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GRIN1 Gene Record

  • Summary
  • Interactions
  • Claims
  • GRIN1 2902 Druggable Genome

    Alternate Names:

    2902
    GLUTAMATE IONOTROPIC RECEPTOR NMDA TYPE SUBUNIT 1
    GRIN1
    GluN1
    MRD8
    NMD-R1
    NMDA1
    NMDAR1
    NR1
    138249
    4584
    ENSG00000176884
    OTTHUMG00000020976
    NMDZ1_HUMAN
    Q05586
    N-methyl-D-aspartate receptor subunit NR1
    Glutamate [NMDA] receptor subunit zeta-1
    Glutamate receptor ionotropic, NMDA 1
    BE0000365
    GLUTAMATE [NMDA] RECEPTOR SUBUNIT ZETA 1 PRECURSOR (N-METHYL-D- ASPARTATE RECEPTOR SUBUNIT NR1). [SOURCE:UNIPROT/SWISSPROT;ACC:Q05586]
    BE0004852
    455
    NP_015566
    NM_007327
    BE0004956
    Q12879
    GRIN2A
    PA28978
    Glutamate receptor ionotropic NMDA 1
    T62276

    Gene Info:

    Human Readable Name DRUGGABLE GENOME
    Interpro Type Domain
    Uniprot Status Swiss-Prot
    Interpro Acc IPR001320
    Interpro Name Ionotropic glutamate receptor
    Uniprot Evidence 1: Evidence at protein level
    Interpro Short Name Iontro_glu_rcpt
    Transmembrane Helix Count 3
    Target Subclass Ligand_gated_ion_channels
    Target Subclass Glutamate
    Target Subclass Channels
    Target Main Class Receptors
    GuideToPharmacology Gene Category Name Ionotropic glutamate receptors
    GuideToPharmacology Gene Category ID 75
    Target Class Receptors
    Target Subclass TC:1.A.10.1
    Target Subclass TC:1.A.10.1.6
    Gene Biotype PROTEIN_CODING
    (14 More Sources)

    Gene Categories: Category Details

    CELL SURFACE
    ION CHANNEL
    DRUGGABLE GENOME

    Publications:

    Rook Y et al., 2010, Bivalent beta-carbolines as potential multitarget anti-Alzheimer agents., J Med Chem
    Berman et al., 2000, The Protein Data Bank., Nucleic Acids Res.
    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
    Ebert et al., 1995, Ketobemidone, methadone and pethidine are non-competitive N-methyl-D-aspartate (NMDA) antagonists in the rat cortex and spinal cord., Neurosci. Lett.
    Chanasong R et al., 2013, Genetic variation of GRIN1 confers vulnerability to methamphetamine-dependent psychosis in a Thai population., Neurosci Lett
    Frølund S et al., 2010, Assessment of structurally diverse philanthotoxin analogues for inhibitory activity on ionotropic glutamate receptor subtypes: discovery of nanomolar, nonselective, and use-dependent antagonists., J Med Chem
    Ludolph et al., 2010, Atomoxetine acts as an NMDA receptor blocker in clinically relevant concentrations., Br. J. Pharmacol.
    Snell et al., 1988, Cycloleucine competitively antagonizes the strychnine-insensitive glycine receptor., Eur. J. Pharmacol.
    Herberg et al., 1990, Effects of D-cycloserine and cycloleucine, ligands for the NMDA-associated strychnine-insensitive glycine site, on brain-stimulation reward and spontaneous locomotion., Pharmacol. Biochem. Behav.
    Hershkowitz et al., 1989, Cycloleucine blocks NMDA responses in cultured hippocampal neurones under voltage clamp: antagonism at the strychnine-insensitive glycine receptor., Br. J. Pharmacol.
    Kornhuber et al., 1995, Orphenadrine is an uncompetitive N-methyl-D-aspartate (NMDA) receptor antagonist: binding and patch clamp studies., J. Neural Transm. Gen. Sect.
    Robinson DM et al., 2006, Memantine: a review of its use in Alzheimer's disease., Drugs
    Rogawski et al., 2003, The neuropharmacological basis for the use of memantine in the treatment of Alzheimer's disease., CNS Drug Rev
    Kotermanski et al., 2009, Memantine binding to a superficial site on NMDA receptors contributes to partial trapping., J. Physiol. (Lond.)
    Cacabelos R et al., 1999, The glutamatergic system and neurodegeneration in dementia: preventive strategies in Alzheimer's disease., Int J Geriatr Psychiatry
    Daniell, 1994, Effect of anesthetic and convulsant barbiturates on N-methyl-D-aspartate receptor-mediated calcium flux in brain membrane vesicles., Pharmacology
    Miglio et al., 2007, Stimulation of N-methyl-D-aspartate receptors modulates Jurkat T cell growth and adhesion to fibronectin., Biochem. Biophys. Res. Commun.
    Lipton et al., 2002, Cysteine regulation of protein function--as exemplified by NMDA-receptor modulation., Trends Neurosci.
    Zhu et al., 2003, Region-specific changes in NMDA receptor mRNA induced by chronic morphine treatment are prevented by the co-administration of the competitive NMDA receptor antagonist LY274614., Brain Res. Mol. Brain Res.
    Witkiewitz et al., 2012, Acamprosate for treatment of alcohol dependence: mechanisms, efficacy, and clinical utility., Ther Clin Risk Manag
    Mann et al., 2008, Acamprosate: recent findings and future research directions., Alcohol. Clin. Exp. Res.
    Porcelli S et al., 2016, Possible biomarkers modulating haloperidol efficacy and/or tolerability., Pharmacogenomics
    Yang et al., 1999, Agmatine selectively blocks the N-methyl-D-aspartate subclass of glutamate receptor channels in rat hippocampal neurons., J. Pharmacol. Exp. Ther.
    Compagnone et al., 1998, Dehydroepiandrosterone: a potential signalling molecule for neocortical organization during development., Proc. Natl. Acad. Sci. U.S.A.
    Morrison RL et al., 2018, Effect of intranasal esketamine on cognitive functioning in healthy participants: a randomized, double-blind, placebo-controlled study., Psychopharmacology (Berl)
    Seppälä et al., 1988, Effects of the novel 5-hydroxytryptamine reuptake inhibitor indalpine and ethanol on psychomotor performance., Arzneimittelforschung
    Kohno et al., 2012, Milnacipran inhibits glutamatergic N-methyl-D-aspartate receptor activity in spinal dorsal horn neurons., Mol Pain
    Shuto et al., 1995, (+/-)-(Z)-2-(aminomethyl)-1-phenylcyclopropanecarboxamide derivatives as a new prototype of NMDA receptor antagonists., J. Med. Chem.
    Warach et al., 2006, Effect of the Glycine Antagonist Gavestinel on cerebral infarcts in acute stroke patients, a randomized placebo-controlled trial: The GAIN MRI Substudy., Cerebrovasc. Dis.
    Yamakura et al., 2000, N-methyl-D-aspartate receptor channel block by meperidine is dependent on extracellular pH., Anesth. Analg.
    Shen H et al., 2010, Neuroprotection by donepezil against glutamate excitotoxicity involves stimulation of alpha7 nicotinic receptors and internalization of NMDA receptors., Br J Pharmacol
    Eap CB et al., 2002, Interindividual variability of the clinical pharmacokinetics of methadone: implications for the treatment of opioid dependence., Clin Pharmacokinet
    Sotgiu et al., 2009, Cooperative N-methyl-D-aspartate (NMDA) receptor antagonism and mu-opioid receptor agonism mediate the methadone inhibition of the spinal neuron pain-related hyperactivity in a rat model of neuropathic pain., Pharmacol. Res.
    Hanania T et al., 2020, The N-methyl-D-aspartate receptor antagonist d-methadone acutely improves depressive-like behavior in the forced swim test performance of rats., Exp Clin Psychopharmacol
    de Bartolomeis A et al., 2015, Update on the Mechanism of Action of Aripiprazole: Translational Insights into Antipsychotic Strategies Beyond Dopamine Receptor Antagonism., CNS Drugs
    Hara et al., 2005, The effects of tramadol and its metabolite on glycine, gamma-aminobutyric acidA, and N-methyl-D-aspartate receptors expressed in Xenopus oocytes., Anesth. Analg.
    Barakat A, 2019, Revisiting Tramadol: A Multi-Modal Agent for Pain Management., CNS Drugs
    Nikolaev MV et al., 2012, Influence of external magnesium ions on the NMDA receptor channel block by different types of organic cations., Neuropharmacology
    Keshavarz M et al., 2013, Anticonvulsant Effect of Guaifenesin against Pentylenetetrazol-Induced Seizure in Mice., Iran J Med Sci
    Cheng G et al., 2000, Enflurane directly depresses glutamate AMPA and NMDA currents in mouse spinal cord motor neurons independent of actions on GABAA or glycine receptors., Anesthesiology
    Dildy-Mayfield et al., 1996, Anesthetics produce subunit-selective actions on glutamate receptors., J. Pharmacol. Exp. Ther.
  • CYCLOLEUCINE   GRIN1

