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ADRA2A Gene Record

  • Summary
  • Interactions
  • Claims
  • ADRA2A 150 Druggable Genome

    Alternate Names:

    150
    ADRENOCEPTOR ALPHA 2A
    ADRA2A
    ADRA2
    ADRA2R
    ADRAR
    ALPHA2AAR
    ZNF32
    104210
    281
    ENSG00000150594
    OTTHUMG00000019050
    P08913
    ADA2A_HUMAN
    PA35
    ALPHA-2A ADRENERGIC RECEPTOR
    Alpha-2AAR
    Alpha-2A adrenoceptor
    Alpha-2A adrenoreceptor
    Alpha-2 adrenergic receptor subtype C10
    ALPHA-2A ADRENERGIC RECEPTOR (ALPHA-2A ADRENOCEPTOR) (ALPHA-2A ADRENORECEPTOR) (ALPHA-2AAR SUBTYPE C10). [SOURCE:UNIPROT/SWISSPROT;ACC:P08913]
    Adrenergic receptor Alpha-2
    T31424
    Adrenergic receptor alpha-2A
    T11448

    Gene Info:

    Target Class Receptors
    Target Subclass GPCR
    Target Subclass Rhodopsin
    Transmembrane Helix Count 7
    Target Main Class Receptors
    Uniprot Evidence 1: Evidence at protein level
    Human Readable Name DRUGGABLE GENOME
    Human Readable Name G PROTEIN COUPLED RECEPTOR
    Interpro Short Name 7TM_GPCR_Rhodpsn
    Interpro Type Family
    Interpro Acc IPR000276
    Interpro Name GPCR, rhodopsin-like, 7TM
    Uniprot Status Swiss-Prot
    Gene Biotype PROTEIN_CODING
    (9 More Sources)

    Gene Categories: Category Details

    G PROTEIN COUPLED RECEPTOR
    DRUGGABLE GENOME

    Publications:

