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ADRA2C Gene Record

  • Summary
  • Interactions
  • Claims
  • 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
    &alpha;<sub>2C</sub>-adrenoceptor
    NP_000674
    BE0000342
    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
    (8 More Sources)

    Gene Categories: Category Details

    G PROTEIN COUPLED RECEPTOR
    DRUGGABLE GENOME

    Publications:

    Nasrallah, 2008, Atypical antipsychotic-induced metabolic side effects: insights from receptor-binding profiles., Mol. Psychiatry
    Kvernmo et al., 2008, Receptor-binding and pharmacokinetic properties of dopaminergic agonists., Curr Top Med Chem
    Lam, 2000, Clinical pharmacology of dopamine agonists., Pharmacotherapy
    Gilsbach et al., 2008, Presynaptic metabotropic receptors for acetylcholine and adrenaline/noradrenaline., Handb Exp Pharmacol
    Shreve et al., 1991, Alpha 2A- and alpha 2C-adrenoceptor subtypes are differentially down-regulated by norepinephrine., Eur. 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.
    Overington et al., 2006, How many drug targets are there?, Nat Rev Drug Discov
    Imming et al., 2006, Drugs, their targets and the nature and number of drug targets., Nat Rev Drug Discov
    Rump et al., 1995, Alpha 2C-adrenoceptor-modulated release of noradrenaline in human right atrium., Br. J. Pharmacol.
    Rizzo et al., 2001, Postjunctional alpha(2C)-adrenoceptor contractility in human saphenous vein., Eur. J. Pharmacol.
    Cleary et al., 2005, The alpha (1D)-adrenoceptor antagonist BMY 7378 is also an alpha (2C)-adrenoceptor antagonist., Auton Autacoid 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.
    Cleary et al., 2002, Investigation of neurotransmission in vas deferens from alpha(2A/D)-adrenoceptor knockout mice., 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
    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.
    Uys MM et al., 2017, Therapeutic Potential of Selectively Targeting the α<sub>2C</sub>-Adrenoceptor in Cognition, Depression, and Schizophrenia-New Developments and Future Perspective., Front Psychiatry
    Richelson et al., 2000, Binding of antipsychotic drugs to human brain receptors focus on newer generation compounds., Life Sci.
    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.
    Orito et al., 2001, alpha(2)-adrenoceptor antagonist properties of OPC-28326, a novel selective peripheral vasodilator., Br. J. Pharmacol.
    Zhang et al., 2003, The alpha2C-adrenoceptor modulates GABA release in mouse striatum., Brain Res. Mol. Brain Res.
    Trendelenburg et al., 2003, All three alpha2-adrenoceptor types serve as autoreceptors in postganglionic sympathetic neurons., Naunyn Schmiedebergs Arch. Pharmacol.
    Prinster et al., 2006, Alpha2C-adrenergic receptors exhibit enhanced surface expression and signaling upon association with beta2-adrenergic receptors., J. Pharmacol. Exp. Ther.
    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.
    Koshimizu et al., 2004, Carvedilol selectively inhibits oscillatory intracellular calcium changes evoked by human alpha1D- and alpha1B-adrenergic receptors., Cardiovasc. Res.
    Trendelenburg et al., 1997, Presynaptic alpha 2A/D-autoreceptors in the brain cortex of Cercopithecus aethiops., Naunyn Schmiedebergs Arch. Pharmacol.
    Corena-McLeod M, 2015, Comparative Pharmacology of Risperidone and Paliperidone., Drugs R D
    Fenton et al., 2005, Risperidone: a review of its use in the treatment of bipolar mania., CNS Drugs
    Fernández et al., 2005, Discovery of new tetracyclic tetrahydrofuran derivatives as potential broad-spectrum psychotropic agents., J. Med. Chem.
    de Boer et al., 1988, Neurochemical and autonomic pharmacological profiles of the 6-aza-analogue of mianserin, Org 3770 and its enantiomers., Neuropharmacology
    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
    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
    Dahl et al., 1986, Phenothiazine drugs and metabolites: molecular conformation and dopaminergic, alpha adrenergic and muscarinic cholinergic receptor binding., Biochem. Pharmacol.
    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
    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.
    Kobayashi et al., 2003, The sympathomimetic actions of l-ephedrine and d-pseudoephedrine: direct receptor activation or norepinephrine release?, Anesth. Analg.
    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.
    Davis, 2010, Recent advances in the treatment of pain., F1000 Med Rep
    Giovannoni et al., 2009, Alpha2-agonists as analgesic agents., Med Res Rev
    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
    Frang et al., 2001, Phenoxybenzamine binding reveals the helical orientation of the third transmembrane domain of adrenergic receptors., J. Biol. Chem.
    Oosterhof et al., 2014, Acute effects of brexpiprazole on serotonin, dopamine, and norepinephrine systems: an in vivo electrophysiologic characterization., J. Pharmacol. Exp. Ther.
    Li et al., 1994, Agmatine: an endogenous clonidine-displacing substance in the brain., Science
    Villamil-Hernández MT et al., 2013, Pharmacological identification of α1- and α2-adrenoceptor subtypes involved in the vasopressor responses induced by ergotamine in pithed rats., Eur J Pharmacol
    Mylecharane EJ, 1991, 5-HT2 receptor antagonists and migraine therapy., J Neurol
    Nawarskas JJ et al., 2017, Celiprolol: A Unique Selective Adrenoceptor Modulator., Cardiol Rev
    Kroeze et al., 2003, H1-histamine receptor affinity predicts short-term weight gain for typical and atypical antipsychotic drugs., Neuropsychopharmacology
  • TETRASUL   ADRA2C

