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GLRA1 Gene Record

  • Summary
  • Interactions
  • Claims
  • GLRA1 2741 Druggable Genome

    Alternate Names:

    2741
    GLYCINE RECEPTOR ALPHA 1
    GLRA1
    HKPX1
    STHE
    138491
    4326
    ENSG00000145888
    OTTHUMG00000130121
    GLYCINE RECEPTOR ALPHA-1 CHAIN PRECURSOR (GLYCINE RECEPTOR 48 KDA SUBUNIT) (STRYCHNINE BINDING SUBUNIT). [SOURCE:UNIPROT/SWISSPROT;ACC:P23415]
    BE0000433
    P23415
    GLRA1_HUMAN
    Glycine receptor strychnine-binding subunit
    Glycine receptor 48 kDa subunit
    Glycine receptor subunit alpha-1
    BE0004857
    glycine receptor α1 subunit
    Strychnine-binding glycine receptor
    T50269
    NP_000162
    NM_000171
    423
    BE0009666

    Gene Info:

    Human Readable Name DRUGGABLE GENOME
    Target Main Class Receptors
    Transmembrane Helix Count 3
    Target Subclass Channels
    Target Subclass Ligand_gated_ion_channels
    Target Subclass cys-loop
    Target Class Receptors
    Target Subclass TC:1.A.9.3.1
    Uniprot Status Swiss-Prot
    Interpro Type Family
    Human Readable Name ION CHANNEL
    Interpro Short Name Neur_channel
    Interpro Acc IPR006202
    Uniprot Evidence 1: Evidence at protein level
    Interpro Acc IPR006201
    Interpro Type Domain
    Interpro Short Name Neur_chan_lig-bd
    Interpro Name Neurotransmitter-gated ion-channel ligand-binding
    Interpro Name Neurotransmitter-gated ion-channel
    Gene Biotype PROTEIN_CODING
    GuideToPharmacology Gene Category Name Glycine receptors
    GuideToPharmacology Gene Category ID 73
    (11 More Sources)

    Gene Categories: Category Details

    ION CHANNEL
    EXTERNAL SIDE OF PLASMA MEMBRANE
    DRUGGABLE GENOME

    Publications:

    Overington et al., 2006, How many drug targets are there?, Nat Rev Drug Discov
    Imming et al., 2006, Drugs, their targets and the nature and number of drug targets., Nat Rev Drug Discov
    Franks NP et al., 1994, Molecular and cellular mechanisms of general anaesthesia., Nature
    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
    Ye et al., 1998, Enhancement of glycine receptor function by ethanol is inversely correlated with molecular volume at position alpha267., J. Biol. Chem.
    Fuentealba et al., Potentiation and inhibition of glycine receptors by tutin., Neuropharmacology
    Baenziger et al., 2011, 3D structure and allosteric modulation of the transmembrane domain of pentameric ligand-gated ion channels., Neuropharmacology
    Balansa W et al., 2010, Ircinialactams: subunit-selective glycine receptor modulators from Australian sponges of the family Irciniidae., Bioorg Med Chem
    Jensen AA et al., 2004, Functional characterisation of the human alpha1 glycine receptor in a fluorescence-based membrane potential assay., Biochem Pharmacol
    Schofield et al., 2004, Alanine-scanning mutagenesis in the signature disulfide loop of the glycine receptor alpha 1 subunit: critical residues for activation and modulation., Biochemistry
    Borghese CM, 2015, The molecular pharmacology of volatile anesthetics., Int Anesthesiol Clin
    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.
    Chen et al., 2002, TTD: Therapeutic Target Database., Nucleic Acids Res.
    Mascia et al., 2007, Thiocolchicoside inhibits the activity of various subtypes of recombinant GABA(A) receptors expressed in Xenopus laevis oocytes., Eur. J. Pharmacol.
    Vale et al., 2003, The organochlorine pesticides gamma-hexachlorocyclohexane (lindane), alpha-endosulfan and dieldrin differentially interact with GABA(A) and glycine-gated chloride channels in primary cultures of cerebellar granule cells., Neuroscience
    Heusinkveld et al., 2010, Dual actions of lindane (γ-hexachlorocyclohexane) on calcium homeostasis and exocytosis in rat PC12 cells., Toxicol. Appl. Pharmacol.
    Heinze et al., 2007, Diversity of glycine receptors in the mouse retina: localization of the alpha4 subunit., J. Comp. Neurol.
    Eulenburg et al., 2006, Mutations within the human GLYT2 (SLC6A5) gene associated with hyperekplexia., Biochem. Biophys. Res. Commun.
    Chen Z et al., 2006, Identification of residues critical for Cu2+-mediated inhibition of glycine alpha1 receptors., Neuropharmacology
    Limapichat W et al., 2013, Key binding interactions for memantine in the NMDA receptor., ACS Chem Neurosci
    Xia P et al., 2010, Memantine preferentially blocks extrasynaptic over synaptic NMDA receptor currents in hippocampal autapses., J Neurosci
    Ahrens J et al., 2009, The nonpsychotropic cannabinoid cannabidiol modulates and directly activates alpha-1 and alpha-1-Beta glycine receptor function., Pharmacology
    Ibeas Bih C et al., 2015, Molecular Targets of Cannabidiol in Neurological Disorders., Neurotherapeutics
    Bialer M et al., 2007, Progress report on new antiepileptic drugs: a summary of the Eigth Eilat Conference (EILAT VIII)., Epilepsy Res
  • CHEMBL464651   GLRA1