    Erb et al., 2000, Alpha-2 adrenergic receptor agonists block stress-induced reinstatement of cocaine seeking., Neuropsychopharmacology
    Strang et al., 1999, Lofexidine for opiate detoxification: review of recent randomised and open controlled trials., Am J Addict
    Jin et al., 1992, Effects of lofexidine, an alpha 2-adrenoreceptor agonist, on ocular blood flow and ion transport of rabbit iris-ciliary body., J Ocul Pharmacol
    Scheibner et al., 2002, Alpha 2-adrenoceptors in the enteric nervous system: a study in alpha 2A-adrenoceptor-deficient mice., Br. J. Pharmacol.
    Dawson et al., 2004, Dexmedetomidine enhances analgesic action of nitrous oxide: mechanisms of action., Anesthesiology
    Ozdogan et al., 2004, The involvement of alpha 2A-adrenoceptors in morphine analgesia, tolerance and withdrawal in mice., Eur. J. Pharmacol.
    Fairbanks et al., 2002, alpha(2C)-Adrenergic receptors mediate spinal analgesia and adrenergic-opioid synergy., J. Pharmacol. Exp. Ther.
    Davies et al., 2004, Activation of alpha2 adrenergic receptors suppresses fear conditioning: expression of c-Fos and phosphorylated CREB in mouse amygdala., Neuropsychopharmacology
    Menon et al., 2007, Central sympatholysis as a novel countermeasure for cocaine-induced sympathetic activation and vasoconstriction in humans., J. Am. Coll. Cardiol.
    Yağar S et al., 2011, The role of the ADRA2A C1291G genetic polymorphism in response to dexmedetomidine on patients undergoing coronary artery surgery., Mol Biol Rep
    Vilardaga JP et al., 2005, Molecular basis of inverse agonism in a G protein-coupled receptor., Nat Chem Biol
    Lavand'homme et al., 2002, Perineural alpha(2A)-adrenoceptor activation inhibits spinal cord neuroplasticity and tactile allodynia after nerve injury., Anesthesiology
    Wang et al., 2002, Effect of antisense knock-down of alpha(2a)- and alpha(2c)-adrenoceptors on the antinociceptive action of clonidine on trigeminal nociception in the rat., Pain
    Ozdoğan et al., 2004, Loss of amitriptyline analgesia in alpha 2A-adrenoceptor deficient mice., Eur. J. Pharmacol.
    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
    Bockman et al., 1993, Binding and functional characterization of alpha-2 adrenergic receptor subtypes on pig vascular endothelium., J. Pharmacol. Exp. Ther.
    Bockman et al., 1996, Alpha-2 adrenoceptor subtype causing nitric oxide-mediated vascular relaxation in rats., J. Pharmacol. Exp. Ther.
    Galeotti et al., 2004, Alpha-2 agonist-induced memory impairment is mediated by the alpha-2A-adrenoceptor subtype., Behav. Brain Res.
    van Zwieten, 1997, Centrally acting antihypertensives: a renaissance of interest. Mechanisms and haemodynamics., J Hypertens Suppl
    Piletz et al., 1993, Nonadrenergic imidazoline binding sites on human platelets., J. Pharmacol. Exp. Ther.
    Ivgy-May et al., 2015, Esmirtazapine in non-elderly adult patients with primary insomnia: efficacy and safety from a randomized, 6-week sleep laboratory trial., Sleep Med.
    Dekeyne et al., 2006, Discriminative stimulus properties of the selective and highly potent alpha2-adrenoceptor agonist, S18616, in rats: mediation by the alpha2A subtype, and blockade by the atypical antidepressants, mirtazapine and mianserin., Neuropharmacology
    Liljedahl U et al., 2004, Single nucleotide polymorphisms predict the change in left ventricular mass in response to antihypertensive treatment., J Hypertens
    Sueke et al., 2010, Using apraclonidine in diagnosing Horner syndrome in children., Am. J. Ophthalmol.
    Mirzai et al., 2006, Congenital Horner's syndrome and the usefulness of the apraclonidine test in its diagnosis., Indian J Ophthalmol
    Moodley et al., 2007, Apraclonidine in the diagnosis of Horner's syndrome., S. Afr. Med. J.
    Chen et al., 2006, Efficacy of apraclonidine 0.5% in the diagnosis of Horner syndrome in pediatric patients under low or high illumination., Am. J. Ophthalmol.
    Wikberg-Matsson et al., 2001, Potent alpha(2A)-adrenoceptor-mediated vasoconstriction by brimonidine in porcine ciliary arteries., Invest. Ophthalmol. Vis. Sci.
    Costa et al., 2003, The effects of antiglaucoma and systemic medications on ocular blood flow., Prog Retin Eye Res
    Scheinfeld, 2005, The use of apraclonidine eyedrops to treat ptosis after the administration of botulinum toxin to the upper face., Dermatol. Online J.
    Watts et al., 2007, Adverse effects of apraclonidine used in the diagnosis of Horner syndrome in infants., J AAPOS
    2003, New topical drugs for open-angle glaucoma., Drug Ther Bull
    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.
    Fairbanks CA et al., 2009, Pharmacological profiles of alpha 2 adrenergic receptor agonists identified using genetically altered mice and isobolographic analysis., Pharmacol Ther
    Giovannitti JA Jr et al., 2015, Alpha-2 adrenergic receptor agonists: a review of current clinical applications., Anesth Prog
    Leiphart JW et al., 2004, Alpha2-adrenergic receptor subtype specificity of intrathecally administered tizanidine used for analgesia for neuropathic pain., J Neurosurg
    Spencer RC et al., 2015, The cognition-enhancing effects of psychostimulants involve direct action in the prefrontal cortex., Biol Psychiatry
    Trendelenburg et al., 2003, Crosstalk between presynaptic angiotensin receptors, bradykinin receptors and alpha 2-autoreceptors in sympathetic neurons: a study in alpha 2-adrenoceptor-deficient mice., Br. J. Pharmacol.
    Bylund, 1992, Subtypes of alpha 1- and alpha 2-adrenergic receptors., FASEB J.
    Polak et al., 2005, Dynamic strength training improves insulin sensitivity and functional balance between adrenergic alpha 2A and beta pathways in subcutaneous adipose tissue of obese subjects., Diabetologia
    Giussani et al., 1995, Alpha 1- and alpha 2-adrenoreceptor actions of phentolamine and prazosin on breathing movements in fetal sheep in utero., J. Physiol. (Lond.)
    Blandizzi et al., 2003, Altered prejunctional modulation of intestinal cholinergic and noradrenergic pathways by alpha2-adrenoceptors in the presence of experimental colitis., Br. J. Pharmacol.
    Vonend et al., 2007, Alpha(2A)-adrenoceptors regulate sympathetic transmitter release in mice kidneys., Br. J. Pharmacol.
    Molderings et al., 2000, Species-specific pharmacological properties of human alpha(2A)-adrenoceptors., Hypertension
    Saeed et al., Alpha-adrenoceptor blockade by phentolamine causes beta-adrenergic vasodilation by increased catecholamine release due to presynaptic alpha-blockade., J. Cardiovasc. Pharmacol.
    Leprêtre et al., 1994, Alpha 2-adrenoceptors activate dihydropyridine-sensitive calcium channels via Gi-proteins and protein kinase C in rat portal vein myocytes., Pflugers Arch.
    MacKinnon et al., 1992, [3H]-RS-15385-197, a selective and high affinity radioligand for alpha 2-adrenoceptors: implications for receptor classification., Br. J. Pharmacol.
    Mitrani et al., 2007, Role of the autonomic nervous system in the development of hyperinsulinemia by high-carbohydrate formula feeding to neonatal rats., Am. J. Physiol. Endocrinol. Metab.
    Kawasaki, 1997, [Centrally acting sympathetic inhibitors for therapy of patients with hypertension]., Nippon Rinsho
    van Zwieten, New central mediators as targets of centrally acting antihypertensive drugs., Clin. Exp. Hypertens.
    Head, 1999, Central imidazoline- and alpha 2-receptors involved in the cardiovascular actions of centrally acting antihypertensive agents., Ann. N. Y. Acad. Sci.
    van Zwieten, 1992, Development and trends in the drug treatment of essential hypertension., J Hypertens Suppl
    Sica, 2007, Centrally acting antihypertensive agents: an update., J Clin Hypertens (Greenwich)
