DGIdb - ADRA2C Gene Record

ADRA2C 152 Druggable Genome

Alternate Names:

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
PA37
Adrenergic receptor alpha-2C
T01777

Gene Info:

GuideToPharmacology Gene Category Name	Adrenoceptors
GuideToPharmacology Gene Category ID	4
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

(7 More Sources)

Gene Categories: Category Details

G PROTEIN COUPLED RECEPTOR
DRUGGABLE GENOME

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
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.
Shreve et al., 1991, Alpha 2A- and alpha 2C-adrenoceptor subtypes are differentially down-regulated by norepinephrine., Eur. 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
Nasrallah, 2008, Atypical antipsychotic-induced metabolic side effects: insights from receptor-binding profiles., Mol. Psychiatry
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.
Lalchandani et al., 2002, Yohimbine dimers exhibiting selectivity for the human alpha 2C-adrenoceptor subtype., J. Pharmacol. Exp. Ther.
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
Cleary et al., 2005, The alpha (1D)-adrenoceptor antagonist BMY 7378 is also an alpha (2C)-adrenoceptor antagonist., Auton Autacoid Pharmacol
Shahid et al., 2009, Asenapine: a novel psychopharmacologic agent with a unique human receptor signature., J. Psychopharmacol. (Oxford)
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.
Haenisch et al., 2010, Alpha-adrenoceptor agonistic activity of oxymetazoline and xylometazoline., Fundam Clin Pharmacol
Bylund, 1992, Subtypes of alpha 1- and alpha 2-adrenergic receptors., FASEB J.
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.
Trendelenburg et al., 2003, All three alpha2-adrenoceptor types serve as autoreceptors in postganglionic sympathetic neurons., Naunyn Schmiedebergs Arch. Pharmacol.
Martin et al., 1995, Renal vasodilatation by dopexamine and fenoldopam due to alpha 1-adrenoceptor blockade., Br. J. Pharmacol.
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.
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.
Trendelenburg et al., 1997, Presynaptic alpha 2A/D-autoreceptors in the brain cortex of Cercopithecus aethiops., Naunyn Schmiedebergs Arch. Pharmacol.
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.
O'Connor CM et al., 2012, Combinatorial pharmacogenetic interactions of bucindolol and β1, α2C adrenergic receptor polymorphisms., PLoS One
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
George et al., 2013, Newer antipsychotics and upcoming molecules for schizophrenia., Eur. J. Clin. Pharmacol.
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.
Giovannoni et al., 2009, Alpha2-agonists as analgesic agents., Med Res Rev
Davis, 2010, Recent advances in the treatment of pain., F1000 Med Rep

TETRASUL ADRA2C

Interaction Score: 0.77

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
TTD
PROPYLHEXEDRINE ADRA2C

Interaction Score: 0.77

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
TTD
ORM-12741 ADRA2C

Interaction Score: 0.77

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
TTD
XYLOMETAZOLINE ADRA2C

Interaction Score: 0.77

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

PMIDs:
20030735

Sources:
TTD
TETRAHYDROZOLINE ADRA2C

Interaction Score: 0.77

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
TTD
AMEZINIUM ADRA2C

Interaction Score: 0.77

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
TTD
BRIMONIDINE ADRA2C

Interaction Score: 0.68

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Specific Action of the Ligand Partial agonist

Endogenous Drug? False

Direct Interaction? True

PMIDs:
16757535 12670699 11606316 14610637

Sources:
TEND GuideToPharmacology PharmGKB TTD

LOFEXIDINE ADRA2C

Interaction Score: 0.58

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.

