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GABRA1 Gene Record

  • Summary
  • Interactions
  • Claims
  • GABRA1 2554 Druggable Genome

    Alternate Names:

    2554
    GAMMA-AMINOBUTYRIC ACID TYPE A RECEPTOR ALPHA1 SUBUNIT
    GABRA1
    ECA4
    EIEE19
    EJM
    EJM5
    137160
    4075
    ENSG00000022355
    OTTHUMG00000163586
    GABA(A) receptor subunit alpha-1
    Gamma-aminobutyric acid receptor subunit alpha-1
    P14867
    GBRA1_HUMAN
    BE0008668
    BE0000795
    404
    NP_000797
    NM_000806
    BE0004797
    GAMMA-AMINOBUTYRIC-ACID RECEPTOR ALPHA-1 SUBUNIT PRECURSOR (GABA(A) RECEPTOR). [SOURCE:UNIPROT/SWISSPROT;ACC:P14867]
    GABA<sub>A</sub> receptor &alpha;1 subunit
    GABRD
    PA28489
    GABA(A) receptor alpha-1
    T51487
    gamma-aminobutyric acid type A receptor subunit alpha1

    Gene Info:

    GuideToPharmacology Gene Category Name GABA<sub>A</sub> receptors
    GuideToPharmacology Gene Category ID 72
    Human Readable Name ION CHANNEL
    Interpro Short Name Neur_chan_lig-bd
    Human Readable Name DRUGGABLE GENOME
    Interpro Name Neurotransmitter-gated ion-channel
    Interpro Acc IPR006202
    Interpro Name Neurotransmitter-gated ion-channel ligand-binding
    Interpro Type Domain
    Interpro Acc IPR006201
    Interpro Short Name Neur_channel
    Uniprot Evidence 1: Evidence at protein level
    Uniprot Status Swiss-Prot
    Interpro Type Family
    Target Subclass Channels
    Target Subclass Ligand_gated_ion_channels
    Target Subclass cys-loop
    Target Main Class Receptors
    Transmembrane Helix Count 4
    Target Class Receptors
    Target Subclass TC:1.A.9
    Gene Biotype PROTEIN_CODING
    (11 More Sources)

    Gene Categories: Category Details

    ION CHANNEL
    DRUGGABLE GENOME

    Publications:

    Riss et al., 2008, Benzodiazepines in epilepsy: pharmacology and pharmacokinetics., Acta Neurol. Scand.
    Möhler et al., 2002, A new benzodiazepine pharmacology., J. Pharmacol. Exp. Ther.
    Zhu S et al., 2018, Structure of a human synaptic GABA<sub>A</sub> receptor., Nature
    Sigel E et al., 2012, Structure, function, and modulation of GABA(A) receptors., J Biol Chem
    Feigenspan et al., 2004, Electrophysiological properties of mouse horizontal cell GABAA receptors., J. Neurophysiol.
    Whiting, 2003, The GABAA receptor gene family: new opportunities for drug development., Curr Opin Drug Discov Devel
    Steinbach et al., 2001, Modulation of GABA(A) receptor channel gating by pentobarbital., J. Physiol. (Lond.)
    Yamakura et al., 2001, Anesthetics and ion channels: molecular models and sites of action., Annu. Rev. Pharmacol. Toxicol.
    Chen et al., 2002, TTD: Therapeutic Target Database., Nucleic Acids Res.
    Overington et al., 2006, How many drug targets are there?, Nat Rev Drug Discov
    Mehta et al., 1999, An update on GABAA receptors., Brain Res. Brain Res. Rev.
    Davies et al., 2001, Pressure-sensitive and -insensitive coupling in gamma-aminobutyric acid(A) receptors., Psychopharmacology (Berl.)
    Imming et al., 2006, Drugs, their targets and the nature and number of drug targets., Nat Rev Drug Discov
    Krasowski et al., 1999, General anaesthetic actions on ligand-gated ion channels., Cell. Mol. Life Sci.
    Rahman et al., 2006, GABA-site antagonism and pentobarbital actions do not depend on the alpha-subunit type in the recombinant rat GABA receptor., Acta Physiol (Oxf)
    Koltchine et al., 1996, Chimeric GABAA/glycine receptors: expression and barbiturate pharmacology., Neuropharmacology
    Verster et al., 2004, Clinical pharmacology, clinical efficacy, and behavioral toxicity of alprazolam: a review of the literature., CNS Drug Rev
    McCracken et al., 2010, A transmembrane amino acid in the GABAA receptor β2 subunit critical for the actions of alcohols and anesthetics., J. Pharmacol. Exp. Ther.
    Seo et al., 2010, Genetic reduction of GABA(A) receptor gamma2 subunit expression potentiates the immobilizing action of isoflurane., Neurosci. Lett.
    Nowakowska et al., 2009, Memory improving and antidepressant effects of topiramate in rats., Arzneimittelforschung
    Chung JY et al., 2014, Efficacy of zonisamide in migraineurs with nonresponse to topiramate., Biomed Res Int
    Garnett WR, 2000, Clinical pharmacology of topiramate: a review., Epilepsia
    Braga et al., 2009, Topiramate reduces excitability in the basolateral amygdala by selectively inhibiting GluK1 (GluR5) kainate receptors on interneurons and positively modulating GABAA receptors on principal neurons., J. Pharmacol. Exp. Ther.
    Buckley et al., 1998, Can the fatal toxicity of antidepressant drugs be predicted with pharmacological and toxicological data?, Drug Saf
    Wei et al., 1990, [Comparison of the affinities of amoxapine and loxapine for various receptors in rat brain and the receptor down-regulation after chronic administration]., Yao Xue Xue Bao
    de Fiebre et al., 1992, Classical genetic analyses of responses to sedative-hypnotic drugs in crosses derived from long-sleep and short-sleep mice., Alcohol. Clin. Exp. Res.
    Sethy et al., 1984, Determination of biological activity of adinazolam and its metabolites., J. Pharm. Pharmacol.
    Lahti et al., 1983, Pharmacological profile of the antidepressant adinazolam, a triazolobenzodiazepine., Neuropharmacology
    Amin et al., 1997, Two tyrosine residues on the alpha subunit are crucial for benzodiazepine binding and allosteric modulation of gamma-aminobutyric acidA receptors., Mol. Pharmacol.
    Whitwam et al., 1995, Pharmacology of flumazenil., Acta Anaesthesiol Scand Suppl
    Wingrove et al., 2002, Mechanism of alpha-subunit selectivity of benzodiazepine pharmacology at gamma-aminobutyric acid type A receptors., Eur. J. Pharmacol.
    Iorio et al., 1984, Selective affinity of 1-N-trifluoroethyl benzodiazepines for cerebellar type 1 receptor sites., Life Sci.
    Wamsley et al., 1985, Autoradiographic demonstration of the selectivity of two 1-N-trifluoroethyl benzodiazepines for the BZD-1 receptors in the rat brain., Pharmacol. Biochem. Behav.
    Rho et al., 1997, Barbiturate-like actions of the propanediol dicarbamates felbamate and meprobamate., J. Pharmacol. Exp. Ther.
    Gonzalez et al., 2009, Carisoprodol-mediated modulation of GABAA receptors: in vitro and in vivo studies., J. Pharmacol. Exp. Ther.
    Grasshoff et al., 2006, Effects of isoflurane and enflurane on GABAA and glycine receptors contribute equally to depressant actions on spinal ventral horn neurones in rats., Br J Anaesth
    Franks, 2006, Molecular targets underlying general anaesthesia., Br. J. Pharmacol.
    Greenblatt et al., 2001, Divergence of volatile anesthetic effects in inhibitory neurotransmitter receptors., Anesthesiology
    Roden et al., 2010, Altered GABA(A) receptor subunit expression and pharmacology in human Angelman syndrome cortex., Neurosci. Lett.
    Olsen et al., 2011, GABA(A) receptors as molecular targets of general anesthetics: identification of binding sites provides clues to allosteric modulation., Can J Anaesth
    Dixon CL et al., 2015, Zolpidem and eszopiclone prime α1β2γ2 GABAA receptors for longer duration of activity., Br J Pharmacol
    Hanson et al., 2008, Structural requirements for eszopiclone and zolpidem binding to the gamma-aminobutyric acid type-A (GABAA) receptor are different., J. Med. Chem.
    Döble A et al., 1995, The mechanism of action of zopiclone., Eur Psychiatry
    Wadworth AN et al., 1993, Zopiclone. A review of its pharmacological properties and therapeutic efficacy as an hypnotic., Drugs Aging
    Nutt et al., 2010, Searching for perfect sleep: the continuing evolution of GABAA receptor modulators as hypnotics., J. Psychopharmacol. (Oxford)
    Martin et al., 2009, Etomidate targets alpha5 gamma-aminobutyric acid subtype A receptors to regulate synaptic plasticity and memory blockade., Anesthesiology
    Husain SS et al., 2006, Synthesis of trifluoromethylaryl diazirine and benzophenone derivatives of etomidate that are potent general anesthetics and effective photolabels for probing sites on ligand-gated ion channels., J Med Chem
    Husain SS et al., 2010, p-Trifluoromethyldiazirinyl-etomidate: a potent photoreactive general anesthetic derivative of etomidate that is selective for ligand-gated cationic ion channels., J Med Chem
    Desai et al., 2009, Gamma-amino butyric acid type A receptor mutations at beta2N265 alter etomidate efficacy while preserving basal and agonist-dependent activity., Anesthesiology
    Smith et al., 2001, Effect of alpha subunit on allosteric modulation of ion channel function in stably expressed human recombinant gamma-aminobutyric acid(A) receptors determined using (36)Cl ion flux., Mol. Pharmacol.
    Tan KR et al., 2011, Hooked on benzodiazepines: GABAA receptor subtypes and addiction., Trends Neurosci
    Sramka M et al., 1975, Surgical complication of posterior hypothalamotomy., Confin Neurol
    Vlainić et al., 2009, Effects of acute and repeated zolpidem treatment on pentylenetetrazole-induced seizure threshold and on locomotor activity: comparison with diazepam., Neuropharmacology
    Pritchett et al., 1990, Gamma-aminobutyric acidA receptor alpha 5-subunit creates novel type II benzodiazepine receptor pharmacology., J. Neurochem.
    Meldrum et al., 1986, Benzodiazepine receptors and their relationship to the treatment of epilepsy., Epilepsia
    Billard et al., 1988, Selective affinity of the benzodiazepines quazepam and 2-oxo-quazepam for BZ1 binding site and demonstration of 3H-2-oxo-quazepam as a BZ1 selective radioligand., Life Sci.
    Nakatsuka et al., 1985, Benzodiazepines and their metabolites: relationship between binding affinity to the benzodiazepine receptor and pharmacological activity., Life Sci.
    Franks NP et al., 1994, Molecular and cellular mechanisms of general anaesthesia., Nature
    Qi ZH et al., 2007, Protein kinase C epsilon regulates gamma-aminobutyrate type A receptor sensitivity to ethanol and benzodiazepines through phosphorylation of gamma2 subunits., J Biol Chem
    Mandrioli et al., 2008, Benzodiazepine metabolism: an analytical perspective., Curr. Drug Metab.
    Baburin et al., 2008, Estimating the efficiency of benzodiazepines on GABA(A) receptors comprising gamma1 or gamma2 subunits., Br. J. Pharmacol.
    Derry et al., 2004, Identification of a residue in the gamma-aminobutyric acid type A receptor alpha subunit that differentially affects diazepam-sensitive and -insensitive benzodiazepine site binding., J. Neurochem.
    Barbera et al., 2005, Benefit-risk assessment of zaleplon in the treatment of insomnia., Drug Saf
    Terzano et al., 2003, New drugs for insomnia: comparative tolerability of zopiclone, zolpidem and zaleplon., Drug Saf
    Sanger et al., 1999, Discriminative stimulus effects of drugs acting at GABA(A) receptors: differential profiles and receptor selectivity., Pharmacol. Biochem. Behav.
    Patat et al., 2001, Pharmacodynamic profile of Zaleplon, a new non-benzodiazepine hypnotic agent., Hum Psychopharmacol
    Grech et al., 1993, Pentobarbital-like discriminative stimulus effects of direct GABA agonists in rats., Psychopharmacology (Berl.)
    Fadda et al., 1985, Suppression by progabide of ethanol withdrawal syndrome in rats., Eur. J. Pharmacol.
    Agmo et al., 1998, Interactions between dopamine and GABA in the control of ambulatory activity and neophobia in the mouse., Pharmacol. Biochem. Behav.
    Ramerstorfer et al., 2010, The point mutation gamma 2F77I changes the potency and efficacy of benzodiazepine site ligands in different GABAA receptor subtypes., Eur. J. Pharmacol.
    Sanger, 2004, The pharmacology and mechanisms of action of new generation, non-benzodiazepine hypnotic agents., CNS Drugs
    Skerritt et al., 1983, Enhancement of GABA binding by benzodiazepines and related anxiolytics., Eur. J. Pharmacol.
    Zhou BT et al., 2012, Effects of SCN1A and GABA receptor genetic polymorphisms on carbamazepine tolerability and efficacy in Chinese patients with partial seizures: 2-year longitudinal clinical follow-up., CNS Neurosci Ther
    Sugimura et al., 2002, Effects of GABAergic agents on anesthesia induced by halothane, isoflurane, and thiamylal in mice., Pharmacol. Biochem. Behav.
    Grasshoff et al., 2008, Depression of spinal network activity by thiopental: shift from phasic to tonic GABA(A) receptor-mediated inhibition., Neuropharmacology
    Moody et al., 1988, The imidazobenzodiazepine Ro 15-4513 antagonizes methoxyflurane anesthesia., Life Sci.
    Moody et al., 1988, Modulation of the benzodiazepine/gamma-aminobutyric acid receptor chloride channel complex by inhalation anesthetics., J. Neurochem.
    Krasowski et al., 2000, The actions of ether, alcohol and alkane general anaesthetics on GABAA and glycine receptors and the effects of TM2 and TM3 mutations., Br. J. Pharmacol.
    Stewart DS et al., 2011, p-(4-Azipentyl)propofol: a potent photoreactive general anesthetic derivative of propofol., J Med Chem
    Braestrup et al., 1978, Pharmacological characterization of benzodiazepine receptors in the brain., Eur. J. Pharmacol.
    Miller et al., 1987, Benzodiazepine receptor binding of triazolobenzodiazepines in vivo: increased receptor number with low-dose alprazolam., J. Neurochem.
    Giersch et al., 2010, Atypical behavioural effects of lorazepam: clues to the design of novel therapies?, Pharmacol. Ther.
    Hedera P et al., 2013, Pharmacotherapy of essential tremor., J Cent Nerv Syst Dis
    Cutrer et al., Attenuation by butalbital of capsaicin-induced c-fos-like immunoreactivity in trigeminal nucleus caudalis., Headache
    Bymaster et al., 1996, Radioreceptor binding profile of the atypical antipsychotic olanzapine., Neuropsychopharmacology
    Brafford MV et al., 2014, Olanzapine: an antiemetic option for chemotherapy-induced nausea and vomiting., J Adv Pract Oncol
    Blaschke et al., 1986, [Racemation of the benzodiazepines camazepam and ketazolam and receptor binding of enantiomers]., Arzneimittelforschung
    Nishikawa K et al., 2002, Volatile anesthetic actions on the GABAA receptors: contrasting effects of alpha 1(S270) and beta 2(N265) point mutations., Neuropharmacology
    Nishikawa K et al., 2003, The actions of sevoflurane and desflurane on the gamma-aminobutyric acid receptor type A: effects of TM2 mutations in the alpha and beta subunits., Anesthesiology
    Richter et al., 2010, Intrinsic activation of GABA(A) receptors suppresses epileptiform activity in the cerebral cortex of immature mice., Epilepsia
    Law et al., 2008, Gaba receptor insecticide non-competitive antagonists may bind at allosteric modulator sites., Int. J. Neurosci.
    Macdonald et al., 1986, Anticonvulsant drugs: mechanisms of action., Adv Neurol
    Miller et al., 1988, Acute barbiturate administration increases benzodiazepine receptor binding in vivo., Psychopharmacology (Berl.)
    Peters et al., 1988, Modulation of the GABAA receptor by depressant barbiturates and pregnane steroids., Br. J. Pharmacol.
    Kirkness et al., 1986, The gamma-aminobutyrate/benzodiazepine receptor from pig brain. Purification and characterization of the receptor complex from cerebral cortex and cerebellum., Biochem. J.
    Zaugg J et al., 2011, Identification and characterization of GABA(A) receptor modulatory diterpenes from Biota orientalis that decrease locomotor activity in mice., J Nat Prod
    Podhorna et al., 2000, Behavioural effects of a benzodiazepine receptor partial agonist, Ro 19-8022, in the social conflict test in mice., Behav Pharmacol
    Tanaka et al., 2008, Comparison of short- and long-acting benzodiazepine-receptor agonists with different receptor selectivity on motor coordination and muscle relaxation following thiopental-induced anesthesia in mice., J. Pharmacol. Sci.
    Smeyatsky et al., 1992, The treatment of sleep disorders., S. Afr. Med. J.
    Skerritt et al., 1983, Interactions of some anaesthetic, convulsant, and anticonvulsant drugs at GABA-benzodiazepine receptor-ionophore complexes in rat brain synaptosomal membranes., Neurochem. Res.
    Williams, 2005, Medications for treating alcohol dependence., Am Fam Physician
    Tomlin et al., 1999, Preparation of barbiturate optical isomers and their effects on GABA(A) receptors., Anesthesiology
    Santhakumar et al., 2007, Ethanol acts directly on extrasynaptic subtypes of GABAA receptors to increase tonic inhibition., Alcohol
    Davies, 2003, The role of GABAA receptors in mediating the effects of alcohol in the central nervous system., J Psychiatry Neurosci
    Earl et al., 2011, Inhibition of recombinant L-type voltage-gated calcium channels by positive allosteric modulators of GABAA receptors., J. Pharmacol. Exp. Ther.
    Petersen JG et al., 2014, Synthesis and pharmacological evaluation of 6-aminonicotinic acid analogues as novel GABA(A) receptor agonists., Eur J Med Chem
    Carta et al., 2006, The muscle relaxant thiocolchicoside is an antagonist of GABAA receptor function in the central nervous system., Neuropharmacology
    Mascia et al., 2007, Thiocolchicoside inhibits the activity of various subtypes of recombinant GABA(A) receptors expressed in Xenopus laevis oocytes., Eur. J. Pharmacol.
    Keppel Hesselink JM, 2017, Phenytoin: a step by step insight into its multiple mechanisms of action-80 years of mechanistic studies in neuropharmacology., J Neurol
    Sousa et al., 1997, Interactions of the neurosteroid dehydroepiandrosterone sulfate with the GABA(A) receptor complex reveals that it may act via the picrotoxin site., J. Pharmacol. Exp. Ther.
    Anzini M et al., 2011, New insight into the central benzodiazepine receptor-ligand interactions: design, synthesis, biological evaluation, and molecular modeling of 3-substituted 6-phenyl-4H-imidazo[1,5-a][1,4]benzodiazepines and related compounds., J Med Chem
    Meldrum BS, 1996, Update on the mechanism of action of antiepileptic drugs., Epilepsia
    Abelaira HM et al., 2012, Lamotrigine treatment reverses depressive-like behavior and alters BDNF levels in the brains of maternally deprived adult rats., Pharmacol Biochem Behav
    Braga MF et al., 2002, Lamotrigine reduces spontaneous and evoked GABAA receptor-mediated synaptic transmission in the basolateral amygdala: implications for its effects in seizure and affective disorders., Neuropharmacology
    Wang JF et al., 2002, Lamotrigine increases gene expression of GABA-A receptor beta3 subunit in primary cultured rat hippocampus cells., Neuropsychopharmacology
    Molinaro G et al., 2009, Memantine treatment reduces the expression of the K(+)/Cl(-) cotransporter KCC2 in the hippocampus and cerebral cortex, and attenuates behavioural responses mediated by GABA(A) receptor activation in mice., Brain Res
    Fernandes H et al., 2014, Mexazolam: clinical efficacy and tolerability in the treatment of anxiety., Neurol Ther
    Kilb W et al., 2017, Taurine as an Essential Neuromodulator during Perinatal Cortical Development., Front Cell Neurosci
    Clegg NJ et al., 2012, ARN-509: a novel antiandrogen for prostate cancer treatment., Cancer Res
    Gonzalez LA et al., 2009, Abuse Potential of Soma: the GABA(A) Receptor as a Target., Mol Cell Pharmacol
    Kumar M et al., 2016, Assessment of direct gating and allosteric modulatory effects of meprobamate in recombinant GABA(A) receptors., Eur J Pharmacol
    Fisher JL, 2009, The anti-convulsant stiripentol acts directly on the GABA(A) receptor as a positive allosteric modulator., Neuropharmacology
    Huen MS et al., 2003, Naturally occurring 2'-hydroxyl-substituted flavonoids as high-affinity benzodiazepine site ligands., Biochem Pharmacol
  • METHOHEXITAL   GABRA1