    Interaction Score: 0.54

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    TTD

  • ORM-12741   ADRA2C

    Interaction Score: 0.54

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    TTD

  • BRIMONIDINE   ADRA2C

    Interaction Score: 0.54

    Interaction Types & Directionality:
    agonist (activating)

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

    PMIDs:
    11606316 12670699 14610637 16757535


    Sources:
    TEND PharmGKB TTD DrugBank GuideToPharmacology

  • TETRAHYDROZOLINE   ADRA2C

    Interaction Score: 0.54

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    TTD

  • AMEZINIUM   ADRA2C

    Interaction Score: 0.54

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    TTD

  • LURASIDONE   ADRA2C

    Interaction Score: 0.36

    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 DrugBank GuideToPharmacology

  • BUCINDOLOL   ADRA2C

    Interaction Score: 0.36

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    23071495


    Sources:
    PharmGKB

  • YOHIMBINE   ADRA2C

    Interaction Score: 0.31

    Interaction Types & Directionality:
    antagonist (inhibitory)

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

    PMIDs:
    11226402 16176444 12591093 12438517 12110610 10611634


    Sources:
    TEND PharmGKB TdgClinicalTrial DrugBank GuideToPharmacology

  • CLONIDINE   ADRA2C

    Interaction Score: 0.29

    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:
    PharmGKB TdgClinicalTrial DrugBank GuideToPharmacology ChemblInteractions

  • DROXIDOPA   ADRA2C

    Interaction Score: 0.27

    Interaction Types & Directionality:
    agonist (activating)

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

    PMIDs:
    21173850 18680204 8590979


    Sources:
    DrugBank ChemblInteractions

  • FADOLMIDINE   ADRA2C

    Interaction Score: 0.27

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    TTD

  • AMOSULALOL   ADRA2C

    Interaction Score: 0.27

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    TTD

  • TOLAZOLINE   ADRA2C

    Interaction Score: 0.23

    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

  • XYLOMETAZOLINE   ADRA2C

    Interaction Score: 0.23

    Interaction Types & Directionality:
    agonist (activating)

    Interaction Info:

    PMIDs:
    20030735


    Sources:
    TTD DrugBank

  • FENOLDOPAM   ADRA2C

    Interaction Score: 0.23

    Interaction Types & Directionality:
    antagonist (inhibitory)

    Interaction Info:

    PMIDs:
    7670737 17139284 17016423


    Sources:
    TEND DrugBank

  • NOREPINEPHRINE   ADRA2C

    Interaction Score: 0.22

    Interaction Types & Directionality:
    agonist (activating)