PMIDs:
None found

Sources:
TdgClinicalTrial TEND GuideToPharmacology

YOHIMBINE ADRA2C

Interaction Score: 0.55

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Specific Action of the Ligand Antagonist

Endogenous Drug? False

Direct Interaction? True

PMIDs:
12110610 11226402 12591093 12438517 10611634 16176444

Sources:
TdgClinicalTrial TEND GuideToPharmacology PharmGKB
BUCINDOLOL ADRA2C

Interaction Score: 0.51

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
23071495

Sources:
PharmGKB
CLONIDINE ADRA2C

Interaction Score: 0.46

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

PMIDs:
20833658 11082457

Sources:
TdgClinicalTrial ChemblInteractions GuideToPharmacology PharmGKB
DROXIDOPA ADRA2C

Interaction Score: 0.38

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Mechanism of Interaction Adrenergic receptor agonist

Direct Interaction yes

PMIDs:
18680204 8590979 21173850

Sources:
ChemblInteractions
LURASIDONE ADRA2C

Interaction Score: 0.38

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Trial Name lurasidone, SM-13496,Latuda

Novel drug target Established target

Specific Action of the Ligand Antagonist

PMIDs:
23545936

Sources:
TdgClinicalTrial GuideToPharmacology
APRACLONIDINE ADRA2C

Interaction Score: 0.38

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Direct Interaction? True

Endogenous Drug? False

Specific Action of the Ligand Agonist

PMIDs:
None found

Sources:
GuideToPharmacology
FADOLMIDINE ADRA2C

Interaction Score: 0.38

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
TTD
AMOSULALOL ADRA2C

Interaction Score: 0.38

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
TTD
TIZANIDINE ADRA2C

Interaction Score: 0.38

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
FENOLDOPAM ADRA2C

Interaction Score: 0.34

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

PMIDs:
17016423 17139284 7670737

Sources:
TEND
NOREPINEPHRINE ADRA2C

Interaction Score: 0.33

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
8590979 1980236 17410123 1654268 18064417 17016423 17139284

Sources:
TdgClinicalTrial TEND PharmGKB
TOLAZOLINE ADRA2C

Interaction Score: 0.31

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:
GuideToPharmacology
APRACLONIDINE HYDROCHLORIDE ADRA2C

Interaction Score: 0.26

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Mechanism of Interaction Adrenergic receptor alpha-2 agonist

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
MOXONIDINE ADRA2C

Interaction Score: 0.26

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
TTD
DEBRISOQUIN ADRA2C

Interaction Score: 0.26

Interaction Types & Directionality:

n/a

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
None found

Sources:
TdgClinicalTrial TEND
BRIMONIDINE TARTRATE ADRA2C

Interaction Score: 0.26

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 ADRA2C

Interaction Score: 0.26

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Mechanism of Interaction Adrenergic receptor alpha-2 agonist

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
CHEMBL362051 ADRA2C

Interaction Score: 0.26

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Specific Action of the Ligand Antagonist

Endogenous Drug? False

PMIDs:
None found

Sources:
GuideToPharmacology
METHYLDOPATE HYDROCHLORIDE ADRA2C

Interaction Score: 0.26

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Mechanism of Interaction Adrenergic receptor alpha-2 agonist

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
XYLAZINE ADRA2C

Interaction Score: 0.26

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Specific Action of the Ligand Partial agonist

Endogenous Drug? False

PMIDs:
None found

Sources:
GuideToPharmacology
RILMENIDINE ADRA2C

Interaction Score: 0.26

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
TTD
CLONIDINE HYDROCHLORIDE ADRA2C

Interaction Score: 0.26

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 ADRA2C

Interaction Score: 0.26

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Adrenergic receptor alpha-2 agonist

PMIDs:
None found

Sources:
ChemblInteractions
FIPAMEZOLE ADRA2C

Interaction Score: 0.26

Interaction Types & Directionality:

n/a

Interaction Info:

Trial Name fipamezole, JP-1730

Novel drug target Established target

PMIDs:
None found

Sources:
TdgClinicalTrial
DEXMEDETOMIDINE HYDROCHLORIDE ADRA2C

Interaction Score: 0.26

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Adrenergic receptor alpha-2 agonist