    Interaction Score: 3.52

    Interaction Types & Directionality:
    antagonist (inhibitory)

    Interaction Info:
    Trial Name -
    Novel drug target Established target

    PMIDs:
    9014160 11752352 17139284 17016423


    Sources:
    TEND TdgClinicalTrial TTD DrugBank

  • KETAZOLAM   GABRA1

    Interaction Score: 3.08

    Interaction Types & Directionality:
    ligand
    positive modulator (activating)
    potentiator

    Interaction Info:

    PMIDs:
    18384456 11752090 15009644 29950725 2874815 23038269


    Sources:
    DrugBank

  • MEXAZOLAM   GABRA1

    Interaction Score: 1.76

    Interaction Types & Directionality:
    ligand
    positive modulator (activating)

    Interaction Info:

    PMIDs:
    26000220 29950725 23038269


    Sources:
    DrugBank

  • PROGABIDE   GABRA1

    Interaction Score: 1.76

    Interaction Types & Directionality:
    agonist (activating)

    Interaction Info:
    Novel drug target Established target
    Trial Name -

    PMIDs:
    7831422 2985405 17139284 17016423 9443561


    Sources:
    TEND TdgClinicalTrial DrugBank

  • INDIPLON   GABRA1

    Interaction Score: 1.76

    Interaction Types & Directionality:
    positive modulator (activating)
    allosteric modulator

    Interaction Info:
    Mechanism of Interaction GABA receptor alpha-1 subunit positive allosteric modulator
    Direct Interaction yes
    Trial Name Indiplon

    PMIDs:
    None found


    Sources:
    TdgClinicalTrial TTD GuideToPharmacology ChemblInteractions

  • CHEMBL146245   GABRA1

    Interaction Score: 1.32

    Interaction Types & Directionality:
    ligand
    positive modulator (activating)

    Interaction Info:

    PMIDs:
    29950725 23038269


    Sources:
    DrugBank

  • NORDAZEPAM   GABRA1

    Interaction Score: 1.32

    Interaction Types & Directionality:
    ligand
    positive modulator (activating)

    Interaction Info:

    PMIDs:
    29950725 23038269


    Sources:
    DrugBank

  • PINAZEPAM   GABRA1

    Interaction Score: 1.32

    Interaction Types & Directionality:
    ligand
    positive modulator (activating)

    Interaction Info:

    PMIDs:
    29950725 23038269


    Sources:
    DrugBank

  • CAMAZEPAM   GABRA1

    Interaction Score: 1.32

    Interaction Types & Directionality:
    ligand
    positive modulator (activating)

    Interaction Info:

    PMIDs:
    29950725 23038269


    Sources:
    DrugBank

  • CINAZEPAM   GABRA1

    Interaction Score: 1.32

    Interaction Types & Directionality:
    ligand
    positive modulator (activating)

    Interaction Info:

    PMIDs:
    29950725 23038269


    Sources:
    DrugBank

  • ETHYL LOFLAZEPATE   GABRA1

    Interaction Score: 1.32

    Interaction Types & Directionality:
    ligand
    positive modulator (activating)

    Interaction Info:

    PMIDs:
    29950725 23038269


    Sources:
    DrugBank

  • MEDAZEPAM   GABRA1

    Interaction Score: 1.32

    Interaction Types & Directionality:
    ligand
    positive modulator (activating)

    Interaction Info:

    PMIDs:
    29950725 23038269


    Sources:
    DrugBank

  • CLOXAZOLAM   GABRA1

    Interaction Score: 1.32

    Interaction Types & Directionality:
    ligand
    positive modulator (activating)

    Interaction Info:

    PMIDs:
    29950725 23038269


    Sources:
    DrugBank

  • DOXEFAZEPAM   GABRA1

    Interaction Score: 1.32

    Interaction Types & Directionality:
    ligand
    positive modulator (activating)

    Interaction Info:

    PMIDs:
    29950725 23038269


    Sources:
    DrugBank

  • LORMETAZEPAM   GABRA1

    Interaction Score: 1.32

    Interaction Types & Directionality:
    ligand
    positive modulator (activating)

    Interaction Info:

    PMIDs:
    29950725 23038269


    Sources:
    DrugBank

  • DELORAZEPAM   GABRA1

    Interaction Score: 1.32

    Interaction Types & Directionality:
    ligand
    positive modulator (activating)

    Interaction Info:

    PMIDs:
    29950725 23038269


    Sources:
    DrugBank

  • LOPRAZOLAM   GABRA1

    Interaction Score: 1.32

    Interaction Types & Directionality:
    ligand
    positive modulator (activating)

    Interaction Info:

    PMIDs:
    29950725 23038269


    Sources:
    DrugBank

  • THIAMYLAL   GABRA1

    Interaction Score: 1.21

    Interaction Types & Directionality:
    agonist (activating)

    Interaction Info:
    Novel drug target Established target
    Trial Name -

    PMIDs:
    14579514 11900777 11264449 17139284 10209232 17016423 10487207 18619475


    Sources:
    TEND TdgClinicalTrial DrugBank

  • ZALEPLON   GABRA1

    Interaction Score: 1.21

    Interaction Types & Directionality:
    positive modulator (activating)
    potentiator

    Interaction Info:
    Direct Interaction yes
    Mechanism of Interaction GABA A receptor alpha-1/beta-1/gamma-2 positive allosteric modulator
    Trial Name AZ-007, Staccato zaleplon

