-2 agonist

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
XYLAZINE ADRA2B

Interaction Score: 0.21

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Specific Action of the Ligand Partial agonist

Endogenous Drug? False

PMIDs:
None found

Sources:
GuideToPharmacology
METHYLDOPATE HYDROCHLORIDE ADRA2B

Interaction Score: 0.21

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Mechanism of Interaction Adrenergic receptor alpha-2 agonist

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
FADOLMIDINE HYDROCHLORIDE ADRA2B

Interaction Score: 0.21

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Mechanism of Interaction Adrenergic receptor alpha-2 agonist

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
DEXMEDETOMIDINE HYDROCHLORIDE ADRA2B

Interaction Score: 0.21

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Adrenergic receptor alpha-2 agonist

PMIDs:
None found

Sources:
ChemblInteractions
FIPAMEZOLE ADRA2B

Interaction Score: 0.21

Interaction Types & Directionality:

n/a

Interaction Info:

Novel drug target Established target

Trial Name fipamezole, JP-1730

PMIDs:
None found

Sources:
TdgClinicalTrial

LOFEXIDINE ADRA2B

Interaction Score: 0.21

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

PMIDs:
None found

Sources:
TdgClinicalTrial TEND GuideToPharmacology

TIZANIDINE ADRA2B

Interaction Score: 0.21

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Trial Name NVD-422, tizanidine oral spray

Novel drug target Established target

Trial Name tizanidine hydrochloride,Zanaflex

PMIDs:
8930173

Sources:
TdgClinicalTrial
CLONIDINE HYDROCHLORIDE ADRA2B

Interaction Score: 0.21

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Mechanism of Interaction Adrenergic receptor alpha-2 agonist

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
OXYMETAZOLINE ADRA2B

Interaction Score: 0.21

Interaction Types & Directionality:

binder

agonist (activating)

Interaction Info:

Specific Action of the Ligand Partial agonist

Endogenous Drug? False

PMIDs:
1666366 21948594

Sources:
DrugBank GuideToPharmacology
EPINEPHRINE ADRA2B

Interaction Score: 0.2

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

PMIDs:
1980236 1979424 11053214 11728431 18064417 6134529

Sources:
DrugBank TdgClinicalTrial ChemblInteractions PharmGKB
EPHEDRA ADRA2B

Interaction Score: 0.19

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

PMIDs:
14570629 15955613 12954796

Sources:
DrugBank
CABERGOLINE ADRA2B

Interaction Score: 0.19

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Specific Action of the Ligand Antagonist

Endogenous Drug? False

PMIDs:
12388667 18992242 18691132 10641988

Sources:
DrugBank GuideToPharmacology
ETOMIDATE ADRA2B

Interaction Score: 0.18

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Novel drug target Established target

Trial Name -

PMIDs:
20496522 14508322

Sources:
DrugBank TdgClinicalTrial TEND
CELIPROLOL ADRA2B

Interaction Score: 0.18

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

PMIDs:
28742547

Sources:
DrugBank
ROTIGOTINE ADRA2B

Interaction Score: 0.18

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

PMIDs:
18704368

Sources:
DrugBank
XYLOMETAZOLINE ADRA2B

Interaction Score: 0.18

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

PMIDs:
20030735

Sources:
DrugBank
DEBRISOQUIN ADRA2B

Interaction Score: 0.18

Interaction Types & Directionality:

n/a

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
None found

Sources:
TdgClinicalTrial TEND
GUANFACINE HYDROCHLORIDE ADRA2B

Interaction Score: 0.15

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Mechanism of Interaction Adrenergic receptor alpha-2 agonist

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
MOXONIDINE ADRA2B

Interaction Score: 0.15

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
TTD
GUANABENZ ACETATE ADRA2B

Interaction Score: 0.15

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Adrenergic receptor alpha-2 agonist