PMIDs:
None found

Sources:
ChemblInteractions
CABERGOLINE ADRA2C

Interaction Score: 0.2

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Endogenous Drug? False

Specific Action of the Ligand Antagonist

PMIDs:
12388667 18691132 10641988

Sources:
GuideToPharmacology
GUANABENZ ADRA2C

Interaction Score: 0.19

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Direct Interaction? True

Endogenous Drug? False

Specific Action of the Ligand Agonist

PMIDs:
None found

Sources:
GuideToPharmacology
GUANABENZ ACETATE ADRA2C

Interaction Score: 0.19

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Adrenergic receptor alpha-2 agonist

PMIDs:
None found

Sources:
ChemblInteractions
DIHYDROERGOCRISTINE ADRA2C

Interaction Score: 0.19

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
TTD
BETHANIDINE ADRA2C

Interaction Score: 0.19

Interaction Types & Directionality:

n/a

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
None found

Sources:
TdgClinicalTrial TEND
GUANFACINE HYDROCHLORIDE ADRA2C

Interaction Score: 0.19

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Mechanism of Interaction Adrenergic receptor alpha-2 agonist

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
MIRTAZAPINE ADRA2C

Interaction Score: 0.16

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

PMIDs:
3419539 15771415

Sources:
ChemblInteractions GuideToPharmacology
PERGOLIDE ADRA2C

Interaction Score: 0.15

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Specific Action of the Ligand Partial agonist

Endogenous Drug? False

PMIDs:
18691132 10641988

Sources:
GuideToPharmacology
CYCLOBENZAPRINE ADRA2C

Interaction Score: 0.15

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
TTD
RAUWOLFIA SERPENTINA ADRA2C

Interaction Score: 0.15

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Adrenergic receptor alpha antagonist

PMIDs:
None found

Sources:
ChemblInteractions
TETRAHYDROZOLINE HYDROCHLORIDE ADRA2C

Interaction Score: 0.13

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Mechanism of Interaction Adrenergic receptor alpha agonist

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
ESMIRTAZAPINE MALEATE ADRA2C

Interaction Score: 0.13

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Mechanism of Interaction Adrenergic receptor alpha-2 antagonist

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
ALSEROXYLON ADRA2C

Interaction Score: 0.13

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Mechanism of Interaction Adrenergic receptor alpha antagonist

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
MEDETOMIDINE ADRA2C

Interaction Score: 0.13

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
TTD
NAPHAZOLINE HYDROCHLORIDE ADRA2C

Interaction Score: 0.13

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Mechanism of Interaction Adrenergic receptor alpha agonist

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
OXYMETAZOLINE ADRA2C

Interaction Score: 0.13

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Direct Interaction? False

Endogenous Drug? False

Specific Action of the Ligand Partial agonist

PMIDs:
20030735

Sources:
GuideToPharmacology
SENREBOTASE ADRA2C

Interaction Score: 0.13

Interaction Types & Directionality:

n/a

Interaction Info:

Novel drug target Established target

Trial Name AGN-214868

PMIDs:
None found

Sources:
TdgClinicalTrial
GUANFACINE ADRA2C

Interaction Score: 0.11

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Specific Action of the Ligand Partial agonist

Endogenous Drug? False

Direct Interaction? True

PMIDs:
None found

Sources:
GuideToPharmacology
OXYMETAZOLINE HYDROCHLORIDE ADRA2C

Interaction Score: 0.11

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Mechanism of Interaction Adrenergic receptor alpha agonist

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
BROMOCRIPTINE ADRA2C

Interaction Score: 0.11

Interaction Types & Directionality:

agonist (activating)

antagonist (inhibitory)

Interaction Info:

Specific Action of the Ligand Antagonist

Endogenous Drug? False

PMIDs:
20138024 18691132 10641988

Sources:
GuideToPharmacology
RAUWOLSCINE ADRA2C

Interaction Score: 0.11

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Specific Action of the Ligand Antagonist

Endogenous Drug? False

PMIDs:
None found

Sources:
GuideToPharmacology
DIPIVEFRIN HYDROCHLORIDE ADRA2C

Interaction Score: 0.1

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Mechanism of Interaction Adrenergic receptor agonist