    Velliquette et al., 2003, Contrasting metabolic effects of antihypertensive agents., J. Pharmacol. Exp. Ther.
    Jeng et al., 1998, Methamphetamine modulates GABA-induced electrophysiological depression by alternating noradrenergic actions in cerebellar Purkinje neurons., Psychopharmacology (Berl.)
    Nishio et al., 2002, Methamphetamine increases the hippocampal alpha(2A)-adrenergic receptor and Galpha(o) in mice., Neurosci. Lett.
    Sulzer et al., 2005, Mechanisms of neurotransmitter release by amphetamines: a review., Prog. Neurobiol.
    Zádori et al., 2007, Pre- and postsynaptic mechanisms in the clonidine- and oxymetazoline-induced inhibition of gastric motility in the rat., Neurochem. Int.
    Laurila et al., 2007, The second extracellular loop of alpha2A-adrenoceptors contributes to the binding of yohimbine analogues., Br. J. Pharmacol.
    Ozdoğan et al., 2006, The analgesic efficacy of partial opioid agonists is increased in mice with targeted inactivation of the alpha2A-adrenoceptor gene., Eur. J. Pharmacol.
    Kalkman et al., 2003, alpha2C-Adrenoceptor blockade by clozapine and other antipsychotic drugs., Eur. J. Pharmacol.
    Paul et al., 1999, Molecular mechanism of thromboxane A(2)-induced platelet aggregation. Essential role for p2t(ac) and alpha(2a) receptors., J. Biol. Chem.
    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
    Johnson DA et al., 1993, The pharmacology of alpha-adrenergic decongestants., Pharmacotherapy
    Nash, 1990, Alpha-adrenergic blockers: mechanism of action, blood pressure control, and effects of lipoprotein metabolism., Clin Cardiol
    Hieble et al., 1998, Molecular basis for the stereoselective interactions of catecholamines with alpha-adrenoceptors., Proc. West. Pharmacol. Soc.
    Giovannoni et al., 2009, Alpha2-agonists as analgesic agents., Med Res Rev
    Nyrönen et al., 2001, Molecular mechanism for agonist-promoted alpha(2A)-adrenoceptor activation by norepinephrine and epinephrine., Mol. Pharmacol.
    MacLennan et al., 2000, Characterization of human recombinant alpha(2A)-adrenoceptors expressed in Chinese hamster lung cells using extracellular acidification rate changes., Br. J. Pharmacol.
    Gilsbach et al., 2008, Presynaptic metabotropic receptors for acetylcholine and adrenaline/noradrenaline., Handb Exp Pharmacol
    Rauly et al., 2000, alpha(2A)-adrenoceptor: G(alphai1) protein-mediated pertussis toxin-resistant attenuation of G(s) coupling to the cyclic AMP pathway., Biochem. Pharmacol.
    Meana et al., 1992, Decreased density of presynaptic alpha 2-adrenoceptors in postmortem brains of patients with Alzheimer's disease., J. Neurochem.
    Chen et al., 2002, TTD: Therapeutic Target Database., Nucleic Acids Res.
    Davis, 2010, Recent advances in the treatment of pain., F1000 Med Rep
    Anttila et al., 2001, A review of the pharmacological and clinical profile of mirtazapine., CNS Drug Rev
    Rogoz et al., 2002, Effect of repeated treatment with mirtazapine on the central alpha1-adrenergic receptors., J. Physiol. Pharmacol.
    Besson et al., 2000, Effects of the co-administration of mirtazapine and paroxetine on serotonergic neurotransmission in the rat brain., Eur Neuropsychopharmacol
    Rogóz et al., Effect of repeated treatment with mirtazapine on the central dopaminergic D2/D3 receptors., Pol J Pharmacol
    Schreiber et al., Venlafaxine and mirtazapine: different mechanisms of antidepressant action, common opioid-mediated antinociceptive effects--a possible opioid involvement in severe depression?, J. Mol. Neurosci.
    García-Sevilla et al., 2004, Regulation of platelet alpha 2A-adrenoceptors, Gi proteins and receptor kinases in major depression: effects of mirtazapine treatment., Neuropsychopharmacology
    Haddjeri N et al., 1997, Effects of long-term treatment with the alpha 2-adrenoceptor antagonist mirtazapine on 5-HT neurotransmission., Naunyn Schmiedebergs Arch Pharmacol
    Lee HY et al., 2009, Association of the adrenergic alpha 2a receptor--1291C/G polymorphism with weight change and treatment response to mirtazapine in patients with major depressive disorder., Brain Res
    de Boer, 1995, The effects of mirtazapine on central noradrenergic and serotonergic neurotransmission., Int Clin Psychopharmacol
    de Andrade et al., 2009, Involvement of central alpha1-adrenoceptors on renal responses to central moxonidine and alpha-methylnoradrenaline., Eur. J. Pharmacol.
    Avery et al., 2000, The alpha-2A-adrenoceptor agonist, guanfacine, increases regional cerebral blood flow in dorsolateral prefrontal cortex of monkeys performing a spatial working memory task., Neuropsychopharmacology
    Sagvolden, 2006, The alpha-2A adrenoceptor agonist guanfacine improves sustained attention and reduces overactivity and impulsiveness in an animal model of Attention-Deficit/Hyperactivity Disorder (ADHD)., Behav Brain Funct
    Birnbaum et al., 2000, Noradrenergic alpha-2 receptor agonists reverse working memory deficits induced by the anxiogenic drug, FG7142, in rats., Pharmacol. Biochem. Behav.
    Stahl, 2010, Mechanism of action of alpha 2A-adrenergic agonists in attention-deficit/hyperactivity disorder with or without oppositional symptoms., J Clin Psychiatry
    Yuan et al., 2005, G-protein-coupled alpha2A-adrenoreceptor agonists differentially alter citrus leaf and fruit abscission by affecting expression of ACC synthase and ACC oxidase., J. Exp. Bot.
    Millan, 1992, Evidence that an alpha 2A-adrenoceptor subtype mediates antinociception in mice., Eur. J. Pharmacol.
    Nasrallah, 2008, Atypical antipsychotic-induced metabolic side effects: insights from receptor-binding profiles., Mol. Psychiatry
    Cusack et al., 1994, Binding of antidepressants to human brain receptors: focus on newer generation compounds., Psychopharmacology (Berl.)
    Marek et al., 1992, A comparison of trazodone and fluoxetine: implications for a serotonergic mechanism of antidepressant action., Psychopharmacology (Berl.)
    Price LH et al., 1986, Effects of trazodone treatment on alpha-2 adrenoceptor function in depressed patients., Psychopharmacology (Berl)
    Arthur S et al., 2011, Update on the role of alpha-agonists in glaucoma management., Exp Eye Res
    Flavahan, 2005, Phenylpropanolamine constricts mouse and human blood vessels by preferentially activating alpha2-adrenoceptors., J. Pharmacol. Exp. Ther.
    Ariëns EJ et al., 1983, Physiological and pharmacological aspects of adrenergic receptor classification., Biochem Pharmacol
    Noshiro et al., 1989, Functional relationship between platelet alpha 2-adrenoceptors and sympathetic nerve activity in man., Clin Exp Hypertens A
    Noshiro et al., 1990, Functional relationships between platelet alpha 2-adrenoceptors and sympathetic nerve activity in clinical hypertensive states., J. Hypertens.
    Martin et al., 1995, Renal vasodilatation by dopexamine and fenoldopam due to alpha 1-adrenoceptor blockade., Br. J. Pharmacol.
    Stone LS et al., 2003, Moxonidine, a mixed alpha(2)-adrenergic and imidazoline receptor agonist, identifies a novel adrenergic target for spinal analgesia., Ann N Y Acad Sci
    Buccafusco JJ et al., 1995, Role of medullary I1-imidazoline and alpha 2-adrenergic receptors in the antihypertensive responses evoked by central administration of clonidine analogs in conscious spontaneously hypertensive rats., J Pharmacol Exp Ther
    Zhu QM et al., 1999, Cardiovascular effects of rilmenidine, moxonidine and clonidine in conscious wild-type and D79N alpha2A-adrenoceptor transgenic mice., Br J Pharmacol
    Shahid et al., 2009, Asenapine: a novel psychopharmacologic agent with a unique human receptor signature., J. Psychopharmacol. (Oxford)
  • APRACLONIDINE   ADRA2A