PMIDs:
None found

Sources:
ChemblInteractions
BETHANIDINE ADRA2B

Interaction Score: 0.14

Interaction Types & Directionality:

n/a

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
None found

Sources:
TdgClinicalTrial TEND
PHENOXYBENZAMINE ADRA2B

Interaction Score: 0.13

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Direct Interaction? True

Endogenous Drug? False

Specific Action of the Ligand Antagonist

PMIDs:
11395517

Sources:
DrugBank GuideToPharmacology
RAUWOLFIA SERPENTINA ADRA2B

Interaction Score: 0.12

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Adrenergic receptor alpha antagonist

PMIDs:
None found

Sources:
ChemblInteractions
LEVOMEPROMAZINE ADRA2B

Interaction Score: 0.12

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

PMIDs:
6149771 15701205 2870716

Sources:
DrugBank
LISURIDE ADRA2B

Interaction Score: 0.11

Interaction Types & Directionality:

antagonist (inhibitory)

other/unknown

Interaction Info:

Specific Action of the Ligand Antagonist

Endogenous Drug? False

PMIDs:
18691132

Sources:
DrugBank GuideToPharmacology
ESMIRTAZAPINE MALEATE ADRA2B

Interaction Score: 0.1

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Mechanism of Interaction Adrenergic receptor alpha-2 antagonist

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
MEDETOMIDINE ADRA2B

Interaction Score: 0.1

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
TTD
PERGOLIDE ADRA2B

Interaction Score: 0.1

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Specific Action of the Ligand Partial agonist

Endogenous Drug? False

PMIDs:
18691132 10641988

Sources:
GuideToPharmacology
ALSEROXYLON ADRA2B

Interaction Score: 0.1

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Mechanism of Interaction Adrenergic receptor alpha antagonist

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
NAPHAZOLINE HYDROCHLORIDE ADRA2B

Interaction Score: 0.1

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Mechanism of Interaction Adrenergic receptor alpha agonist

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
TETRAHYDROZOLINE HYDROCHLORIDE ADRA2B

Interaction Score: 0.1

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Mechanism of Interaction Adrenergic receptor alpha agonist

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
SENREBOTASE ADRA2B

Interaction Score: 0.1

Interaction Types & Directionality:

n/a

Interaction Info:

Trial Name AGN-214868

Novel drug target Established target

PMIDs:
None found

Sources:
TdgClinicalTrial
BROMOCRIPTINE ADRA2B

Interaction Score: 0.1

Interaction Types & Directionality:

antagonist (inhibitory)

agonist (activating)

Interaction Info:

Endogenous Drug? False

Specific Action of the Ligand Antagonist

PMIDs:
20138024 18691132 10641988

Sources:
DrugBank GuideToPharmacology
METHAMPHETAMINE ADRA2B

Interaction Score: 0.09

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Trial Name low dose intravenous methamphetamine

Novel drug target Established target

PMIDs:
9551769 15955613

Sources:
DrugBank TdgClinicalTrial
RAUWOLSCINE ADRA2B

Interaction Score: 0.09

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Specific Action of the Ligand Antagonist

Endogenous Drug? False

PMIDs:
None found

Sources:
GuideToPharmacology
OXYMETAZOLINE HYDROCHLORIDE ADRA2B

Interaction Score: 0.09

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Mechanism of Interaction Adrenergic receptor alpha agonist

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
ASENAPINE ADRA2B

Interaction Score: 0.08

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Novel drug target Established target

Trial Name Asenapine

PMIDs:
18308814

Sources:
DrugBank TdgClinicalTrial
PIZOTYLINE ADRA2B

Interaction Score: 0.08

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

PMIDs:
2045831

Sources:
DrugBank
DIPIVEFRIN HYDROCHLORIDE ADRA2B

Interaction Score: 0.08

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Mechanism of Interaction Adrenergic receptor agonist

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
TOLAZOLINE HYDROCHLORIDE ADRA2B

Interaction Score: 0.08

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Mechanism of Interaction Adrenergic receptor alpha antagonist

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
DEXMEDETOMIDINE ADRA2B

Interaction Score: 0.08

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Specific Action of the Ligand Full agonist

Endogenous Drug? False

Direct Interaction? True

PMIDs:
None found

Sources:
GuideToPharmacology
MEPHENTERMINE SULFATE ADRA2B

Interaction Score: 0.08

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Mechanism of Interaction Adrenergic receptor agonist