    Interaction Info:
    Trial Name -
    Novel drug target Established target

    PMIDs:
    18064417 1654268 1980236 17410123 17139284 17016423 8590979


    Sources:
    TEND PharmGKB TdgClinicalTrial DrugBank

  • APRACLONIDINE HYDROCHLORIDE   ADRA2C

    Interaction Score: 0.18

    Interaction Types & Directionality:
    agonist (activating)

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

    PMIDs:
    None found


    Sources:
    ChemblInteractions

  • BRIMONIDINE TARTRATE   ADRA2C

    Interaction Score: 0.18

    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: 0.18

    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: 0.18

    Interaction Types & Directionality:
    antagonist (inhibitory)

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

    PMIDs:
    None found


    Sources:
    GuideToPharmacology

  • PROPYLHEXEDRINE   ADRA2C

    Interaction Score: 0.18

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    TTD

  • METHYLDOPATE HYDROCHLORIDE   ADRA2C

    Interaction Score: 0.18

    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: 0.18

    Interaction Types & Directionality:
    agonist (activating)

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

    PMIDs:
    None found


    Sources:
    GuideToPharmacology

  • CLONIDINE HYDROCHLORIDE   ADRA2C

    Interaction Score: 0.18

    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: 0.18

    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: 0.18

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    Trial Name fipamezole, JP-1730
    Novel drug target Established target

    PMIDs:
    None found


    Sources:
    TdgClinicalTrial

  • LOFEXIDINE   ADRA2C

    Interaction Score: 0.18

    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:
    TEND TdgClinicalTrial GuideToPharmacology

  • TIZANIDINE   ADRA2C

    Interaction Score: 0.18

    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

  • DEXMEDETOMIDINE HYDROCHLORIDE   ADRA2C

    Interaction Score: 0.18

    Interaction Types & Directionality:
    agonist (activating)

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

    PMIDs:
    None found


    Sources:
    ChemblInteractions

  • EPHEDRA   ADRA2C

    Interaction Score: 0.17

    Interaction Types & Directionality:
    agonist (activating)

    Interaction Info:

    PMIDs:
    14570629 12954796 15955613


    Sources:
    DrugBank

  • CELIPROLOL   ADRA2C

    Interaction Score: 0.15

    Interaction Types & Directionality:
    antagonist (inhibitory)

    Interaction Info:

    PMIDs:
    28742547


    Sources:
    DrugBank

  • AGMATINE   ADRA2C

    Interaction Score: 0.15

    Interaction Types & Directionality:
    agonist (activating)

    Interaction Info:

    PMIDs:
    7906055


    Sources:
    DrugBank

  • BREXPIPRAZOLE   ADRA2C

    Interaction Score: 0.15

    Interaction Types & Directionality:
    antagonist (inhibitory)

    Interaction Info:

    PMIDs:
    25225185


    Sources:
    DrugBank

  • DEBRISOQUIN   ADRA2C

    Interaction Score: 0.15

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    Trial Name -
    Novel drug target Established target

    PMIDs:
    None found


    Sources:
    TEND TdgClinicalTrial

  • MOXONIDINE   ADRA2C

    Interaction Score: 0.14

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    TTD

  • GUANABENZ   ADRA2C

    Interaction Score: 0.14

    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: 0.14

    Interaction Types & Directionality:
    agonist (activating)

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

    PMIDs:
    None found


    Sources:
    ChemblInteractions

  • RILMENIDINE   ADRA2C

    Interaction Score: 0.14

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    TTD

  • GUANFACINE HYDROCHLORIDE   ADRA2C

    Interaction Score: 0.14

    Interaction Types & Directionality:
    agonist (activating)

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

    PMIDs:
    None found


    Sources:
    ChemblInteractions

  • APRACLONIDINE   ADRA2C

    Interaction Score: 0.14

    Interaction Types & Directionality:
    agonist (activating)

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

    PMIDs:
    None found


    Sources:
    GuideToPharmacology

  • CABERGOLINE   ADRA2C

    Interaction Score: 0.14

    Interaction Types & Directionality:
    antagonist (inhibitory)