    Interaction Score: 12.19

    Interaction Types & Directionality:
    agonist (activating)

    Interaction Info:
    Novel drug target Established target
    Trial Name -

    PMIDs:
    20399934 16921219 17824139 16935593 11481271 14575724 15748550 17572343 12630335 17016423 17139284


    Sources:
    TdgClinicalTrial TEND TTD

  • GUANABENZ   ADRA2A

    Interaction Score: 3.48

    Interaction Types & Directionality:
    agonist (activating)

    Interaction Info:
    Trial Name -
    Novel drug target Established target

    PMIDs:
    7903385 8819507 15265636 9050980 8263811


    Sources:
    TdgClinicalTrial TEND TTD

  • PHENYLPROPANOLAMINE   ADRA2A

    Interaction Score: 2.18

    Interaction Types & Directionality:
    agonist (activating)

    Interaction Info:
    Trial Name -
    Novel drug target Established target

    PMIDs:
    15608085 17016423 17139284


    Sources:
    TdgClinicalTrial TEND

  • DIPIVEFRIN   ADRA2A

    Interaction Score: 2.18

    Interaction Types & Directionality:
    agonist (activating)

    Interaction Info:
    Trial Name -
    Novel drug target Established target

    PMIDs:
    17016423 17139284 21524649


    Sources:
    TdgClinicalTrial TEND

  • CHEMBL1257057   ADRA2A

    Interaction Score: 1.74

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    16407989


    Sources:
    DTC

  • CHEMBL10332   ADRA2A

    Interaction Score: 1.74

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    16407989


    Sources:
    DTC

  • MOXONIDINE   ADRA2A

    Interaction Score: 1.74

    Interaction Types & Directionality:
    agonist (activating)