    Interaction Score: 4.24

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    2843389 2170997 10592235 2556198


    Sources:
    DrugBank

  • RENACIDIN   GRIN1

    Interaction Score: 1.7

    Interaction Types & Directionality:
    blocker (inhibitory)

    Interaction Info:

    PMIDs:
    22261381


    Sources:
    DrugBank

  • GAVESTINEL   GRIN1

    Interaction Score: 1.7

    Interaction Types & Directionality:
    antagonist (inhibitory)

    Interaction Info:

    PMIDs:
    16340185


    Sources:
    DrugBank

  • MAGNESIUM ACETATE TETRAHYDRATE   GRIN1

    Interaction Score: 0.85

    Interaction Types & Directionality:
    ligand

    Interaction Info:

    PMIDs:
    None found


    Sources:
    DrugBank

  • CHEMBL50267   GRIN1

    Interaction Score: 0.85

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    10592235


    Sources:
    DrugBank

  • ORPHENADRINE   GRIN1

    Interaction Score: 0.73

    Interaction Types & Directionality:
    antagonist (inhibitory)

    Interaction Info:
    Novel drug target Established target
    Trial Name -

    PMIDs:
    17139284 17016423 8788072


    Sources:
    TEND TdgClinicalTrial DrugBank

  • MEMANTINE   GRIN1

    Interaction Score: 0.68

    Interaction Types & Directionality:
    binder
    antagonist (inhibitory)

    Interaction Info:
    Trial Name memantine
    Novel drug target Established target
    Trial Name Namenda

    PMIDs:
    16906789 20361801 14530799 19687120 10029935


    Sources:
    DTC TdgClinicalTrial DrugBank

  • (D)-SERINE   GRIN1

    Interaction Score: 0.64

    Interaction Types & Directionality:
    agonist (activating)

    Interaction Info:
    Specific Binding Site for Interaction glycine site
    Specific Action of the Ligand Agonist
    Endogenous Drug? True

    PMIDs:
    10592235 17139284 17016423


    Sources:
    TTD DrugBank GuideToPharmacology

  • PHILANTHOTOXIN 343   GRIN1

    Interaction Score: 0.57

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    20873775


    Sources:
    DTC

  • ACAMPROSATE   GRIN1

    Interaction Score: 0.51

    Interaction Types & Directionality:
    antagonist (inhibitory)

    Interaction Info:

    PMIDs:
    22346357 18540918


    Sources:
    DrugBank

  • TRAXOPRODIL   GRIN1

    Interaction Score: 0.42

    Interaction Types & Directionality:
    antagonist (inhibitory)

    Interaction Info:
    Mechanism of Interaction Glutamate NMDA receptor; GRIN1/GRIN2B antagonist
    Direct Interaction yes

    PMIDs:
    None found


    Sources:
    ChemblInteractions

  • MILNACIPRAN   GRIN1

    Interaction Score: 0.42

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:

    PMIDs:
    22716121 7636857


    Sources:
    DrugBank

  • IFENPRODIL   GRIN1

    Interaction Score: 0.42

    Interaction Types & Directionality:
    antagonist (inhibitory)

    Interaction Info:

    PMIDs:
    3365283


    Sources:
    DrugBank

  • RADIPRODIL   GRIN1

    Interaction Score: 0.42

    Interaction Types & Directionality:
    antagonist (inhibitory)

    Interaction Info:
    Mechanism of Interaction Glutamate NMDA receptor; GRIN1/GRIN2B antagonist
    Direct Interaction yes

    PMIDs:
    None found


    Sources:
    ChemblInteractions

  • RISLENEMDAZ   GRIN1

    Interaction Score: 0.42

    Interaction Types & Directionality:
    antagonist (inhibitory)

    Interaction Info:
    Direct Interaction yes
    Mechanism of Interaction Glutamate NMDA receptor; GRIN1/GRIN2B antagonist