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

    PMIDs:
    12388667 18691132 10641988


    Sources:
    DrugBank GuideToPharmacology

  • OXYMETAZOLINE   ADRA2C

    Interaction Score: 0.14

    Interaction Types & Directionality:
    agonist (activating)

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

    PMIDs:
    20030735


    Sources:
    DrugBank GuideToPharmacology

  • BETHANIDINE   ADRA2C

    Interaction Score: 0.12

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    Trial Name -
    Novel drug target Established target

    PMIDs:
    None found


    Sources:
    TEND TdgClinicalTrial

  • RAUWOLFIA SERPENTINA   ADRA2C

    Interaction Score: 0.11

    Interaction Types & Directionality:
    antagonist (inhibitory)

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

    PMIDs:
    None found


    Sources:
    ChemblInteractions

  • LEVOMEPROMAZINE   ADRA2C

    Interaction Score: 0.1

    Interaction Types & Directionality:
    antagonist (inhibitory)

    Interaction Info:

    PMIDs:
    2870716 6149771 15701205


    Sources:
    DrugBank

  • MIRTAZAPINE   ADRA2C

    Interaction Score: 0.1

    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:
    15771415 3419539


    Sources:
    GuideToPharmacology ChemblInteractions

  • 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:
    DrugBank GuideToPharmacology

  • TETRAHYDROZOLINE HYDROCHLORIDE   ADRA2C

    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

  • ESMIRTAZAPINE MALEATE   ADRA2C

    Interaction Score: 0.09

    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: 0.09

    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: 0.09

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    TTD

  • NAPHAZOLINE HYDROCHLORIDE   ADRA2C

    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

  • PERGOLIDE   ADRA2C

    Interaction Score: 0.09

    Interaction Types & Directionality:
    agonist (activating)

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

    PMIDs:
    18691132 10641988


    Sources:
    GuideToPharmacology

  • SENREBOTASE   ADRA2C

    Interaction Score: 0.09

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    Novel drug target Established target
    Trial Name AGN-214868

    PMIDs:
    None found


    Sources:
    TdgClinicalTrial

  • BROMOCRIPTINE   ADRA2C

    Interaction Score: 0.08

    Interaction Types & Directionality:
    agonist (activating)
    antagonist (inhibitory)

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

    PMIDs:
    18691132 10641988 20138024


    Sources:
    DrugBank GuideToPharmacology

  • METHAMPHETAMINE   ADRA2C

    Interaction Score: 0.08

    Interaction Types & Directionality:
    agonist (activating)

    Interaction Info:
    Trial Name low dose intravenous methamphetamine
    Novel drug target Established target

    PMIDs:
    9551769 15955613


    Sources:
    TdgClinicalTrial DrugBank

  • PHENOXYBENZAMINE   ADRA2C

    Interaction Score: 0.08

    Interaction Types & Directionality:
    antagonist (inhibitory)

    Interaction Info:

    PMIDs:
    11395517


    Sources:
    DrugBank

  • DIHYDROERGOCRISTINE   ADRA2C

    Interaction Score: 0.08

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    TTD

  • GUANFACINE   ADRA2C

    Interaction Score: 0.08

    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: 0.08

    Interaction Types & Directionality:
    agonist (activating)

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

    PMIDs:
    None found


    Sources:
    ChemblInteractions

  • RAUWOLSCINE   ADRA2C

    Interaction Score: 0.08

    Interaction Types & Directionality:
    antagonist (inhibitory)

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

    PMIDs:
    None found


    Sources:
    GuideToPharmacology

  • ASENAPINE   ADRA2C

    Interaction Score: 0.07

    Interaction Types & Directionality:
    antagonist (inhibitory)

    Interaction Info:
    Trial Name Asenapine
    Novel drug target Established target

    PMIDs:
    18308814


    Sources:
    TdgClinicalTrial DrugBank

  • PIZOTYLINE   ADRA2C

    Interaction Score: 0.07

    Interaction Types & Directionality:
    antagonist (inhibitory)

    Interaction Info:

    PMIDs:
    2045831


    Sources:
    DrugBank

  • DIPIVEFRIN HYDROCHLORIDE   ADRA2C

    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

  • TOLAZOLINE HYDROCHLORIDE   ADRA2C

    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

  • PHENTOLAMINE MESYLATE   ADRA2C

    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

  • DEXMEDETOMIDINE   ADRA2C

    Interaction Score: 0.07

    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   ADRA2C

    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

  • 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:
    DrugBank GuideToPharmacology

  • ILOPERIDONE   ADRA2C

    Interaction Score: 0.07

    Interaction Types & Directionality:
    antagonist (inhibitory)

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

    PMIDs:
    None found


    Sources:
    TdgClinicalTrial DrugBank

  • ERGOTAMINE   ADRA2C

    Interaction Score: 0.06

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    23707349


    Sources:
    DrugBank

  • LABETALOL HYDROCHLORIDE   ADRA2C

    Interaction Score: 0.06

    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: 0.06

    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: 0.06

    Interaction Types & Directionality:
    agonist (activating)

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

    PMIDs:
    None found


    Sources:
    ChemblInteractions

  • DRONEDARONE   ADRA2C

    Interaction Score: 0.06

    Interaction Types & Directionality:
    antagonist (inhibitory)

    Interaction Info:

    PMIDs:
    17389667 23997577


    Sources:
    DrugBank

  • SPIROXATRINE   ADRA2C

    Interaction Score: 0.05

    Interaction Types & Directionality:
    antagonist (inhibitory)

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

    PMIDs:
    None found


    Sources:
    GuideToPharmacology

  • EPINEPHRINE   ADRA2C

    Interaction Score: 0.05

    Interaction Types & Directionality:
    agonist (activating)

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

    PMIDs:
    1346768


    Sources:
    PharmGKB ChemblInteractions

  • PALIPERIDONE   ADRA2C

    Interaction Score: 0.05

    Interaction Types & Directionality:
    agonist (activating)

    Interaction Info:

    PMIDs:
    11132243


    Sources:
    DrugBank

  • QUETIAPINE   ADRA2C

    Interaction Score: 0.05

    Interaction Types & Directionality:
    antagonist (inhibitory)

    Interaction Info:

    PMIDs:
    28855875 17848919 11132243


    Sources:
    DrugBank

  • CHEMBL609728   ADRA2C

    Interaction Score: 0.05

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    DrugBank

  • RACEPINEPHRINE   ADRA2C

    Interaction Score: 0.05

    Interaction Types & Directionality:
    agonist (activating)

    Interaction Info:

    PMIDs:
    None found


    Sources:
    DrugBank

  • PIRIBEDIL   ADRA2C

    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

  • ERGOLOID MESYLATES   ADRA2C

    Interaction Score: 0.05

    Interaction Types & Directionality:
    antagonist (inhibitory)

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

    PMIDs:
    None found


    Sources:
    ChemblInteractions

  • LEVONORDEFRIN   ADRA2C

    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

  • CYCLOBENZAPRINE   ADRA2C

    Interaction Score: 0.04

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    TTD

  • PRAZOSIN   ADRA2C

    Interaction Score: 0.04

    Interaction Types & Directionality:
    antagonist (inhibitory)

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

    PMIDs:
    None found


    Sources:
    GuideToPharmacology

  • PHENTOLAMINE   ADRA2C

    Interaction Score: 0.04

    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: 0.04

    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: 0.04

    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: 0.04

    Interaction Types & Directionality:
    agonist (activating)

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

    PMIDs:
    None found


    Sources:
    ChemblInteractions

  • OCAPERIDONE   ADRA2C

    Interaction Score: 0.04

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    DrugBank

  • ARIPIPRAZOLE   ADRA2C

    Interaction Score: 0.03

    Interaction Types & Directionality:
    other/unknown
    antagonist (inhibitory)

    Interaction Info:

    PMIDs:
    17848919 26346901


    Sources:
    DrugBank

  • EPINEPHRINE BITARTRATE   ADRA2C

    Interaction Score: 0.03

    Interaction Types & Directionality:
    agonist (activating)