    Interaction Info:

    PMIDs:
    16407989 15028616 7791087 10217548


    Sources:
    DTC TTD

  • RAUWOLSCINE   ADRA2A

    Interaction Score: 1.74

    Interaction Types & Directionality:
    antagonist (inhibitory)

    Interaction Info:

    PMIDs:
    16407989


    Sources:
    DTC

  • YOHIMBINE   ADRA2A

    Interaction Score: 1.74

    Interaction Types & Directionality:
    antagonist (inhibitory)

    Interaction Info:
    Trial Name -
    Novel drug target Established target

    PMIDs:
    17664022 17558432 16325800 12591093 10506165 10611634 16407989


    Sources:
    DTC TdgClinicalTrial TEND PharmGKB TTD

  • DEXMEDETOMIDINE   ADRA2A

    Interaction Score: 1.6

    Interaction Types & Directionality:
    agonist (activating)

    Interaction Info:
    Trial Name -
    Novel drug target Established target

    PMIDs:
    11834617 15087625 15306201 11752127 14583739 17692748 21104443


    Sources:
    TdgClinicalTrial TEND PharmGKB TTD

  • TIZANIDINE   ADRA2A

    Interaction Score: 1.52

    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 19393691 25849473 15481719


    Sources:
    TdgClinicalTrial TEND TTD

  • BENZPHETAMINE   ADRA2A

    Interaction Score: 1.45

    Interaction Types & Directionality:
    agonist (activating)

    Interaction Info:
    Trial Name -
    Novel drug target Established target

    PMIDs:
    17016423 17139284 25499957


    Sources:
    TdgClinicalTrial TEND

  • GUANFACINE   ADRA2A

    Interaction Score: 1.39

    Interaction Types & Directionality:
    agonist (activating)

    Interaction Info:
    Trial Name guanfacine, SPD 503,Intuniv
    Novel drug target Established target

    PMIDs:
    10942848 17173664 11164065 20331927 15928018 1356794


    Sources:
    TdgClinicalTrial TEND

  • OXYMETAZOLINE   ADRA2A

    Interaction Score: 1.39

    Interaction Types & Directionality:
    partial agonist (activating)
    agonist (activating)

    Interaction Info:
    Trial Name OMS-103HP
    Novel drug target Established target

    PMIDs:
    16407989 7892112 1327384 17164433


    Sources:
    DTC TdgClinicalTrial TEND TTD

  • LOFEXIDINE   ADRA2A

    Interaction Score: 1.31

    Interaction Types & Directionality:
    agonist (activating)

    Interaction Info:
    Trial Name lofexidine,BritLofex
    Novel drug target Established target

    PMIDs:
    10882840 10598217 1357064


    Sources:
    TdgClinicalTrial TEND TTD

  • CLONIDINE   ADRA2A

    Interaction Score: 1.26

    Interaction Types & Directionality:
    agonist (activating)

    Interaction Info:
    Mechanism of Interaction Adrenergic receptor alpha-2 agonist
    Direct Interaction yes
    Trial Name ARC-4558, 0.1% clonidine hycrochloride gel

    PMIDs:
    16407989 12357167 12098614 15306201 11752127 14757140 11082457


    Sources:
    DTC TdgClinicalTrial ChemblInteractions TEND PharmGKB TTD

  • PHENTOLAMINE   ADRA2A

    Interaction Score: 1.16

    Interaction Types & Directionality:
    antagonist (inhibitory)

    Interaction Info:
    Trial Name aviptadil,Invicorp
    Novel drug target Established target
    Trial Name -

    PMIDs:
    16407989 12721093 1346768 16273345 7562640 12770936 17115069 10988273 6176798


    Sources:
    DTC TdgClinicalTrial TEND

  • BRIMONIDINE   ADRA2A

    Interaction Score: 0.97

    Interaction Types & Directionality:
    agonist (activating)

    Interaction Info:
    Trial Name brimonidine tartrate,Alphagan
    Novel drug target Established target
    Trial Name brimonidine tartrate/timolol maleate,Combigan

    PMIDs:
    16407989 10799649 1373179 11481271 11752352


    Sources:
    DTC TdgClinicalTrial TEND PharmGKB TTD

  • FIPAMEZOLE   ADRA2A

    Interaction Score: 0.58

    Interaction Types & Directionality:
    n/a

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

    PMIDs:
    None found


    Sources:
    TdgClinicalTrial TTD

  • ESMIRTAZAPINE   ADRA2A

    Interaction Score: 0.58

    Interaction Types & Directionality:
    antagonist (inhibitory)

    Interaction Info:
    Novel drug target Established target
    Trial Name esmirtazapine, ORG-4420

    PMIDs:
    26047892


    Sources:
    TdgClinicalTrial

  • MIRTAZAPINE   ADRA2A

    Interaction Score: 0.55

    Interaction Types & Directionality:
    antagonist (inhibitory)

    Interaction Info:
    Mechanism of Interaction Adrenergic receptor alpha-2 antagonist
    Direct Interaction yes
    Trial Name mirtazapine,Remeron, Remeron SolTab, Reflex