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
TOLAZOLINE HYDROCHLORIDE ADRA2C

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
PHENTOLAMINE MESYLATE ADRA2C

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
DEXMEDETOMIDINE ADRA2C

Interaction Score: 0.1

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
LISURIDE ADRA2C

Interaction Score: 0.1

Interaction Types & Directionality:

other/unknown

antagonist (inhibitory)

Interaction Info:

Specific Action of the Ligand Antagonist

Endogenous Drug? False

PMIDs:
18691132

Sources:
GuideToPharmacology
MEPHENTERMINE SULFATE ADRA2C

Interaction Score: 0.1

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Mechanism of Interaction Adrenergic receptor agonist

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
METHAMPHETAMINE ADRA2C

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:
TdgClinicalTrial
LABETALOL HYDROCHLORIDE ADRA2C

Interaction Score: 0.09

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Mechanism of Interaction Adrenergic receptor antagonist

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
PHENOXYBENZAMINE HYDROCHLORIDE ADRA2C

Interaction Score: 0.09

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Mechanism of Interaction Adrenergic receptor alpha antagonist

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
HYDROXYAMPHETAMINE HYDROBROMIDE ADRA2C

Interaction Score: 0.09

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Mechanism of Interaction Adrenergic receptor agonist

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
EPINEPHRINE ADRA2C

Interaction Score: 0.08

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Adrenergic receptor agonist

PMIDs:
1346768

Sources:
ChemblInteractions PharmGKB
SPIROXATRINE ADRA2C

Interaction Score: 0.08

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Direct Interaction? False

Endogenous Drug? False

Specific Action of the Ligand Antagonist

PMIDs:
None found

Sources:
GuideToPharmacology
ASENAPINE ADRA2C

Interaction Score: 0.08

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Trial Name Asenapine

Novel drug target Established target

PMIDs:
18308814

Sources:
TdgClinicalTrial
APOMORPHINE ADRA2C

Interaction Score: 0.07

Interaction Types & Directionality:

agonist (activating)

antagonist (inhibitory)

Interaction Info:

Endogenous Drug? False

Specific Action of the Ligand Antagonist

PMIDs:
18691132

Sources:
GuideToPharmacology
PIRIBEDIL ADRA2C

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
ERGOLOID MESYLATES ADRA2C

Interaction Score: 0.06

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Mechanism of Interaction Adrenergic receptor alpha antagonist

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
PRAZOSIN ADRA2C

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
LEVONORDEFRIN ADRA2C

Interaction Score: 0.06

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Mechanism of Interaction Adrenergic receptor alpha-2 agonist

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
PHENTOLAMINE ADRA2C

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
TERGURIDE ADRA2C

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
ROXINDOLE ADRA2C

Interaction Score: 0.05

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Endogenous Drug? False

Specific Action of the Ligand Antagonist

PMIDs:
None found

Sources:
GuideToPharmacology
NOREPINEPHRINE BITARTRATE ADRA2C

Interaction Score: 0.05

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Mechanism of Interaction Adrenergic receptor agonist

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
ILOPERIDONE ADRA2C

Interaction Score: 0.05

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Trial Name iloperidone,Fanapt, Fiapta, Zomaril

Novel drug target Established target

PMIDs:
None found

Sources:
TdgClinicalTrial
EPINEPHRINE BITARTRATE ADRA2C

Interaction Score: 0.05

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Mechanism of Interaction Adrenergic receptor agonist

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
DOPAMINE ADRA2C

Interaction Score: 0.03

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
PharmGKB
METHYLDOPA ADRA2C

Interaction Score: 0.03

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Mechanism of Interaction Adrenergic receptor alpha-2 agonist

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
ISOPROTERENOL ADRA2C

Interaction Score: 0.03

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
PharmGKB
CHLORPROMAZINE ADRA2C