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
PHENTOLAMINE MESYLATE ADRA2B

Interaction Score: 0.08

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Mechanism of Interaction Adrenergic receptor alpha antagonist

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
APOMORPHINE ADRA2B

Interaction Score: 0.08

Interaction Types & Directionality:

agonist (activating)

antagonist (inhibitory)

Interaction Info:

Specific Action of the Ligand Antagonist

Endogenous Drug? False

PMIDs:
18691132

Sources:
DrugBank GuideToPharmacology
PHENOXYBENZAMINE HYDROCHLORIDE ADRA2B

Interaction Score: 0.07

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Mechanism of Interaction Adrenergic receptor alpha antagonist

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
LABETALOL HYDROCHLORIDE ADRA2B

Interaction Score: 0.07

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Mechanism of Interaction Adrenergic receptor antagonist

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
HYDROXYAMPHETAMINE HYDROBROMIDE ADRA2B

Interaction Score: 0.07

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Mechanism of Interaction Adrenergic receptor agonist

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
QUETIAPINE ADRA2B

Interaction Score: 0.07

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

PMIDs:
11132243 17848919 25028535 18059438

Sources:
DrugBank
DRONEDARONE ADRA2B

Interaction Score: 0.06

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

PMIDs:
17389667 23997577

Sources:
DrugBank
SPIROXATRINE ADRA2B

Interaction Score: 0.06

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Specific Action of the Ligand Antagonist

Endogenous Drug? False

PMIDs:
None found

Sources:
GuideToPharmacology
TRIMIPRAMINE ADRA2B

Interaction Score: 0.06

Interaction Types & Directionality:

other/unknown

Interaction Info:

PMIDs:
8863001

Sources:
DrugBank
PALIPERIDONE ADRA2B

Interaction Score: 0.06

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

PMIDs:
11132243

Sources:
DrugBank
MIRTAZAPINE ADRA2B

Interaction Score: 0.06

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Direct Interaction? True

Endogenous Drug? False

Specific Action of the Ligand Antagonist

PMIDs:
None found

Sources:
ChemblInteractions GuideToPharmacology
CHEMBL609728 ADRA2B

Interaction Score: 0.05

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DrugBank
RACEPINEPHRINE ADRA2B

Interaction Score: 0.05

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

PMIDs:
None found

Sources:
DrugBank
LEVONORDEFRIN ADRA2B

Interaction Score: 0.05

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Mechanism of Interaction Adrenergic receptor alpha-2 agonist

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
ERGOLOID MESYLATES ADRA2B

Interaction Score: 0.05

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Adrenergic receptor alpha antagonist

PMIDs:
None found

Sources:
ChemblInteractions
TERGURIDE ADRA2B

Interaction Score: 0.05

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Specific Action of the Ligand Antagonist

Endogenous Drug? False

PMIDs:
None found

Sources:
GuideToPharmacology
PHENTOLAMINE ADRA2B

Interaction Score: 0.05

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Specific Action of the Ligand Antagonist

Endogenous Drug? False

PMIDs:
None found

Sources:
GuideToPharmacology
NOREPINEPHRINE BITARTRATE ADRA2B

Interaction Score: 0.04

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Mechanism of Interaction Adrenergic receptor agonist

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
ROXINDOLE ADRA2B

Interaction Score: 0.04

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Endogenous Drug? False

Specific Action of the Ligand Antagonist

PMIDs:
None found

Sources:
GuideToPharmacology
OCAPERIDONE ADRA2B

Interaction Score: 0.04

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DrugBank
ARIPIPRAZOLE ADRA2B

Interaction Score: 0.04

Interaction Types & Directionality:

antagonist (inhibitory)

ligand

Interaction Info:

PMIDs:
17848919 26346901

Sources:
DrugBank
CARVEDILOL ADRA2B

Interaction Score: 0.04

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

PMIDs:
15306222

Sources:
DrugBank
EPINEPHRINE BITARTRATE ADRA2B

Interaction Score: 0.04

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Adrenergic receptor agonist

PMIDs:
None found

Sources:
ChemblInteractions
ZOTEPINE ADRA2B

Interaction Score: 0.04

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Specific Action of the Ligand Antagonist