    PMIDs:
    11607047 11939713 10793320 12523492 11931344 14628003 9007838 19401164 8930006


    Sources:
    TdgClinicalTrial ChemblInteractions TEND

  • NOREPINEPHRINE   ADRA2A

    Interaction Score: 0.49

    Interaction Types & Directionality:
    agonist (activating)

    Interaction Info:
    Trial Name -
    Novel drug target Established target

    PMIDs:
    16407989 1980236 9836297 18680204 11306720 10742288 18064417 17016423 17139284


    Sources:
    DTC TdgClinicalTrial TEND PharmGKB

  • FENOLDOPAM   ADRA2A

    Interaction Score: 0.44

    Interaction Types & Directionality:
    antagonist (inhibitory)

    Interaction Info:

    PMIDs:
    17016423 17139284 7670737


    Sources:
    TEND

  • BETHANIDINE   ADRA2A

    Interaction Score: 0.44

    Interaction Types & Directionality:
    agonist (activating)

    Interaction Info:
    Trial Name -
    Novel drug target Established target

    PMIDs:
    2545383 1962798


    Sources:
    TdgClinicalTrial TEND

  • FADOLMIDINE   ADRA2A

    Interaction Score: 0.44

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    TTD

  • NICERGOLINE   ADRA2A

    Interaction Score: 0.44

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    TTD

  • DROXIDOPA   ADRA2A

    Interaction Score: 0.44

    Interaction Types & Directionality:
    agonist (activating)

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

    PMIDs:
    18680204 21173850 11306720


    Sources:
    ChemblInteractions

  • TRAZODONE   ADRA2A

    Interaction Score: 0.4

    Interaction Types & Directionality:
    antagonist (inhibitory)

    Interaction Info:

    PMIDs:
    7855217 17016423 17139284 1365657 3016788


    Sources:
    TEND

  • METHYLDOPA   ADRA2A

    Interaction Score: 0.34

    Interaction Types & Directionality:
    agonist (activating)

    Interaction Info:
    Trial Name -
    Novel drug target Established target
    Mechanism of Interaction Adrenergic receptor alpha-2 agonist

    PMIDs:
    9284427 8743022 10415926 1363322 17485976 14557373 17016423 17139284


    Sources:
    TdgClinicalTrial ChemblInteractions TEND

  • TIZANIDINE HYDROCHLORIDE   ADRA2A

    Interaction Score: 0.29

    Interaction Types & Directionality:
    agonist (activating)

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

    PMIDs:
    None found


    Sources:
    ChemblInteractions

  • CLONIDINE HYDROCHLORIDE   ADRA2A

    Interaction Score: 0.29

    Interaction Types & Directionality:
    agonist (activating)

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

    PMIDs:
    None found


    Sources:
    ChemblInteractions

  • EPINEPHRINE   ADRA2A

    Interaction Score: 0.29

    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 9836297 18680204 11306720 10742288 18064417 6134529


    Sources:
    TdgClinicalTrial ChemblInteractions PharmGKB

  • DEXMEDETOMIDINE HYDROCHLORIDE   ADRA2A

    Interaction Score: 0.29

    Interaction Types & Directionality:
    agonist (activating)

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

    PMIDs:
    None found


    Sources:
    ChemblInteractions

  • FADOLMIDINE HYDROCHLORIDE   ADRA2A

    Interaction Score: 0.29

    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   ADRA2A

    Interaction Score: 0.29

    Interaction Types & Directionality:
    agonist (activating)

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

    PMIDs:
    None found


    Sources:
    ChemblInteractions

  • METHYLDOPATE HYDROCHLORIDE   ADRA2A

    Interaction Score: 0.29

    Interaction Types & Directionality:
    agonist (activating)

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

    PMIDs:
    None found


    Sources:
    ChemblInteractions

  • DEBRISOQUIN   ADRA2A

    Interaction Score: 0.29

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    Novel drug target Established target
    Trial Name -

    PMIDs:
    None found


    Sources:
    TdgClinicalTrial TEND

  • BRIMONIDINE TARTRATE   ADRA2A

    Interaction Score: 0.29

    Interaction Types & Directionality:
    agonist (activating)

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

    PMIDs:
    None found


    Sources:
    ChemblInteractions

  • MIANSERIN   ADRA2A

    Interaction Score: 0.26

    Interaction Types & Directionality:
    antagonist (inhibitory)

    Interaction Info:
    Novel drug target Established target
    Trial Name -

    PMIDs:
    16814817


    Sources:
    TdgClinicalTrial TEND

  • PSEUDOEPHEDRINE   ADRA2A

    Interaction Score: 0.26

    Interaction Types & Directionality:
    agonist (activating)

    Interaction Info:
    Trial Name fexofenadine + ps/
    Novel drug target Established target

    PMIDs:
    17016423 17139284 7507588


    Sources:
    TdgClinicalTrial TEND

  • GUANFACINE HYDROCHLORIDE   ADRA2A

    Interaction Score: 0.22

    Interaction Types & Directionality:
    agonist (activating)