Interaction Score: 0.02

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Endogenous Drug? False

Specific Action of the Ligand Antagonist

PMIDs:
None found

Sources:
GuideToPharmacology
OLANZAPINE ADRA2C

Interaction Score: 0.02

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)

PMIDs:
17848919

Sources:
TdgClinicalTrial

Ensembl: ENSG00000184160
- Version: 101_38
Alternate Names:

ADRA2C Ensembl Gene Name

Gene Info:

Gene Biotype PROTEIN_CODING

Publications:
TdgClinicalTrial: P18825
- Version: January-2014
Alternate Names:

ADRA2C Gene Symbol

Gene Info:

Target Class Receptors

Target Subclass GPCR

Target Subclass Rhodopsin

Publications:
TEND: P18825
- Version: 01-August-2011
Alternate Names:

ADRA2C Gene Symbol

ADA2C_HUMAN Uniprot Id

ENSG00000184160 Ensembl Gene Id

Gene Info:

Target Subclass Rhodopsin

Transmembrane Helix Count 7

Target Main Class Receptors

Publications:
HopkinsGroom: P18825
- Version: 11-September-2012
Alternate Names:

ALPHA-2C ADRENERGIC RECEPTOR Uniprot Protein Name

152 Entrez Gene Id

ADA2C_HUMAN Uniprot Id

Gene Info:

Human Readable Name G PROTEIN COUPLED RECEPTOR

Human Readable Name DRUGGABLE GENOME

Uniprot Evidence 2: Evidence at transcript level

Gene Categories:

G PROTEIN COUPLED RECEPTOR, DRUGGABLE GENOME

Publications:
GuideToPharmacology: 152
- Version: 29-September-2020
Alternate Names:

283 HUGO Gene ID

283 HUGO Gene Symbol

adrenoceptor alpha 2C HUGO Gene Name

Gene Info:

GuideToPharmacology Gene Category Name Adrenoceptors

GuideToPharmacology Gene Category ID 4

Gene Categories:

G PROTEIN COUPLED RECEPTOR

Publications:

PharmGKB: ADRA2C

Version: 18-August-2020

Alternate Names:

PA37 PharmGKB ID

Gene Info:

Publications:

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

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

HingoraniCasas: ENSG00000184160
- Version: 31-May-2017
Alternate Names:

ENSG00000184160 Gene Symbol

ADRA2C Ensembl Id

Gene Info:

Gene Categories:

DRUGGABLE GENOME

Publications:
ChemblInteractions: ADRA2L2
- Version: chembl_23
Alternate Names:

ADRA2RL2 GENE_SYMBOL

ADRA2C GENE_SYMBOL

Alpha-2C adrenergic receptor UNIPROT

Gene Info:

Publications:
dGene: ADRA2C
- Version: 27-Jun-2013
Alternate Names:

152 Gene ID

ADRA2L2 dGene Synonym

ADRA2RL2 dGene Synonym

Gene Info:

Gene Categories:

G PROTEIN COUPLED RECEPTOR

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

ADRA2C TTD Gene Abbreviation

T01777 TTD Target ID

Gene Info:

Publications:
GO: ADRA2C
- Version: 01-May-2021
Alternate Names:

ADRA2L2 GO Gene Synonym

ADRA2RL2 GO Gene Synonym

Gene Info:

Gene Categories:

G PROTEIN COUPLED RECEPTOR

Publications:

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

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.

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

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

Mechanism of Interaction	Adrenergic receptor agonist
Direct Interaction	yes

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

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

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

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

Direct Interaction	yes
Mechanism of Interaction	Adrenergic receptor alpha antagonist

Mechanism of Interaction	Adrenergic receptor alpha agonist
Direct Interaction	yes

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

Trial Name	low dose intravenous methamphetamine
Novel drug target	Established target

Mechanism of Interaction	Adrenergic receptor antagonist
Direct Interaction	yes

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

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

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

283	HUGO Gene ID
283	HUGO Gene Symbol
adrenoceptor alpha 2C	HUGO Gene Name

ADRA2C Gene Record

ADRA2C 152 Druggable Genome

Alternate Names:

Gene Info:

Gene Categories: Category Details

Publications:

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: None found

Sources: TTD

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: None found

Sources: TTD

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: None found

Sources: TTD

Interaction Types & Directionality: agonist (activating)

Interaction Info:

PMIDs: 20030735

Sources: TTD

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: None found

Sources: TTD

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: None found

Sources: TTD

Interaction Types & Directionality: agonist (activating)

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

PMIDs: 16757535 12670699 11606316 14610637

Sources: TEND GuideToPharmacology PharmGKB TTD

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.

PMIDs: None found

Sources: TdgClinicalTrial TEND GuideToPharmacology

Interaction Types & Directionality: antagonist (inhibitory)

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

PMIDs: 12110610 11226402 12591093 12438517 10611634 16176444

Sources: TdgClinicalTrial TEND GuideToPharmacology PharmGKB

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 23071495

Sources: PharmGKB

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

PMIDs: 20833658 11082457

Sources: TdgClinicalTrial ChemblInteractions GuideToPharmacology PharmGKB

Interaction Types & Directionality: agonist (activating)

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

PMIDs: 18680204 8590979 21173850

Sources: ChemblInteractions

Interaction Types & Directionality: antagonist (inhibitory)

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

PMIDs: 23545936

Sources: TdgClinicalTrial GuideToPharmacology

Interaction Types & Directionality: agonist (activating)

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

PMIDs: None found

Sources: GuideToPharmacology

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: None found

Sources: TTD

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: None found

Sources: TTD

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

Interaction Types & Directionality: antagonist (inhibitory)

Interaction Info:

PMIDs: 17016423 17139284 7670737

Sources: TEND

Interaction Types & Directionality: agonist (activating)

Interaction Info: Trial Name - Novel drug target Established target

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
TTD

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
TTD

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
TTD

Interaction Types & Directionality:

agonist (activating)

PMIDs:
20030735

Sources:
TTD

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
TTD

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
TTD

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Specific Action of the Ligand Partial agonist

Endogenous Drug? False

Direct Interaction? True

PMIDs:
16757535 12670699 11606316 14610637

Sources:
TEND GuideToPharmacology PharmGKB TTD

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.

PMIDs:
None found

Sources:
TdgClinicalTrial TEND GuideToPharmacology

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Specific Action of the Ligand Antagonist

Endogenous Drug? False

Direct Interaction? True

PMIDs:
12110610 11226402 12591093 12438517 10611634 16176444

Sources:
TdgClinicalTrial TEND GuideToPharmacology PharmGKB

Interaction Types & Directionality:

n/a

PMIDs:
23071495

Sources:
PharmGKB

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

PMIDs:
20833658 11082457

Sources:
TdgClinicalTrial ChemblInteractions GuideToPharmacology PharmGKB

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Mechanism of Interaction Adrenergic receptor agonist

Direct Interaction yes

PMIDs:
18680204 8590979 21173850

Sources:
ChemblInteractions

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Trial Name lurasidone, SM-13496,Latuda

Novel drug target Established target

Specific Action of the Ligand Antagonist

PMIDs:
23545936

Sources:
TdgClinicalTrial GuideToPharmacology

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Direct Interaction? True

Endogenous Drug? False

Specific Action of the Ligand Agonist

PMIDs:
None found

Sources:
GuideToPharmacology

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
TTD

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
TTD

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

Interaction Types & Directionality:

antagonist (inhibitory)

PMIDs:
17016423 17139284 7670737

Sources:
TEND

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
8590979 1980236 17410123 1654268 18064417 17016423 17139284

Sources:
TdgClinicalTrial TEND 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:
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:

n/a

PMIDs:
None found

Sources:
TTD

Interaction Types & Directionality:

n/a

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
None found

ADRA2RL2	GENE_SYMBOL
ADRA2C	GENE_SYMBOL
Alpha-2C adrenergic receptor	UNIPROT