    PMIDs:
    15783240 12608888 17139284 17016423 10515302 12404558


    Sources:
    TEND TdgClinicalTrial TTD DrugBank ChemblInteractions

  • CHEMBL488994   GABRA1

    Interaction Score: 0.88

    Interaction Types & Directionality:
    ligand

    Interaction Info:

    PMIDs:
    14637197


    Sources:
    DrugBank

  • ZOPICLONE   GABRA1

    Interaction Score: 0.7

    Interaction Types & Directionality:
    potentiator

    Interaction Info:
    Trial Name -
    Novel drug target Established target

    PMIDs:
    18973287 20303942 19942638 15291009 6135616


    Sources:
    TEND TdgClinicalTrial DrugBank

  • BROTIZOLAM   GABRA1

    Interaction Score: 0.66

    Interaction Types & Directionality:
    ligand
    positive modulator (activating)

    Interaction Info:

    PMIDs:
    29950725 23038269


    Sources:
    DrugBank

  • BENTAZEPAM   GABRA1

    Interaction Score: 0.66

    Interaction Types & Directionality:
    ligand
    positive modulator (activating)

    Interaction Info:

    PMIDs:
    29950725 23038269


    Sources:
    DrugBank

  • ETIZOLAM   GABRA1

    Interaction Score: 0.66

    Interaction Types & Directionality:
    ligand
    positive modulator (activating)

    Interaction Info:

    PMIDs:
    29950725 23038269


    Sources:
    DrugBank

  • SECOBARBITAL   GABRA1

    Interaction Score: 0.56

    Interaction Types & Directionality:
    potentiator

    Interaction Info:
    Trial Name -
    Novel drug target Established target

    PMIDs:
    14579514 2906155 2850060 11264449 3006661 11752352 17139284 10209232 17016423 10487207


    Sources:
    TEND TdgClinicalTrial TTD DrugBank

  • HEXOBARBITAL   GABRA1

    Interaction Score: 0.53

    Interaction Types & Directionality:
    potentiator

    Interaction Info:
    Novel drug target Established target
    Trial Name -

    PMIDs:
    14579514 10360871 11264449 11752352 17139284 10209232 17016423 10487207


    Sources:
    TEND TdgClinicalTrial TTD DrugBank

  • ZOLPIDEM   GABRA1

    Interaction Score: 0.53

    Interaction Types & Directionality:
    agonist (activating)
    allosteric modulator
    potentiator

    Interaction Info:
    Details of the Assay for Interaction Assay using recombinant GABA<sub>A</sub> channels with subunit composition; &alpha;1&beta;3&gamma;2.
    Specific Action of the Ligand Positive
    Endogenous Drug? False

    PMIDs:
    11306694 21353710 17139284 1093783 19345234 17016423 2157817


    Sources:
    TEND TdgClinicalTrial TTD DrugBank GuideToPharmacology

  • BUTETHAL   GABRA1

    Interaction Score: 0.48

    Interaction Types & Directionality:
    potentiator

    Interaction Info:
    Trial Name -
    Novel drug target Established target

    PMIDs:
    14579514 11264449 11752352 17139284 10209232 17016423 10487207


    Sources:
    TEND TdgClinicalTrial TTD DrugBank

  • APALUTAMIDE   GABRA1

    Interaction Score: 0.44

    Interaction Types & Directionality:
    antagonist (inhibitory)

    Interaction Info:

    PMIDs:
    22266222


    Sources:
    DrugBank

  • ISOPIMARIC ACID   GABRA1

    Interaction Score: 0.44

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    21793559


    Sources:
    DTC

  • SANDARACOPIMARIC ACID   GABRA1

    Interaction Score: 0.44

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    21793559


    Sources:
    DTC

  • MEPHOBARBITAL   GABRA1

    Interaction Score: 0.44

    Interaction Types & Directionality:
    potentiator

    Interaction Info:
    Novel drug target Established target
    Trial Name -

    PMIDs:
    20692323 14579514 21194017 11264449 11752352 17139284 10209232 17016423 10487207


    Sources:
    TEND TdgClinicalTrial TTD DrugBank

  • PENTOBARBITAL   GABRA1

    Interaction Score: 0.32

    Interaction Types & Directionality:
    positive modulator (activating)
    potentiator

    Interaction Info:
    Direct Interaction yes
    Mechanism of Interaction GABA-A receptor; anion channel positive allosteric modulator
    Trial Name -

    PMIDs:
    15240758 14579514 11744750 11264449 11752352 17139284 10209232 11605100 17016423 10487207 16866778


    Sources:
    TEND TdgClinicalTrial TTD DrugBank ChemblInteractions

  • ETOMIDATE   GABRA1

    Interaction Score: 0.31

    Interaction Types & Directionality:
    positive modulator (activating)
    agonist (activating)

    Interaction Info:
    Novel drug target Established target
    Trial Name -
    Mechanism of Interaction GABA-A receptor; anion channel positive modulator

    PMIDs:
    19809285 16884293 20704351 11752352 17139284 17016423 19741491


    Sources:
    TEND DTC TdgClinicalTrial DrugBank ChemblInteractions

  • AMOBARBITAL   GABRA1

    Interaction Score: 0.31

    Interaction Types & Directionality:
    potentiator

    Interaction Info:

    PMIDs:
    14579514 11264449 11752352 10209232 10487207


    Sources:
    TTD DrugBank

  • THIOCOLCHICOSIDE   GABRA1

    Interaction Score: 0.29

    Interaction Types & Directionality:
    antagonist (inhibitory)

    Interaction Info:

    PMIDs:
    16806306 17234181


    Sources:
    TTD DrugBank

  • THIOPENTAL   GABRA1

    Interaction Score: 0.29

    Interaction Types & Directionality:
    potentiator

    Interaction Info:
    Novel drug target Established target
    Trial Name -

    PMIDs:
    14579514 11264449 10209232 10487207 18619475


    Sources:
    TEND TdgClinicalTrial DrugBank

  • BUTALBITAL   GABRA1

    Interaction Score: 0.29

    Interaction Types & Directionality:
    positive modulator (activating)
    potentiator

    Interaction Info:
    Mechanism of Interaction GABA-A receptor; anion channel positive allosteric modulator
    Direct Interaction yes
    Trial Name -

    PMIDs:
    14579514 11264449 11752352 17139284 10209232 17016423 10487207 11279945


    Sources:
    TEND TdgClinicalTrial TTD DrugBank ChemblInteractions

  • BARBITAL   GABRA1

    Interaction Score: 0.26

    Interaction Types & Directionality:
    potentiator

    Interaction Info:

    PMIDs:
    14579514 11264449 10209232 10487207


    Sources:
    TTD DrugBank

  • CARISOPRODOL   GABRA1

    Interaction Score: 0.25

    Interaction Types & Directionality:
    activator (activating)
    modulator

    Interaction Info:

    PMIDs:
    20419052 26872987 19244096


    Sources:
    DrugBank

  • METHYPRYLON   GABRA1

    Interaction Score: 0.25

    Interaction Types & Directionality:
    positive modulator (activating)
    agonist (activating)

    Interaction Info:
    Direct Interaction yes
    Mechanism of Interaction GABA-A receptor; anion channel positive allosteric modulator
    Trial Name -

    PMIDs:
    11752352 17139284 1352660 17016423


    Sources:
    TEND TdgClinicalTrial TTD DrugBank ChemblInteractions

  • METHARBITAL   GABRA1

    Interaction Score: 0.24

    Interaction Types & Directionality:
    positive modulator (activating)
    potentiator

    Interaction Info:
    Direct Interaction yes
    Mechanism of Interaction GABA-A receptor; anion channel positive allosteric modulator
    Trial Name -

    PMIDs:
    14579514 11264449 11752352 17139284 10209232 17016423 10487207


    Sources:
    TEND TdgClinicalTrial DrugBank ChemblInteractions

  • QUAZEPAM   GABRA1

    Interaction Score: 0.24

    Interaction Types & Directionality:
    ligand
    positive modulator (activating)
    potentiator

    Interaction Info:
    Direct Interaction yes
    Mechanism of Interaction GABA-A receptor; anion channel positive allosteric modulator
    Trial Name -

    PMIDs:
    3017690 11752352 17139284 2892106 17016423 29950725 23038269


    Sources:
    TEND TdgClinicalTrial DrugBank ChemblInteractions

  • TALBUTAL   GABRA1

    Interaction Score: 0.24

    Interaction Types & Directionality:
    positive modulator (activating)
    potentiator

    Interaction Info:
    Direct Interaction yes
    Mechanism of Interaction GABA-A receptor; anion channel positive allosteric modulator
    Trial Name -

    PMIDs:
    14579514 11264449 11752352 17139284 10209232 17016423 10487207


    Sources:
    TEND TdgClinicalTrial DrugBank ChemblInteractions

  • HALAZEPAM   GABRA1

    Interaction Score: 0.24

    Interaction Types & Directionality:
    ligand
    positive modulator (activating)
    potentiator