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

    PMIDs:
    None found


    Sources:
    ChemblInteractions

  • GUANABENZ ACETATE   ADRA2A

    Interaction Score: 0.22

    Interaction Types & Directionality:
    agonist (activating)

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

    PMIDs:
    None found


    Sources:
    ChemblInteractions

  • MEPERIDINE   ADRA2A

    Interaction Score: 0.22

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    TTD

  • RAUWOLFIA SERPENTINA   ADRA2A

    Interaction Score: 0.17

    Interaction Types & Directionality:
    antagonist (inhibitory)

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

    PMIDs:
    None found


    Sources:
    ChemblInteractions

  • MILNACIPRAN   ADRA2A

    Interaction Score: 0.17

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    PharmGKB

  • LEVONORDEFRIN   ADRA2A

    Interaction Score: 0.16

    Interaction Types & Directionality:
    agonist (activating)

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

    PMIDs:
    19326476


    Sources:
    ChemblInteractions

  • ALSEROXYLON   ADRA2A

    Interaction Score: 0.15

    Interaction Types & Directionality:
    antagonist (inhibitory)

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

    PMIDs:
    None found


    Sources:
    ChemblInteractions

  • MEDETOMIDINE   ADRA2A

    Interaction Score: 0.15

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    TTD

  • NAPHAZOLINE HYDROCHLORIDE   ADRA2A

    Interaction Score: 0.15

    Interaction Types & Directionality:
    agonist (activating)

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

    PMIDs:
    None found


    Sources:
    ChemblInteractions

  • ESMIRTAZAPINE MALEATE   ADRA2A

    Interaction Score: 0.15

    Interaction Types & Directionality:
    antagonist (inhibitory)

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

    PMIDs:
    None found


    Sources:
    ChemblInteractions

  • TETRAHYDROZOLINE HYDROCHLORIDE   ADRA2A

    Interaction Score: 0.15

    Interaction Types & Directionality:
    agonist (activating)

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

    PMIDs:
    None found


    Sources:
    ChemblInteractions

  • SENREBOTASE   ADRA2A

    Interaction Score: 0.15

    Interaction Types & Directionality:
    n/a

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

    PMIDs:
    None found


    Sources:
    TdgClinicalTrial

  • DOPAMINE   ADRA2A

    Interaction Score: 0.14

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    16407989


    Sources:
    DTC PharmGKB

  • METHAMPHETAMINE   ADRA2A

    Interaction Score: 0.13

    Interaction Types & Directionality:
    agonist (activating)

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

    PMIDs:
    9551769 12453616 15955613


    Sources:
    TdgClinicalTrial

  • PARDOPRUNOX   ADRA2A

    Interaction Score: 0.12

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    Trial Name pardoprunox, SLV 308
    Novel drug target Established target

    PMIDs:
    None found


    Sources:
    TdgClinicalTrial

  • OXYMETAZOLINE HYDROCHLORIDE   ADRA2A

    Interaction Score: 0.12

    Interaction Types & Directionality:
    agonist (activating)

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

    PMIDs:
    None found


    Sources:
    ChemblInteractions

  • MEPHENTERMINE SULFATE   ADRA2A

    Interaction Score: 0.11

    Interaction Types & Directionality:
    agonist (activating)

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

    PMIDs:
    None found


    Sources:
    ChemblInteractions

  • DIPIVEFRIN HYDROCHLORIDE   ADRA2A

    Interaction Score: 0.11

    Interaction Types & Directionality:
    agonist (activating)

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

    PMIDs:
    None found


    Sources:
    ChemblInteractions

  • TOLAZOLINE HYDROCHLORIDE   ADRA2A

    Interaction Score: 0.11

    Interaction Types & Directionality:
    antagonist (inhibitory)

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

    PMIDs:
    None found


    Sources:
    ChemblInteractions

  • PHENTOLAMINE MESYLATE   ADRA2A

    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

  • ASENAPINE   ADRA2A

    Interaction Score: 0.1

    Interaction Types & Directionality:
    antagonist (inhibitory)

    Interaction Info:
    Trial Name Asenapine
    Novel drug target Established target

    PMIDs:
    18308814


    Sources:
    TdgClinicalTrial

  • HYDROXYAMPHETAMINE HYDROBROMIDE   ADRA2A

    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

  • LABETALOL HYDROCHLORIDE   ADRA2A

    Interaction Score: 0.1

    Interaction Types & Directionality:
    antagonist (inhibitory)

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

    PMIDs:
    None found


    Sources:
    ChemblInteractions

  • PHENOXYBENZAMINE HYDROCHLORIDE   ADRA2A

    Interaction Score: 0.1

    Interaction Types & Directionality:
    antagonist (inhibitory)

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

    PMIDs:
    None found


    Sources:
    ChemblInteractions

  • NOREPINEPHRINE BITARTRATE   ADRA2A

    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

  • ERGOLOID MESYLATES   ADRA2A

    Interaction Score: 0.07

    Interaction Types & Directionality:
    antagonist (inhibitory)