Endogenous Drug? False

Direct Interaction? False

PMIDs:
None found

Sources:
GuideToPharmacology
RISPERIDONE ADRA2B

Interaction Score: 0.04

Interaction Types & Directionality:

antagonist (inhibitory)

agonist (activating)

Interaction Info:

PMIDs:
11132243 15907153 25943458

Sources:
DrugBank
ZIPRASIDONE ADRA2B

Interaction Score: 0.04

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

PMIDs:
17848919

Sources:
DrugBank
MIANSERIN ADRA2B

Interaction Score: 0.02

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

PMIDs:
None found

Sources:
DrugBank
DOPAMINE ADRA2B

Interaction Score: 0.02

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
PharmGKB
LOXAPINE ADRA2B

Interaction Score: 0.02

Interaction Types & Directionality:

binder

Interaction Info:

PMIDs:
None found

Sources:
DrugBank
ISOPROTERENOL ADRA2B

Interaction Score: 0.02

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
PharmGKB
OLANZAPINE ADRA2B

Interaction Score: 0.02

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)

PMIDs:
17848919

Sources:
TdgClinicalTrial
HALOPERIDOL ADRA2B

Interaction Score: 0.02

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
12629531

Sources:
DrugBank
CLOZAPINE ADRA2B

Interaction Score: 0.02

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

PMIDs:
17848919

Sources:
DrugBank
CHLORPROMAZINE ADRA2B

Interaction Score: 0.02

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Specific Action of the Ligand Antagonist

Endogenous Drug? False

PMIDs:
None found

Sources:
GuideToPharmacology
METHYLDOPA ADRA2B

Interaction Score: 0.0

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Mechanism of Interaction Adrenergic receptor alpha-2 agonist

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions

Ensembl: ENSG00000274286
- Version: 101_38
Alternate Names:

ADRA2B Ensembl Gene Name

Gene Info:

Gene Biotype PROTEIN_CODING

Publications:
HopkinsGroom: P18089
- Version: 11-September-2012
Alternate Names:

ADA2B_HUMAN Uniprot Id

ALPHA-2B ADRENERGIC RECEPTOR Uniprot Protein Name

ADRA2B Uniprot Gene Name

Gene Info:

Uniprot Status Swiss-Prot

Interpro Short Name 7TM_GPCR_Rhodpsn

Human Readable Name G PROTEIN COUPLED RECEPTOR

Gene Categories:

G PROTEIN COUPLED RECEPTOR, DRUGGABLE GENOME

Publications:
TdgClinicalTrial: P18089
- Version: January-2014
Alternate Names:

ADRA2B Gene Symbol

Gene Info:

Target Class Receptors

Target Subclass GPCR

Target Subclass Rhodopsin

Publications:

RussLampel: ENSG00000181210

Version: 26-July-2011

Alternate Names:

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

Gene Info:

Human Readable Name DRUGGABLE GENOME

Gene Categories:

DRUGGABLE GENOME

Publications:

TEND: P18089
- Version: 01-August-2011
Alternate Names:

ADA2B_HUMAN Uniprot Id

ENSG00000222040 Ensembl Gene Id

ADRA2B Gene Symbol

Gene Info:

Transmembrane Helix Count 7

Target Subclass Rhodopsin

Target Subclass GPCR

Publications:
GuideToPharmacology: 151
- Version: 29-September-2020
Alternate Names:

282 HUGO Gene ID

282 HUGO Gene Symbol

adrenoceptor alpha 2B HUGO Gene Name

Gene Info:

GuideToPharmacology Gene Category Name Adrenoceptors

GuideToPharmacology Gene Category ID 4

Gene Categories:

G PROTEIN COUPLED RECEPTOR

Publications:

DrugBank: BE0000572

Version: 5.1.7

Alternate Names:

ADRA2B DrugBank Gene Name

P18089 UniProt Accession

151 Entrez Gene Id

Gene Info:

Publications:

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

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

HingoraniCasas: ENSG00000222040
- Version: 31-May-2017
Alternate Names:

ENSG00000222040 Gene Symbol

ADRA2B Ensembl Id

Gene Info:

Gene Categories:

DRUGGABLE GENOME

Publications:
ChemblInteractions: ADRA2L1
- Version: chembl_23
Alternate Names:

ADRA2RL1 GENE_SYMBOL

ADRA2B GENE_SYMBOL

Alpha-2B adrenergic receptor UNIPROT

Gene Info:

Publications:
PharmGKB: ADRA2B
- Version: 18-August-2020
Alternate Names:

PA36 PharmGKB ID

Gene Info:

Publications:
GO: ADRA2B
- Version: 05-September-2020
Alternate Names:

ADRA2L1 GO Gene Synonym

ADRA2RL1 GO Gene Synonym

Gene Info:

Gene Categories:

CELL SURFACE, G PROTEIN COUPLED RECEPTOR

Publications:
dGene: ADRA2B
- Version: 27-Jun-2013
Alternate Names:

151 Gene ID

ADRA2L1 dGene Synonym

ADRA2RL1 dGene Synonym

Gene Info:

Gene Categories:

G PROTEIN COUPLED RECEPTOR

Publications:
TTD: Adrenergic receptor alpha-2B
- Version: 2020.06.01
Alternate Names:

ADRA2B TTD Gene Abbreviation

T41580 TTD Target ID

Gene Info:

Publications:

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

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

Specific Action of the Ligand	Antagonist
Endogenous Drug?	False

Mechanism of Interaction	Adrenergic receptor agonist
Direct Interaction	yes

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 agonist
Direct Interaction	yes

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

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

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

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

antagonist (inhibitory)
binder

binder
antagonist (inhibitory)

Direct Interaction	yes
Mechanism of Interaction	Adrenergic receptor alpha antagonist

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

Mechanism of Interaction	Adrenergic receptor alpha agonist
Direct Interaction	yes

Trial Name	low dose intravenous methamphetamine
Novel drug target	Established target

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

Mechanism of Interaction	Adrenergic receptor antagonist
Direct Interaction	yes

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

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

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

ADRA2B Gene Record

ADRA2B 151 Druggable Genome

Alternate Names:

Gene Info:

Gene Categories: Category Details

Publications:

Interaction Types & Directionality: binder agonist (activating)

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

PMIDs: 1666366

Sources: DrugBank GuideToPharmacology

Interaction Types & Directionality: agonist (activating)

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

PMIDs: 8097565 14610637

Sources: DrugBank TEND GuideToPharmacology PharmGKB

Interaction Types & Directionality: antagonist (inhibitory)

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

PMIDs: 12110610 10822066 12170055 8872361 10611634 17123717

Sources: DrugBank TdgClinicalTrial TEND GuideToPharmacology PharmGKB

Interaction Types & Directionality: antagonist (inhibitory) binder

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

PMIDs: 1666366 2835476 2989948 6133635 1719824

Sources: DrugBank GuideToPharmacology

Interaction Types & Directionality: agonist (activating)

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

PMIDs: 18680204 18064417 21173850

Sources: DrugBank ChemblInteractions

Interaction Types & Directionality: agonist (activating)

Interaction Info:

PMIDs: 1676991

Sources: DrugBank

Interaction Types & Directionality: agonist (activating)

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

PMIDs: 11082457

Sources: DrugBank TdgClinicalTrial ChemblInteractions GuideToPharmacology PharmGKB

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

PMIDs: 9089664

Sources: DrugBank GuideToPharmacology

Interaction Types & Directionality: agonist (activating) binder

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

PMIDs: 1666366

Sources: DrugBank GuideToPharmacology

Interaction Types & Directionality: antagonist (inhibitory)

Interaction Info:

PMIDs: 17016423 17139284 7670737

Sources: DrugBank TEND

Interaction Types & Directionality: agonist (activating)

Interaction Info: Trial Name - Novel drug target Established target

PMIDs: 1980236 11728431 1979424 11053214 18064417 17016423 17139284

Sources: DrugBank TdgClinicalTrial TEND PharmGKB

Interaction Types & Directionality: antagonist (inhibitory)

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

PMIDs: None found

Sources: GuideToPharmacology

Interaction Types & Directionality: agonist (activating)