    Interaction Info:
    Mechanism of Interaction GABA-A receptor; anion channel positive allosteric modulator
    Direct Interaction yes
    Trial Name -

    PMIDs:
    6738302 2867566 11752352 17139284 17016423 29950725 23038269


    Sources:
    TEND TdgClinicalTrial DrugBank ChemblInteractions

  • NITRAZEPAM   GABRA1

    Interaction Score: 0.23

    Interaction Types & Directionality:
    ligand
    positive modulator (activating)
    potentiator

    Interaction Info:
    Trial Name -
    Novel drug target Established target

    PMIDs:
    10877119 18384456 11752090 18603831 11752352 29950725 23038269


    Sources:
    TEND TdgClinicalTrial TTD DrugBank

  • STIRIPENTOL   GABRA1

    Interaction Score: 0.22

    Interaction Types & Directionality:
    positive modulator (activating)
    agonist (activating)

    Interaction Info:

    PMIDs:
    18585399


    Sources:
    DrugBank

  • BENZODIAZEPINE   GABRA1

    Interaction Score: 0.22

    Interaction Types & Directionality:
    ligand
    positive modulator (activating)

    Interaction Info:

    PMIDs:
    29950725 23038269


    Sources:
    DrugBank

  • CHEMBL2170369   GABRA1

    Interaction Score: 0.22

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    21751815


    Sources:
    DTC

  • APROBARBITAL   GABRA1

    Interaction Score: 0.22

    Interaction Types & Directionality:
    potentiator

    Interaction Info:

    PMIDs:
    14579514 11264449 10209232 10487207


    Sources:
    DrugBank

  • ISONIPECOTIC ACID   GABRA1

    Interaction Score: 0.22

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    25038482


    Sources:
    DTC

  • HEPTABARBITAL   GABRA1

    Interaction Score: 0.22

    Interaction Types & Directionality:
    potentiator

    Interaction Info:

    PMIDs:
    14579514 11264449 10209232 10487207


    Sources:
    DrugBank

  • PRAZEPAM   GABRA1

    Interaction Score: 0.2

    Interaction Types & Directionality:
    ligand
    positive modulator (activating)
    potentiator

    Interaction Info:
    Mechanism of Interaction GABA-A receptor; anion channel positive allosteric modulator
    Direct Interaction yes
    Trial Name -

    PMIDs:
    9145922 11752352 17139284 17016423 29950725 23038269


    Sources:
    TEND TdgClinicalTrial DrugBank ChemblInteractions

  • FLUNITRAZEPAM   GABRA1

    Interaction Score: 0.2

    Interaction Types & Directionality:
    ligand
    positive modulator (activating)
    allosteric modulator

    Interaction Info:
    Specific Binding Site for Interaction benzodiazepine site
    Details of the Assay for Interaction Assay using recombinant GABA<sub>A</sub> channels with subunit composition; &alpha;1&beta;3&gamma;2.
    Specific Action of the Ligand Positive

    PMIDs:
    29950725 23038269


    Sources:
    DrugBank GuideToPharmacology

  • ESZOPICLONE   GABRA1

    Interaction Score: 0.2

    Interaction Types & Directionality:
    positive modulator (activating)
    potentiator

    Interaction Info:
    Direct Interaction yes
    Mechanism of Interaction GABA-A receptor; anion channel positive allosteric modulator
    Trial Name Lunesta

    PMIDs:
    25817320 18973287 19698408 8241608 19942638


    Sources:
    TdgClinicalTrial DrugBank ChemblInteractions

  • MEPROBAMATE   GABRA1

    Interaction Score: 0.2

    Interaction Types & Directionality:
    positive modulator (activating)
    agonist (activating)

    Interaction Info:
    Direct Interaction yes
    Mechanism of Interaction GABA-A receptor; anion channel agonist
    Trial Name -

    PMIDs:
    9067327 11752352 19244096


    Sources:
    TEND TdgClinicalTrial TTD DrugBank ChemblInteractions

  • PICROTOXIN   GABRA1

    Interaction Score: 0.19

    Interaction Types & Directionality:
    antagonist (inhibitory)
    blocker (inhibitory)

    Interaction Info:
    Direct Interaction? True
    Endogenous Drug? False
    Specific Action of the Ligand None

    PMIDs:
    20491873 18446586 11752352 17139284 17016423


    Sources:
    TEND TdgClinicalTrial TTD DrugBank GuideToPharmacology

  • BICUCULLINE   GABRA1

    Interaction Score: 0.19

    Interaction Types & Directionality:
    antagonist (inhibitory)

    Interaction Info:
    Specific Binding Site for Interaction GABA site
    Specific Action of the Ligand Antagonist
    Endogenous Drug? False

    PMIDs:
    17875639


    Sources:
    DTC GuideToPharmacology

  • FLUMAZENIL   GABRA1

    Interaction Score: 0.19

    Interaction Types & Directionality:
    positive modulator (activating)
    allosteric modulator
    antagonist (inhibitory)

    Interaction Info:
    Specific Binding Site for Interaction benzodiazepine site
    Details of the Assay for Interaction Affinity measured using &alpha;1&beta;3&gamma;2 receptors.
    Specific Action of the Ligand Antagonist

    PMIDs:
    8693922 11864636 17016423


    Sources:
    TEND TdgClinicalTrial DrugBank GuideToPharmacology ChemblInteractions

  • CLOTIAZEPAM   GABRA1

    Interaction Score: 0.18

    Interaction Types & Directionality:
    ligand
    positive modulator (activating)
    potentiator

    Interaction Info:
    Trial Name -
    Novel drug target Established target

    PMIDs:
    18855614 29950725 23038269 18604239


    Sources:
    TEND TdgClinicalTrial DrugBank

  • ADINAZOLAM   GABRA1

    Interaction Score: 0.18

    Interaction Types & Directionality:
    ligand
    positive modulator (activating)
    potentiator

    Interaction Info:
    Novel drug target Established target
    Trial Name -

    PMIDs:
    6148400 6320036 29950725 23038269


    Sources:
    TEND TdgClinicalTrial DrugBank

  • PRIMIDONE   GABRA1

    Interaction Score: 0.18

    Interaction Types & Directionality:
    positive modulator (activating)
    potentiator

    Interaction Info:
    Mechanism of Interaction GABA-A receptor; anion channel positive allosteric modulator
    Direct Interaction yes
    Trial Name -

    PMIDs:
    14579514 24385718 11264449 11752352 17139284 10209232 17016423 10487207


    Sources:
    TEND TdgClinicalTrial TTD DrugBank ChemblInteractions

  • BREXANOLONE   GABRA1

    Interaction Score: 0.18

    Interaction Types & Directionality:
    positive modulator (activating)

    Interaction Info:

    PMIDs:
    None found


    Sources:
    TTD DrugBank

  • ACAMPROSATE   GABRA1

    Interaction Score: 0.18

    Interaction Types & Directionality:
    positive modulator (activating)

    Interaction Info:

    PMIDs:
    16300039


    Sources:
    DrugBank

  • CLOBAZAM   GABRA1

    Interaction Score: 0.17

    Interaction Types & Directionality:
    ligand
    positive modulator (activating)

    Interaction Info:
    Novel drug target Established target
    Trial Name Clobazam
    Mechanism of Interaction GABA-A receptor; anion channel positive allosteric modulator

    PMIDs:
    18384456 11752090 29950725 23038269


    Sources:
    TEND TdgClinicalTrial DrugBank ChemblInteractions

  • CLONAZEPAM   GABRA1

    Interaction Score: 0.17

    Interaction Types & Directionality:
    ligand
    positive modulator (activating)
    allosteric modulator

    Interaction Info:
    Trial Name JZP-8
    Novel drug target Established target
    Details of the Assay for Interaction Assay using recombinant GABA<sub>A</sub> channels with subunit composition; &alpha;1&beta;1&gamma;2.