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

    PMIDs:
    None found


    Sources:
    ChemblInteractions

  • AMPHETAMINE   ADRA2A

    Interaction Score: 0.07

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    TEND

  • EPINEPHRINE BITARTRATE   ADRA2A

    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

  • ATENOLOL   ADRA2A

    Interaction Score: 0.05

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    15614026


    Sources:
    PharmGKB

  • ISOPROTERENOL   ADRA2A

    Interaction Score: 0.03

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    PharmGKB

  • OLANZAPINE   ADRA2A

    Interaction Score: 0.03

    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: ENSG00000150594

    • Version: 101_38

    Alternate Names:
    ADRA2A Ensembl Gene Name

    Gene Info:
    Gene Biotype PROTEIN_CODING

    Publications:

  • RussLampel: ENSG00000150594

    • Version: 26-July-2011

    Alternate Names:
    ENSG00000150594 Ensembl Gene Id
    ADRA2A Display Id
    ALPHA-2A ADRENERGIC RECEPTOR (ALPHA-2A ADRENOCEPTOR) (ALPHA-2A ADRENORECEPTOR) (ALPHA-2AAR SUBTYPE C10). [SOURCE:UNIPROT/SWISSPROT;ACC:P08913] Description

    Gene Info:
    Human Readable Name DRUGGABLE GENOME

    Gene Categories:
    DRUGGABLE GENOME

    Publications:

  • TdgClinicalTrial: P08913

    • Version: January-2014

    Alternate Names:
    ADRA2A Gene Symbol

    Gene Info:
    Target Class Receptors
    Target Subclass GPCR
    Target Subclass Rhodopsin

    Publications:

  • TEND: P08913

    • Version: 01-August-2011

    Alternate Names:
    150 Entrez Gene Id
    ADRA2A Gene Symbol
    P08913 Uniprot Accession

    Gene Info:
    Target Subclass Rhodopsin
    Transmembrane Helix Count 7
    Target Main Class Receptors

    Publications:

  • HopkinsGroom: P08913

    • Version: 11-September-2012

    Alternate Names:
    ADRA2A Uniprot Gene Name
    P08913 Uniprot Accession
    150 Entrez Gene Id

    Gene Info:
    Uniprot Evidence 1: Evidence at protein level
    Human Readable Name DRUGGABLE GENOME
    Human Readable Name G PROTEIN COUPLED RECEPTOR

    Gene Categories:
    G PROTEIN COUPLED RECEPTOR, DRUGGABLE GENOME

    Publications:

  • PharmGKB: ADRA2A

    • Version: 18-August-2020

    Alternate Names:
    PA35 PharmGKB ID

    Gene Info:

    Publications:
    Yin L et al., 2015, TPH, SLC6A2, SLC6A3, DRD2 and DRD4 Polymorphisms and Neuroendocrine Factors Predict SSRIs Treatment Outcome in the Chinese Population with Major Depression., Pharmacopsychiatry
    Liljedahl U et al., 2004, Single nucleotide polymorphisms predict the change in left ventricular mass in response to antihypertensive treatment., J Hypertens
    Yağar S et al., 2011, The role of the ADRA2A C1291G genetic polymorphism in response to dexmedetomidine on patients undergoing coronary artery surgery., Mol Biol Rep

  • TTD: Adrenergic receptor Alpha-2

    • Version: 2020.06.01

    Alternate Names:
    ADRA2 TTD Gene Abbreviation
    T31424 TTD Target ID

    Gene Info:

    Publications:
    Khalil A et al., 2008, Effect of antihypertensive therapy with alpha methyldopa on levels of angiogenic factors in pregnancies with hypertensive disorders., PLoS One

  • DTC: ADRA2A

    • Version: 02-September-2020

    Alternate Names:

    Gene Info:

    Publications:
    Vilardaga JP et al., 2005, Molecular basis of inverse agonism in a G protein-coupled receptor., Nat Chem Biol

  • HingoraniCasas: ENSG00000150594

    • Version: 31-May-2017

    Alternate Names:
    ENSG00000150594 Gene Symbol
    ADRA2A Ensembl Id

    Gene Info:

    Gene Categories:
    DRUGGABLE GENOME

    Publications:

  • ChemblInteractions: ADRA2R

    • Version: chembl_23

    Alternate Names:
    ADRAR GENE_SYMBOL
    ADRA2A GENE_SYMBOL
    Alpha-2A adrenergic receptor UNIPROT

    Gene Info:

    Publications:

  • GO: ADRA2A

    • Version: 01-February-2022

    Alternate Names:
    ADRA2R GO Gene Synonym
    ADRAR GO Gene Synonym

    Gene Info:

    Gene Categories:
    G PROTEIN COUPLED RECEPTOR

    Publications:

  • dGene: ADRA2A

    • Version: 27-Jun-2013

    Alternate Names:
    150 Gene ID
    ADRA2 dGene Synonym
    ADRA2R dGene Synonym

    Gene Info:

    Gene Categories:
    G PROTEIN COUPLED RECEPTOR

    Publications:

  • TTD: Adrenergic receptor alpha-2A

    • Version: 2020.06.01

    Alternate Names:
    ADRA2A TTD Gene Abbreviation
    T11448 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