    Interaction Score: 3.44

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    20346682


    Sources:
    DTC

  • CHEMBL497392   GLRA1

    Interaction Score: 1.29

    Interaction Types & Directionality:
    antagonist (inhibitory)

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

    PMIDs:
    20346682


    Sources:
    DTC GuideToPharmacology

  • SELETRACETAM   GLRA1

    Interaction Score: 1.15

    Interaction Types & Directionality:
    binder

    Interaction Info:

    PMIDs:
    17158031


    Sources:
    DrugBank

  • THIOCOLCHICOSIDE   GLRA1

    Interaction Score: 0.86

    Interaction Types & Directionality:
    antagonist (inhibitory)

    Interaction Info:

    PMIDs:
    17234181


    Sources:
    TTD DrugBank

  • (D)-SERINE   GLRA1

    Interaction Score: 0.65

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    11752352


    Sources:
    TTD DrugBank

  • TAURINE   GLRA1

    Interaction Score: 0.57

    Interaction Types & Directionality:
    agonist (activating)

    Interaction Info:

    PMIDs:
    15081878


    Sources:
    DrugBank

  • BILOBALIDE   GLRA1

    Interaction Score: 0.57

    Interaction Types & Directionality:
    antagonist (inhibitory)

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

    PMIDs:
    None found


    Sources:
    GuideToPharmacology

  • MEMANTINE   GLRA1

    Interaction Score: 0.52

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:

    PMIDs:
    23421676 20720132


    Sources:
    DrugBank

  • LINDANE   GLRA1

    Interaction Score: 0.52

    Interaction Types & Directionality:
    antagonist (inhibitory)

    Interaction Info:

    PMIDs:
    12614680 20600211


    Sources:
    DrugBank

  • DEXANABINOL   GLRA1

    Interaction Score: 0.43

    Interaction Types & Directionality:
    allosteric modulator

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

    PMIDs:
    20346682


    Sources:
    DTC GuideToPharmacology

  • PICROTOXININ   GLRA1

    Interaction Score: 0.43

    Interaction Types & Directionality:
    blocker (inhibitory)

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

    PMIDs:
    None found


    Sources:
    GuideToPharmacology

  • PICROTIN   GLRA1

    Interaction Score: 0.43

    Interaction Types & Directionality:
    blocker (inhibitory)

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

    PMIDs:
    None found


    Sources:
    GuideToPharmacology

  • DESFLURANE   GLRA1

    Interaction Score: 0.4

    Interaction Types & Directionality:
    agonist (activating)

    Interaction Info:
    Trial Name -
    Novel drug target Established target
    Mechanism of Interaction Glycine receptor (alpha-1/beta) positive modulator

    PMIDs:
    16973644 17139284 17016423


    Sources:
    TEND TdgClinicalTrial DrugBank ChemblInteractions

  • ISOFLURANE   GLRA1

    Interaction Score: 0.37

    Interaction Types & Directionality:
    agonist (activating)

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

    PMIDs:
    16973644 17139284 17016423


    Sources:
    TEND TdgClinicalTrial DrugBank ChemblInteractions

  • ENFLURANE   GLRA1

    Interaction Score: 0.35

    Interaction Types & Directionality:
    agonist (activating)
    potentiator

    Interaction Info:
    Mechanism of Interaction Glycine receptor (alpha-1/beta) positive modulator
    Direct Interaction yes
    Trial Name -

    PMIDs:
    16973644 25807016 10683198


    Sources:
    TEND TdgClinicalTrial DrugBank ChemblInteractions

  • SEVOFLURANE   GLRA1

    Interaction Score: 0.35

    Interaction Types & Directionality:
    agonist (activating)

    Interaction Info:
    Trial Name -
    Novel drug target Established target
    Mechanism of Interaction Glycine receptor (alpha-1/beta) positive modulator