    PMIDs:
    18384456 11752090 29950725 23038269


    Sources:
    TEND TdgClinicalTrial DrugBank GuideToPharmacology ChemblInteractions

  • TEMAZEPAM   GABRA1

    Interaction Score: 0.16

    Interaction Types & Directionality:
    ligand
    positive modulator (activating)
    potentiator

    Interaction Info:
    Novel drug target Established target
    Trial Name -
    Mechanism of Interaction GABA-A receptor; anion channel positive allosteric modulator

    PMIDs:
    18384456 20138190 29950725 23038269


    Sources:
    TEND TdgClinicalTrial DrugBank ChemblInteractions

  • CINOLAZEPAM   GABRA1

    Interaction Score: 0.16

    Interaction Types & Directionality:
    ligand
    positive modulator (activating)
    potentiator

    Interaction Info:
    Trial Name -
    Novel drug target Established target

    PMIDs:
    9145922 29950725 23038269


    Sources:
    TEND TdgClinicalTrial DrugBank

  • ESTAZOLAM   GABRA1

    Interaction Score: 0.15

    Interaction Types & Directionality:
    ligand
    positive modulator (activating)
    potentiator

    Interaction Info:
    Trial Name -
    Novel drug target Established target
    Mechanism of Interaction GABA-A receptor; anion channel positive allosteric modulator

    PMIDs:
    639854 2889803 29950725 23038269


    Sources:
    TEND TdgClinicalTrial DrugBank ChemblInteractions

  • METHOXYFLURANE   GABRA1

    Interaction Score: 0.15

    Interaction Types & Directionality:
    positive modulator (activating)
    agonist (activating)

    Interaction Info:
    Mechanism of Interaction GABA-A receptor; anion channel positive modulator
    Direct Interaction yes

    PMIDs:
    2845216 11752352 17139284 17016423 2459308 10683198


    Sources:
    TTD DrugBank ChemblInteractions

  • TAURINE   GABRA1

    Interaction Score: 0.15

    Interaction Types & Directionality:
    agonist (activating)

    Interaction Info:

    PMIDs:
    29123472


    Sources:
    DrugBank

  • ZOLPIDEM TARTRATE   GABRA1

    Interaction Score: 0.15

    Interaction Types & Directionality:
    positive modulator (activating)

    Interaction Info:
    Mechanism of Interaction GABA A receptor alpha-1/beta-1/gamma-2 positive allosteric modulator
    Direct Interaction yes

    PMIDs:
    None found


    Sources:
    ChemblInteractions

  • BUTABARBITAL   GABRA1

    Interaction Score: 0.15

    Interaction Types & Directionality:
    positive modulator (activating)

    Interaction Info:
    Novel drug target Established target
    Trial Name -

    PMIDs:
    11264449 10209232


    Sources:
    TEND TdgClinicalTrial TTD DrugBank

  • DIAZEPAM   GABRA1

    Interaction Score: 0.15

    Interaction Types & Directionality:
    ligand
    positive modulator (activating)
    allosteric modulator
    potentiator

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

    PMIDs:
    18384456 11752090 15009644 29950725 23038269


    Sources:
    TEND TdgClinicalTrial DrugBank GuideToPharmacology ChemblInteractions

  • FLURAZEPAM   GABRA1

    Interaction Score: 0.15

    Interaction Types & Directionality:
    ligand
    positive modulator (activating)
    potentiator

    Interaction Info:
    Trial Name -
    Novel drug target Established target

    PMIDs:
    18384456 11752090 29950725 23038269


    Sources:
    TEND TdgClinicalTrial DrugBank

  • CHLORDIAZEPOXIDE   GABRA1

    Interaction Score: 0.15

    Interaction Types & Directionality:
    ligand
    positive modulator (activating)

    Interaction Info:
    Trial Name -
    Novel drug target Established target
    Direct Interaction yes

    PMIDs:
    6135616 29950725 23038269


    Sources:
    TEND TdgClinicalTrial DrugBank ChemblInteractions

  • OXAZEPAM   GABRA1

    Interaction Score: 0.14

    Interaction Types & Directionality:
    ligand
    positive modulator (activating)
    potentiator

    Interaction Info:
    Mechanism of Interaction GABA-A receptor; anion channel positive allosteric modulator
    Direct Interaction yes
    Trial Name -

    PMIDs:
    18384456 11752090 29950725 23038269


    Sources:
    TEND TdgClinicalTrial DrugBank ChemblInteractions

  • LORAZEPAM   GABRA1

    Interaction Score: 0.13

    Interaction Types & Directionality:
    ligand
    positive modulator (activating)

    Interaction Info:
    Mechanism of Interaction GABA-A receptor; anion channel positive allosteric modulator
    Direct Interaction yes
    Trial Name -

    PMIDs:
    18384456 29950725 23038269


    Sources:
    TEND TdgClinicalTrial DrugBank ChemblInteractions

  • TRIAZOLAM   GABRA1

    Interaction Score: 0.13

    Interaction Types & Directionality:
    ligand
    positive modulator (activating)
    allosteric modulator
    potentiator

    Interaction Info:
    Mechanism of Interaction GABA-A receptor; anion channel positive allosteric modulator
    Direct Interaction yes
    Trial Name ARX-03, sufentanil + triazolam NanoTab

    PMIDs:
    18384456 11752090 29950725 23038269


    Sources:
    TEND TdgClinicalTrial DrugBank GuideToPharmacology ChemblInteractions

  • ALPRAZOLAM   GABRA1

    Interaction Score: 0.13

    Interaction Types & Directionality:
    ligand
    positive modulator (activating)
    allosteric modulator

    Interaction Info:
    Direct Interaction yes
    Mechanism of Interaction GABA-A receptor; anion channel positive allosteric modulator
    Specific Binding Site for Interaction benzodiazepine site

    PMIDs:
    14978513 18384456 29950725 23038269


    Sources:
    TEND TdgClinicalTrial DrugBank GuideToPharmacology ChemblInteractions

  • BROMAZEPAM   GABRA1

    Interaction Score: 0.13

    Interaction Types & Directionality:
    ligand
    positive modulator (activating)
    potentiator

    Interaction Info:
    Trial Name -
    Novel drug target Established target

    PMIDs:
    18384456 29950725 23038269


    Sources:
    TEND TdgClinicalTrial DrugBank

  • MUSCIMOL   GABRA1

    Interaction Score: 0.12

    Interaction Types & Directionality:
    agonist (activating)

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

    PMIDs:
    22029276


    Sources:
    DrugBank GuideToPharmacology

  • PHENOBARBITAL   GABRA1

    Interaction Score: 0.12

    Interaction Types & Directionality:
    potentiator

    Interaction Info:
    Trial Name -
    Novel drug target Established target

    PMIDs:
    14579514 11264449 2871724 17139284 10209232 17016423 10487207


    Sources:
    TEND TdgClinicalTrial DrugBank

  • MK-0777   GABRA1

    Interaction Score: 0.11

    Interaction Types & Directionality:
    allosteric modulator

    Interaction Info:
    Specific Binding Site for Interaction benzodiazepine site
    Specific Action of the Ligand Antagonist
    Endogenous Drug? False

    PMIDs:
    None found


    Sources:
    GuideToPharmacology

  • CHEMBL1518572   GABRA1

    Interaction Score: 0.11

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    TTD

  • ETHCHLORVYNOL   GABRA1

    Interaction Score: 0.11

    Interaction Types & Directionality:
    positive modulator (activating)

    Interaction Info:
    Mechanism of Interaction GABA-A receptor; anion channel positive modulator
    Direct Interaction yes

    PMIDs:
    1585214


    Sources:
    TTD DrugBank ChemblInteractions

  • ISOFLURANE   GABRA1

    Interaction Score: 0.11

    Interaction Types & Directionality:
    positive modulator (activating)
    agonist (activating)

    Interaction Info:
    Trial Name -
    Novel drug target Established target
    Mechanism of Interaction GABA-A receptor; anion channel positive allosteric modulator

    PMIDs:
    20826568 20097266 17139284 17016423


    Sources:
    TEND TdgClinicalTrial DrugBank ChemblInteractions

  • FLUDIAZEPAM   GABRA1

    Interaction Score: 0.1

    Interaction Types & Directionality:
    potentiator

    Interaction Info:
    Trial Name -
    Novel drug target Established target

    PMIDs:
    2857046


    Sources:
    TEND TdgClinicalTrial DrugBank

  • GANAXOLONE   GABRA1

    Interaction Score: 0.1

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    Trial Name Ganaxolone
    Novel drug target Established target

    PMIDs:
    None found


    Sources:
    TdgClinicalTrial DrugBank

  • TOPIRAMATE   GABRA1

    Interaction Score: 0.1

    Interaction Types & Directionality:
    positive modulator (activating)
    agonist (activating)

    Interaction Info:
    Mechanism of Interaction GABA-A receptor; anion channel positive modulator
    Direct Interaction yes
    Trial Name topiramate controlled release,Trokesa

    PMIDs:
    19998575 25101297 10768303 17139284 17016423 19417176


    Sources:
    TEND TdgClinicalTrial DrugBank ChemblInteractions

  • SEVOFLURANE   GABRA1

    Interaction Score: 0.09

    Interaction Types & Directionality:
    positive modulator (activating)
    agonist (activating)

    Interaction Info:
    Mechanism of Interaction GABA-A receptor; anion channel positive allosteric modulator
    Direct Interaction yes
    Trial Name -

    PMIDs:
    17139284 17016423 7509043


    Sources:
    TEND TdgClinicalTrial DrugBank ChemblInteractions

  • ENFLURANE   GABRA1

    Interaction Score: 0.09

    Interaction Types & Directionality:
    positive modulator (activating)
    potentiator

    Interaction Info:
    Trial Name -
    Novel drug target Established target
    Mechanism of Interaction GABA-A receptor; anion channel positive modulator