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

PMIDs: None found

Sources: ChemblInteractions

Interaction Types & Directionality: agonist (activating)

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

PMIDs: None found

Sources: ChemblInteractions

Interaction Types & Directionality: agonist (activating)

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

PMIDs: None found

Sources: ChemblInteractions

Interaction Types & Directionality: agonist (activating)

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

PMIDs: None found

Sources: GuideToPharmacology

Interaction Types & Directionality: agonist (activating)

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

PMIDs: None found

Sources: ChemblInteractions

Interaction Types & Directionality: agonist (activating)

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

PMIDs: None found

Sources: ChemblInteractions

Interaction Types & Directionality: agonist (activating)

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

Interaction Types & Directionality:

binder

agonist (activating)

Interaction Info:

Specific Action of the Ligand Agonist

Endogenous Drug? False

Direct Interaction? True

PMIDs:
1666366

Sources:
DrugBank GuideToPharmacology

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Specific Action of the Ligand Partial agonist

Endogenous Drug? False

Direct Interaction? True

PMIDs:
8097565 14610637

Sources:
DrugBank TEND GuideToPharmacology PharmGKB

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Direct Interaction? True

Endogenous Drug? False

Specific Action of the Ligand Antagonist

PMIDs:
12110610 10822066 12170055 8872361 10611634 17123717

Sources:
DrugBank TdgClinicalTrial TEND GuideToPharmacology PharmGKB

Interaction Types & Directionality:

antagonist (inhibitory)

binder

Interaction Info:

Specific Action of the Ligand Antagonist

Endogenous Drug? False

PMIDs:
1666366 2835476 2989948 6133635 1719824

Sources:
DrugBank GuideToPharmacology

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Mechanism of Interaction Adrenergic receptor agonist

Direct Interaction yes

PMIDs:
18680204 18064417 21173850

Sources:
DrugBank ChemblInteractions

Interaction Types & Directionality:

agonist (activating)

PMIDs:
1676991

Sources:
DrugBank

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Specific Action of the Ligand Partial agonist

Endogenous Drug? False

Direct Interaction? True

PMIDs:
11082457

Sources:
DrugBank TdgClinicalTrial ChemblInteractions GuideToPharmacology PharmGKB

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

PMIDs:
9089664

Sources:
DrugBank GuideToPharmacology

Interaction Types & Directionality:

agonist (activating)

binder

Interaction Info:

Direct Interaction? True

Endogenous Drug? False

Specific Action of the Ligand Full agonist

PMIDs:
1666366

Sources:
DrugBank GuideToPharmacology

Interaction Types & Directionality:

antagonist (inhibitory)

PMIDs:
17016423 17139284 7670737

Sources:
DrugBank TEND

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
1980236 11728431 1979424 11053214 18064417 17016423 17139284

Sources:
DrugBank TdgClinicalTrial TEND PharmGKB

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Specific Action of the Ligand Antagonist

Endogenous Drug? False

PMIDs:
None found

Sources:
GuideToPharmacology

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Mechanism of Interaction Adrenergic receptor alpha-2 agonist

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Mechanism of Interaction Adrenergic receptor alpha-2 agonist

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Mechanism of Interaction Adrenergic receptor alpha-2 agonist

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Specific Action of the Ligand Partial agonist

Endogenous Drug? False

PMIDs:
None found

Sources:
GuideToPharmacology

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Mechanism of Interaction Adrenergic receptor alpha-2 agonist

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Mechanism of Interaction Adrenergic receptor alpha-2 agonist

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Adrenergic receptor alpha-2 agonist

PMIDs:
None found

Sources:
ChemblInteractions

Interaction Types & Directionality:

n/a

Interaction Info:

Novel drug target Established target

Trial Name fipamezole, JP-1730

PMIDs:
None found

Sources:
TdgClinicalTrial

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

ADRA2B	DrugBank Gene Name
P18089	UniProt Accession
151	Entrez Gene Id

ADRA2RL1	GENE_SYMBOL
ADRA2B	GENE_SYMBOL
Alpha-2B adrenergic receptor	UNIPROT