    PMIDs:
    17139284 17016423 7509043


    Sources:
    TEND TdgClinicalTrial DrugBank ChemblInteractions

  • METHOXYFLURANE   GLRA1

    Interaction Score: 0.33

    Interaction Types & Directionality:
    agonist (activating)

    Interaction Info:
    Mechanism of Interaction Glycine receptor (alpha-1/beta) agonist
    Direct Interaction yes

    PMIDs:
    17139284 17016423 10683198


    Sources:
    DrugBank ChemblInteractions

  • ATROPINE   GLRA1

    Interaction Score: 0.23

    Interaction Types & Directionality:
    antagonist (inhibitory)

    Interaction Info:

    PMIDs:
    15081878


    Sources:
    DrugBank

  • PICROTOXIN   GLRA1

    Interaction Score: 0.22

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

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

    PMIDs:
    15081878


    Sources:
    DrugBank GuideToPharmacology

  • HALOTHANE   GLRA1

    Interaction Score: 0.2

    Interaction Types & Directionality:
    allosteric modulator

    Interaction Info:
    Mechanism of Interaction Glycine receptor (alpha-1/beta) positive modulator
    Direct Interaction yes

    PMIDs:
    15287733 17139284 17016423


    Sources:
    DrugBank ChemblInteractions

  • WIN-552122   GLRA1

    Interaction Score: 0.19

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    20346682


    Sources:
    DTC

  • STRYCHNINE   GLRA1

    Interaction Score: 0.17

    Interaction Types & Directionality:
    antagonist (inhibitory)

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

    PMIDs:
    None found


    Sources:
    GuideToPharmacology

  • TROPISETRON   GLRA1

    Interaction Score: 0.17

    Interaction Types & Directionality:
    antagonist (inhibitory)

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

    PMIDs:
    None found


    Sources:
    GuideToPharmacology

  • GLYCINE   GLRA1

    Interaction Score: 0.16

    Interaction Types & Directionality:
    ligand

    Interaction Info:

    PMIDs:
    17154252 16884688


    Sources:
    DrugBank

  • CANNABIDIOL   GLRA1

    Interaction Score: 0.12

    Interaction Types & Directionality:
    allosteric modulator

    Interaction Info:

    PMIDs:
    19204413 26264914


    Sources:
    DrugBank

  • ANANDAMIDE   GLRA1

    Interaction Score: 0.11

    Interaction Types & Directionality:
    allosteric modulator

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

    PMIDs:
    None found


    Sources:
    GuideToPharmacology

  • NABIXIMOLS   GLRA1

    Interaction Score: 0.08

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    26264914


    Sources:
    DrugBank

  • ALCOHOL   GLRA1

    Interaction Score: 0.08

    Interaction Types & Directionality:
    agonist (activating)

    Interaction Info:

    PMIDs:
    9452448 21044637 20713066 17139284 17016423


    Sources:
    DrugBank

  • ZINC CHLORIDE   GLRA1

    Interaction Score: 0.04

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:

    PMIDs:
    16842826


    Sources:
    DrugBank

  • COLCHICINE   GLRA1

    Interaction Score: 0.04

    Interaction Types & Directionality:
    antagonist (inhibitory)

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

    PMIDs:
    None found


    Sources:
    GuideToPharmacology

  • NIFEDIPINE   GLRA1

    Interaction Score: 0.03

    Interaction Types & Directionality:
    antagonist (inhibitory)

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

    PMIDs:
    None found


    Sources:
    GuideToPharmacology

  • COPPER   GLRA1

    Interaction Score: 0.02

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    16842826


    Sources:
    DrugBank

  • METHYLDOPA   GLRA1

    Interaction Score: 0.02

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    16842826


    Sources:
    DrugBank

  • Ensembl: ENSG00000145888

    • Version: 101_38

    Alternate Names:
    GLRA1 Ensembl Gene Name

    Gene Info:
    Gene Biotype PROTEIN_CODING

    Publications:

  • RussLampel: ENSG00000145888

    • Version: 26-July-2011

    Alternate Names:
    GLRA1 Display Id
    GLYCINE RECEPTOR ALPHA-1 CHAIN PRECURSOR (GLYCINE RECEPTOR 48 KDA SUBUNIT) (STRYCHNINE BINDING SUBUNIT). [SOURCE:UNIPROT/SWISSPROT;ACC:P23415] Description
    ENSG00000145888 Ensembl Gene Id

    Gene Info:
    Human Readable Name DRUGGABLE GENOME

    Gene Categories:
    DRUGGABLE GENOME

    Publications:

  • TEND: P23415

    • Version: 01-August-2011

    Alternate Names:
    GLRA1 Gene Symbol
    P23415 Uniprot Accession
    2741 Entrez Gene Id