    PMIDs:
    16973644 16402123 11465594


    Sources:
    TEND TdgClinicalTrial DrugBank ChemblInteractions

  • MEMANTINE   GABRA1

    Interaction Score: 0.09

    Interaction Types & Directionality:
    binder

    Interaction Info:

    PMIDs:
    19236854


    Sources:
    DrugBank

  • DESFLURANE   GABRA1

    Interaction Score: 0.09

    Interaction Types & Directionality:
    positive modulator (activating)

    Interaction Info:
    Trial Name -
    Novel drug target Established target
    Mechanism of Interaction GABA-A receptor; anion channel positive allosteric modulator

    PMIDs:
    18384456 11752090


    Sources:
    TEND TdgClinicalTrial DrugBank ChemblInteractions

  • CLORAZEPIC ACID   GABRA1

    Interaction Score: 0.09

    Interaction Types & Directionality:
    positive modulator (activating)

    Interaction Info:
    Trial Name -
    Novel drug target Established target

    PMIDs:
    18384456 11752090


    Sources:
    TEND TdgClinicalTrial

  • MIDAZOLAM   GABRA1

    Interaction Score: 0.08

    Interaction Types & Directionality:
    ligand
    positive modulator (activating)
    potentiator

    Interaction Info:
    Trial Name -
    Novel drug target Established target

    PMIDs:
    18384456 11752090 29950725 23038269


    Sources:
    TEND TdgClinicalTrial DrugBank

  • GABOXADOL   GABRA1

    Interaction Score: 0.08

    Interaction Types & Directionality:
    agonist (activating)

    Interaction Info:
    Mechanism of Interaction GABA-A receptor; agonist GABA site agonist
    Direct Interaction yes
    Specific Binding Site for Interaction GABA site

    PMIDs:
    None found


    Sources:
    TdgClinicalTrial GuideToPharmacology ChemblInteractions

  • GLUTETHIMIDE   GABRA1

    Interaction Score: 0.08

    Interaction Types & Directionality:
    positive modulator (activating)
    agonist (activating)

    Interaction Info:
    Mechanism of Interaction GABA-A receptor; anion channel positive modulator
    Direct Interaction yes

    PMIDs:
    6318143


    Sources:
    DrugBank ChemblInteractions

  • CLOMETHIAZOLE   GABRA1

    Interaction Score: 0.07

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    DrugBank

  • BRETAZENIL   GABRA1

    Interaction Score: 0.07

    Interaction Types & Directionality:
    allosteric modulator

    Interaction Info:
    Specific Binding Site for Interaction benzodiazepine site
    Specific Action of the Ligand Full agonist
    Endogenous Drug? False

    PMIDs:
    None found


    Sources:
    GuideToPharmacology

  • ADIPIPLON   GABRA1

    Interaction Score: 0.07

    Interaction Types & Directionality:
    partial agonist (activating)

    Interaction Info:
    Trial Name NG2-73
    Novel drug target Established target
    Direct Interaction yes

    PMIDs:
    None found


    Sources:
    TdgClinicalTrial DrugBank ChemblInteractions

  • HALOTHANE   GABRA1

    Interaction Score: 0.06

    Interaction Types & Directionality:
    positive modulator (activating)
    other/unknown

    Interaction Info:
    Mechanism of Interaction GABA-A receptor; anion channel positive allosteric modulator
    Direct Interaction yes

    PMIDs:
    11897112 12960553 17139284 17016423


    Sources:
    DrugBank ChemblInteractions

  • AZIETOMIDATE   GABRA1

    Interaction Score: 0.06

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    16884293


    Sources:
    DTC

  • LAMOTRIGINE   GABRA1

    Interaction Score: 0.05

    Interaction Types & Directionality:
    antagonist (inhibitory)
    inducer (activating)
    inhibitor (inhibitory)

    Interaction Info:

    PMIDs:
    8941036 22306746 11955522 11927166


    Sources:
    DrugBank

  • RESEQUINIL   GABRA1

    Interaction Score: 0.05

    Interaction Types & Directionality:
    inverse agonist (inhibitory)

    Interaction Info:
    Mechanism of Interaction GABA-A receptor; benzodiazepine site inverse agonist
    Direct Interaction yes

    PMIDs:
    None found


    Sources:
    ChemblInteractions

  • OCINAPLON   GABRA1

    Interaction Score: 0.05

    Interaction Types & Directionality:
    allosteric modulator

    Interaction Info:
    Trial Name ocinaplon
    Novel drug target Established target
    Specific Binding Site for Interaction benzodiazepine site

    PMIDs:
    None found


    Sources:
    TdgClinicalTrial GuideToPharmacology

  • LOREDIPLON   GABRA1

    Interaction Score: 0.05

    Interaction Types & Directionality:
    positive modulator (activating)

    Interaction Info:
    Direct Interaction yes
    Mechanism of Interaction GABA-A receptor; benzodiazepine site positive allosteric modulator

    PMIDs:
    None found


    Sources:
    ChemblInteractions

  • GABAZINE   GABRA1

    Interaction Score: 0.05

    Interaction Types & Directionality:
    antagonist (inhibitory)

    Interaction Info:
    Specific Binding Site for Interaction GABA site
    Specific Action of the Ligand Antagonist
    Endogenous Drug? False

    PMIDs:
    None found


    Sources:
    GuideToPharmacology

  • ISOGUVACINE   GABRA1

    Interaction Score: 0.05

    Interaction Types & Directionality:
    agonist (activating)

    Interaction Info:
    Specific Binding Site for Interaction GABA site
    Specific Action of the Ligand Full agonist
    Endogenous Drug? False

    PMIDs:
    None found


    Sources:
    GuideToPharmacology

  • AMOXAPINE   GABRA1

    Interaction Score: 0.05

    Interaction Types & Directionality:
    binder
    antagonist (inhibitory)

    Interaction Info:

    PMIDs:
    9589848 1966571


    Sources:
    DrugBank

  • PRASTERONE   GABRA1

    Interaction Score: 0.03

    Interaction Types & Directionality:
    antagonist (inhibitory)

    Interaction Info:

    PMIDs:
    9262347


    Sources:
    DrugBank

  • PHENYTOIN   GABRA1

    Interaction Score: 0.03

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    28349209


    Sources:
    PharmGKB DrugBank

  • PROPOFOL   GABRA1

    Interaction Score: 0.03

    Interaction Types & Directionality:
    positive modulator (activating)

    Interaction Info:
    Mechanism of Interaction GABA-A receptor; anion channel positive allosteric modulator
    Direct Interaction yes

    PMIDs:
    None found


    Sources:
    DrugBank ChemblInteractions

  • TRICLOFOS SODIUM   GABRA1

    Interaction Score: 0.03

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    Mechanism of Interaction GABA-A receptor; anion channel positive modulator
    Direct Interaction yes

    PMIDs:
    None found


    Sources:
    ChemblInteractions

  • CLORAZEPATE DIPOTASSIUM   GABRA1

    Interaction Score: 0.03

    Interaction Types & Directionality:
    positive modulator (activating)

    Interaction Info:
    Mechanism of Interaction GABA-A receptor; anion channel positive allosteric modulator
    Direct Interaction yes

    PMIDs:
    None found


    Sources:
    ChemblInteractions

  • METHOHEXITAL SODIUM   GABRA1

    Interaction Score: 0.03

    Interaction Types & Directionality:
    positive modulator (activating)

    Interaction Info:
    Mechanism of Interaction GABA-A receptor; anion channel positive allosteric modulator
    Direct Interaction yes

    PMIDs:
    None found


    Sources:
    ChemblInteractions

  • PENTOBARBITAL SODIUM   GABRA1

    Interaction Score: 0.03

    Interaction Types & Directionality:
    positive modulator (activating)

    Interaction Info:
    Mechanism of Interaction GABA-A receptor; anion channel positive allosteric modulator
    Direct Interaction yes

    PMIDs:
    None found


    Sources:
    ChemblInteractions

  • BUTABARBITAL SODIUM   GABRA1

    Interaction Score: 0.03

    Interaction Types & Directionality:
    positive modulator (activating)

    Interaction Info:
    Mechanism of Interaction GABA-A receptor; anion channel positive allosteric modulator
    Direct Interaction yes

    PMIDs:
    None found


    Sources:
    ChemblInteractions

  • SECOBARBITAL SODIUM   GABRA1

    Interaction Score: 0.03

    Interaction Types & Directionality:
    positive modulator (activating)

    Interaction Info:
    Mechanism of Interaction GABA-A receptor; anion channel positive allosteric modulator
    Direct Interaction yes

    PMIDs:
    None found


    Sources:
    ChemblInteractions

  • PF-06372865   GABRA1

    Interaction Score: 0.03

    Interaction Types & Directionality:
    agonist (activating)

    Interaction Info:
    Mechanism of Interaction GABA-A receptor; anion channel agonist
    Direct Interaction yes