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

    PMIDs:
    None found


    Sources:
    ChemblInteractions

  • CARVEDILOL   ADRA2C

    Interaction Score: 0.03

    Interaction Types & Directionality:
    antagonist (inhibitory)

    Interaction Info:

    PMIDs:
    15306222


    Sources:
    DrugBank

  • RISPERIDONE   ADRA2C

    Interaction Score: 0.03

    Interaction Types & Directionality:
    agonist (activating)
    antagonist (inhibitory)

    Interaction Info:

    PMIDs:
    11132243 25943458 15907153


    Sources:
    DrugBank

  • ZIPRASIDONE   ADRA2C

    Interaction Score: 0.03

    Interaction Types & Directionality:
    antagonist (inhibitory)

    Interaction Info:

    PMIDs:
    17848919


    Sources:
    DrugBank

  • MIANSERIN   ADRA2C

    Interaction Score: 0.02

    Interaction Types & Directionality:
    antagonist (inhibitory)

    Interaction Info:

    PMIDs:
    None found


    Sources:
    DrugBank

  • DOPAMINE   ADRA2C

    Interaction Score: 0.02

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    PharmGKB

  • LOXAPINE   ADRA2C

    Interaction Score: 0.02

    Interaction Types & Directionality:
    binder

    Interaction Info:

    PMIDs:
    None found


    Sources:
    DrugBank

  • ISOPROTERENOL   ADRA2C

    Interaction Score: 0.02

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    PharmGKB

  • 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

  • HALOPERIDOL   ADRA2C

    Interaction Score: 0.01

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    12629531


    Sources:
    DrugBank

  • CLOZAPINE   ADRA2C

    Interaction Score: 0.01

    Interaction Types & Directionality:
    antagonist (inhibitory)

    Interaction Info:

    PMIDs:
    17848919


    Sources:
    DrugBank

  • CHLORPROMAZINE   ADRA2C

    Interaction Score: 0.01

    Interaction Types & Directionality:
    antagonist (inhibitory)

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

    PMIDs:
    None found


    Sources:
    GuideToPharmacology

  • METHYLDOPA   ADRA2C

    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: 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

  • DrugBank: BE0000342

    • Version: 5.1.7

    Alternate Names:
    ADRA2C DrugBank Gene Name
    P18825 UniProt Accession
    152 Entrez Gene Id

    Gene Info:

    Publications:
    Gilsbach et al., 2008, Presynaptic metabotropic receptors for acetylcholine and adrenaline/noradrenaline., Handb Exp Pharmacol
    Shreve et al., 1991, Alpha 2A- and alpha 2C-adrenoceptor subtypes are differentially down-regulated by norepinephrine., Eur. J. Pharmacol.
    Nash, 1990, Alpha-adrenergic blockers: mechanism of action, blood pressure control, and effects of lipoprotein metabolism., Clin Cardiol

  • 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:

  • GO: ADRA2C

    • Version: 05-September-2020

    Alternate Names:
    ADRA2L2 GO Gene Synonym
    ADRA2RL2 GO Gene Synonym

    Gene Info:

    Gene Categories:
    G PROTEIN COUPLED RECEPTOR

    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:

Disclaimer: This resource is intended for purely research purposes. It should not be used for emergencies or medical or professional advice.

A finding of a drug-gene interaction or potentially druggable category does not necessarily indicate effectiveness (or lack thereof) of any drug or treatment regimen. A finding of no interaction or no potentially druggable category does not necessarily indicate lack of effectiveness of any drug or treatment regimen. Drug-gene interactions or potentially druggable categories are not presented in ranked order of potential or predicted efficacy.

The dgidb.org website does not provide any medical or healthcare products, services or advice, and is not for medical emergencies or urgent situations. IF YOU THINK YOU MAY HAVE A MEDICAL EMERGENCY, CALL YOUR DOCTOR OR 911 IMMEDIATELY. Information contained on this website is not a substitute for a doctor's medical judgment or advice. We recommend that you discuss your specific, individual health concerns with your doctor or health care professional.

DGIdb (v4.2.0 - sha1 afd9f30b) • Last updated 2020-10-21