    Gene Info:
    Transmembrane Helix Count 3
    Target Subclass Channels
    Target Subclass Ligand_gated_ion_channels

    Publications:

  • TdgClinicalTrial: P23415

    • Version: January-2014

    Alternate Names:
    GLRA1 Gene Symbol

    Gene Info:
    Target Class Receptors
    Target Subclass TC:1.A.9.3.1

    Publications:

  • HopkinsGroom: P23415

    • Version: 11-September-2012

    Alternate Names:
    GLRA1_HUMAN Uniprot Id
    ENSG00000145888 Ensembl Gene Id
    P23415 Uniprot Accession

    Gene Info:
    Uniprot Status Swiss-Prot
    Interpro Type Family
    Human Readable Name ION CHANNEL

    Gene Categories:
    ION CHANNEL, DRUGGABLE GENOME

    Publications:

  • GuideToPharmacology: 2741

    • Version: 29-September-2020

    Alternate Names:
    4326 HUGO Gene ID
    4326 HUGO Gene Symbol
    glycine receptor alpha 1 HUGO Gene Name

    Gene Info:
    GuideToPharmacology Gene Category Name Glycine receptors
    GuideToPharmacology Gene Category ID 73

    Gene Categories:
    ION CHANNEL

    Publications:

  • DrugBank: BE0000433

    • Version: 5.1.7

    Alternate Names:
    GLRA1 DrugBank Gene Name
    P23415 UniProt Accession
    2741 Entrez Gene Id

    Gene Info:

    Publications:
    Heinze et al., 2007, Diversity of glycine receptors in the mouse retina: localization of the alpha4 subunit., J. Comp. Neurol.
    Eulenburg et al., 2006, Mutations within the human GLYT2 (SLC6A5) gene associated with hyperekplexia., Biochem. Biophys. Res. Commun.
    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

  • DrugBank: BE0009666

    • Version: 5.1.7

    Alternate Names:
    GLRA1 DrugBank Gene Name
    P23415 UniProt Accession
    2741 Entrez Gene Id

    Gene Info:

    Publications:
    Limapichat W et al., 2013, Key binding interactions for memantine in the NMDA receptor., ACS Chem Neurosci
    Xia P et al., 2010, Memantine preferentially blocks extrasynaptic over synaptic NMDA receptor currents in hippocampal autapses., J Neurosci

  • DrugBank: BE0004857

    • Version: 5.1.7

    Alternate Names:
    GLRA1 DrugBank Gene Name
    P23415 UniProt Accession
    2741 Entrez Gene Id

    Gene Info:

    Publications:
    Bialer M et al., 2007, Progress report on new antiepileptic drugs: a summary of the Eigth Eilat Conference (EILAT VIII)., Epilepsy Res
    Ibeas Bih C et al., 2015, Molecular Targets of Cannabidiol in Neurological Disorders., Neurotherapeutics
    Ahrens J et al., 2009, The nonpsychotropic cannabinoid cannabidiol modulates and directly activates alpha-1 and alpha-1-Beta glycine receptor function., Pharmacology

  • DTC: GLRA1

    • Version: 02-September-2020

    Alternate Names:

    Gene Info:

    Publications:
    Balansa W et al., 2010, Ircinialactams: subunit-selective glycine receptor modulators from Australian sponges of the family Irciniidae., Bioorg Med Chem

  • ChemblInteractions: GLRA1

    • Version: chembl_23

    Alternate Names:
    GLRA1 GENE_SYMBOL
    Glycine receptor subunit alpha-1 UNIPROT
    Glycine receptor 48 kDa subunit UNIPROT

    Gene Info:

    Publications:

  • HingoraniCasas: ENSG00000145888

    • Version: 31-May-2017

    Alternate Names:
    ENSG00000145888 Gene Symbol
    GLRA1 Ensembl Id

    Gene Info:

    Gene Categories:
    DRUGGABLE GENOME

    Publications:

  • Pharos: GLRA1

    • Version: 03-September-2020

    Alternate Names:
    Glycine receptor subunit alpha-1 Gene Name
    P23415 UniProt ID

    Gene Info:

    Gene Categories:
    ION CHANNEL

    Publications:

  • TTD: Strychnine-binding glycine receptor

    • Version: 2020.06.01

    Alternate Names:
    GLRA1 TTD Gene Abbreviation
    T50269 TTD Target ID

    Gene Info:

    Publications:

  • GO: GLRA1

    • Version: 05-September-2020

    Alternate Names:

    Gene Info:

    Gene Categories:
    EXTERNAL SIDE OF PLASMA MEMBRANE

    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