    PMIDs:
    None found


    Sources:
    ChemblInteractions

  • CHLORDIAZEPOXIDE HYDROCHLORIDE   GABRA1

    Interaction Score: 0.03

    Interaction Types & Directionality:
    positive modulator (activating)

    Interaction Info:
    Direct Interaction yes
    Mechanism of Interaction GABA-A receptor; anion channel positive allosteric modulator

    PMIDs:
    None found


    Sources:
    ChemblInteractions

  • ALCOHOL   GABRA1

    Interaction Score: 0.03

    Interaction Types & Directionality:
    agonist (activating)

    Interaction Info:

    PMIDs:
    17591544 12921221 11752352 17139284 17016423 21262851


    Sources:
    TTD DrugBank

  • THIOPENTAL SODIUM   GABRA1

    Interaction Score: 0.03

    Interaction Types & Directionality:
    positive modulator (activating)

    Interaction Info:
    Mechanism of Interaction GABA-A receptor; anion channel positive allosteric modulator
    Direct Interaction yes

    PMIDs:
    None found


    Sources:
    ChemblInteractions

  • MIDAZOLAM HYDROCHLORIDE   GABRA1

    Interaction Score: 0.03

    Interaction Types & Directionality:
    positive modulator (activating)

    Interaction Info:
    Direct Interaction yes
    Mechanism of Interaction GABA-A receptor; anion channel positive allosteric modulator

    PMIDs:
    None found


    Sources:
    ChemblInteractions

  • THIAMYLAL SODIUM   GABRA1

    Interaction Score: 0.03

    Interaction Types & Directionality:
    positive modulator (activating)

    Interaction Info:
    Mechanism of Interaction GABA-A receptor; anion channel positive allosteric modulator
    Direct Interaction yes

    PMIDs:
    None found


    Sources:
    ChemblInteractions

  • REMIMAZOLAM   GABRA1

    Interaction Score: 0.02

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    Trial Name CNS-7056
    Novel drug target Established target

    PMIDs:
    None found


    Sources:
    TdgClinicalTrial

  • OLANZAPINE   GABRA1

    Interaction Score: 0.02

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:

    PMIDs:
    8822531 25032030


    Sources:
    DrugBank

  • ACAMPROSATE CALCIUM   GABRA1

    Interaction Score: 0.02

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    Mechanism of Interaction GABA-A receptor; anion channel positive modulator
    Direct Interaction yes

    PMIDs:
    None found


    Sources:
    ChemblInteractions

  • CARBAMAZEPINE   GABRA1

    Interaction Score: 0.02

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    22591328


    Sources:
    PharmGKB

  • Ensembl: ENSG00000022355

    • Version: 101_38

    Alternate Names:
    GABRA1 Ensembl Gene Name

    Gene Info:
    Gene Biotype PROTEIN_CODING

    Publications:

  • RussLampel: ENSG00000022355

    • Version: 26-July-2011

    Alternate Names:
    GAMMA-AMINOBUTYRIC-ACID RECEPTOR ALPHA-1 SUBUNIT PRECURSOR (GABA(A) RECEPTOR). [SOURCE:UNIPROT/SWISSPROT;ACC:P14867] Description
    GABRA1 Display Id
    ENSG00000022355 Ensembl Gene Id

    Gene Info:
    Human Readable Name DRUGGABLE GENOME

    Gene Categories:
    DRUGGABLE GENOME

    Publications:

  • TEND: P14867

    • Version: 01-August-2011

    Alternate Names:
    2554 Entrez Gene Id
    GBRA1_HUMAN Uniprot Id
    ENSG00000022355 Ensembl Gene Id

    Gene Info:
    Target Subclass Channels
    Target Subclass Ligand_gated_ion_channels
    Target Subclass cys-loop

    Publications:

  • HopkinsGroom: P14867

    • Version: 11-September-2012

    Alternate Names:
    ENSG00000022355 Ensembl Gene Id
    GAMMA-AMINOBUTYRIC ACID RECEPTOR SUBUNIT ALPHA-1 Uniprot Protein Name
    2554 Entrez Gene Id

    Gene Info:
    Human Readable Name ION CHANNEL
    Interpro Short Name Neur_chan_lig-bd
    Human Readable Name DRUGGABLE GENOME

    Gene Categories:
    ION CHANNEL, DRUGGABLE GENOME

    Publications:

  • TdgClinicalTrial: P14867

    • Version: January-2014

    Alternate Names:
    GABRA1 Gene Symbol
    GABRD Gene Symbol

    Gene Info:
    Target Class Receptors
    Target Subclass TC:1.A.9

    Publications:

  • GuideToPharmacology: 2554

    • Version: 29-September-2020

    Alternate Names:
    4075 HUGO Gene ID
    4075 HUGO Gene Symbol
    gamma-aminobutyric acid type A receptor subunit alpha1 HUGO Gene Name

    Gene Info:
    GuideToPharmacology Gene Category Name GABA<sub>A</sub> receptors
    GuideToPharmacology Gene Category ID 72

    Gene Categories:
    ION CHANNEL

    Publications:

  • PharmGKB: GABRA1

    • Version: 18-August-2020

    Alternate Names:
    PA28489 PharmGKB ID

    Gene Info:

    Publications:
    Zhou BT et al., 2012, Effects of SCN1A and GABA receptor genetic polymorphisms on carbamazepine tolerability and efficacy in Chinese patients with partial seizures: 2-year longitudinal clinical follow-up., CNS Neurosci Ther

  • DrugBank: BE0000795

    • Version: 5.1.7

    Alternate Names:
    GABRA1 DrugBank Gene Name
    P14867 UniProt Accession
    2554 Entrez Gene Id

    Gene Info:

    Publications:
    Whiting, 2003, The GABAA receptor gene family: new opportunities for drug development., Curr Opin Drug Discov Devel
    Yamakura et al., 2001, Anesthetics and ion channels: molecular models and sites of action., Annu. Rev. Pharmacol. Toxicol.
    Chen et al., 2002, TTD: Therapeutic Target Database., Nucleic Acids Res.

  • DrugBank: BE0004797

    • Version: 5.1.7

    Alternate Names:
    GABRA1 DrugBank Gene Name
    P14867 UniProt Accession
    2554 Entrez Gene Id

    Gene Info:

    Publications:
    Riss et al., 2008, Benzodiazepines in epilepsy: pharmacology and pharmacokinetics., Acta Neurol. Scand.
    Zhu S et al., 2018, Structure of a human synaptic GABA<sub>A</sub> receptor., Nature
    Sigel E et al., 2012, Structure, function, and modulation of GABA(A) receptors., J Biol Chem

  • DrugBank: BE0008668

    • Version: 5.1.7

    Alternate Names:
    GABRA1 DrugBank Gene Name
    P14867 UniProt Accession
    2554 Entrez Gene Id

    Gene Info:

    Publications:
    Zhu S et al., 2018, Structure of a human synaptic GABA<sub>A</sub> receptor., Nature
    Sigel E et al., 2012, Structure, function, and modulation of GABA(A) receptors., J Biol Chem
    Brafford MV et al., 2014, Olanzapine: an antiemetic option for chemotherapy-induced nausea and vomiting., J Adv Pract Oncol

  • DTC: GABRA1

    • Version: 02-September-2020

    Alternate Names:

    Gene Info:

    Publications:
    Husain SS et al., 2006, Synthesis of trifluoromethylaryl diazirine and benzophenone derivatives of etomidate that are potent general anesthetics and effective photolabels for probing sites on ligand-gated ion channels., J Med Chem
    Anzini M et al., 2011, New insight into the central benzodiazepine receptor-ligand interactions: design, synthesis, biological evaluation, and molecular modeling of 3-substituted 6-phenyl-4H-imidazo[1,5-a][1,4]benzodiazepines and related compounds., J Med Chem
    Zaugg J et al., 2011, Identification and characterization of GABA(A) receptor modulatory diterpenes from Biota orientalis that decrease locomotor activity in mice., J Nat Prod

  • HingoraniCasas: ENSG00000022355

    • Version: 31-May-2017

    Alternate Names:
    ENSG00000022355 Gene Symbol
    GABRA1 Ensembl Id

    Gene Info:

    Gene Categories:
    DRUGGABLE GENOME

    Publications:

  • ChemblInteractions: GABRA1

    • Version: chembl_23

    Alternate Names:
    GABRA1 GENE_SYMBOL
    Gamma-aminobutyric acid receptor subunit alpha-1 UNIPROT
    GABA(A) receptor subunit alpha-1 UNIPROT

    Gene Info:

    Publications:

  • Pharos: GABRA1

    • Version: 03-September-2020

    Alternate Names:
    Gamma-aminobutyric acid receptor subunit alpha-1 Gene Name
    P14867 UniProt ID

    Gene Info:

    Gene Categories:
    ION CHANNEL

    Publications:

  • TTD: GABA(A) receptor alpha-1

    • Version: 2020.06.01

    Alternate Names:
    GABRA1 TTD Gene Abbreviation
    T51487 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