    PMIDs:
    None found


    Sources:
    ChemblInteractions

  • KETOBEMIDONE   GRIN1

    Interaction Score: 0.42

    Interaction Types & Directionality:
    antagonist (inhibitory)

    Interaction Info:

    PMIDs:
    7624018


    Sources:
    DrugBank

  • CNS-5161   GRIN1

    Interaction Score: 0.36

    Interaction Types & Directionality:
    blocker (inhibitory)

    Interaction Info:
    Trial Name CNS-5161
    Novel drug target Established target
    Mechanism of Interaction Glutamate [NMDA] receptor blocker

    PMIDs:
    None found


    Sources:
    TdgClinicalTrial DrugBank ChemblInteractions

  • GUAIFENESIN   GRIN1

    Interaction Score: 0.34

    Interaction Types & Directionality:
    antagonist (inhibitory)

    Interaction Info:

    PMIDs:
    23825891


    Sources:
    DrugBank

  • NERAMEXANE   GRIN1

    Interaction Score: 0.28

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    Trial Name neramexane mesylate
    Novel drug target Established target

    PMIDs:
    None found


    Sources:
    TdgClinicalTrial

  • CYCLOSERINE   GRIN1

    Interaction Score: 0.28

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    TTD

  • EVT-101   GRIN1

    Interaction Score: 0.28

    Interaction Types & Directionality:
    antagonist (inhibitory)

    Interaction Info:
    Mechanism of Interaction Glutamate NMDA receptor; GRIN1/GRIN2B antagonist
    Direct Interaction yes

    PMIDs:
    None found


    Sources:
    ChemblInteractions

  • DIZOCILPINE   GRIN1

    Interaction Score: 0.28

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    20361801


    Sources:
    DTC

  • ESKETAMINE   GRIN1

    Interaction Score: 0.25

    Interaction Types & Directionality:
    antagonist (inhibitory)

    Interaction Info:
    Direct Interaction yes
    Mechanism of Interaction Glutamate [NMDA] receptor negative allosteric modulator

    PMIDs:
    29392371


    Sources:
    DrugBank ChemblInteractions

  • RAPASTINEL   GRIN1

    Interaction Score: 0.24

    Interaction Types & Directionality:
    partial agonist (activating)

    Interaction Info:
    Novel drug target Established target
    Trial Name GLYX-13
    Mechanism of Interaction Glutamate [NMDA] receptor partial agonist

    PMIDs:
    None found


    Sources:
    TdgClinicalTrial ChemblInteractions

  • AGMATINE   GRIN1

    Interaction Score: 0.24

    Interaction Types & Directionality:
    antagonist (inhibitory)

    Interaction Info:

    PMIDs:
    9918557


    Sources:
    DrugBank

  • LANICEMINE   GRIN1

    Interaction Score: 0.24

    Interaction Types & Directionality:
    blocker (inhibitory)

    Interaction Info:
    Mechanism of Interaction Glutamate [NMDA] receptor blocker
    Direct Interaction yes
    Trial Name AZD-6765

    PMIDs:
    None found


    Sources:
    TdgClinicalTrial ChemblInteractions

  • ESKETAMINE HYDROCHLORIDE   GRIN1

    Interaction Score: 0.24

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    Mechanism of Interaction Glutamate [NMDA] receptor negative allosteric modulator
    Direct Interaction yes
    Trial Name AM-101

    PMIDs:
    None found


    Sources:
    TdgClinicalTrial ChemblInteractions

  • ELIPRODIL   GRIN1

    Interaction Score: 0.21

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    TTD

  • DIMIRACETAM   GRIN1

    Interaction Score: 0.21

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    Trial Name dimiracetam, NT-11624
    Novel drug target Established target

    PMIDs:
    None found


    Sources:
    TdgClinicalTrial

  • ATOMOXETINE   GRIN1

    Interaction Score: 0.21

    Interaction Types & Directionality:
    blocker (inhibitory)

    Interaction Info:

    PMIDs:
    20423340


    Sources:
    DrugBank

  • INDANTADOL   GRIN1

    Interaction Score: 0.19

    Interaction Types & Directionality:
    antagonist (inhibitory)

    Interaction Info:
    Novel drug target Established target
    Trial Name V3381
    Direct Interaction yes

    PMIDs:
    None found


    Sources:
    TdgClinicalTrial ChemblInteractions

  • SECOBARBITAL   GRIN1

    Interaction Score: 0.15

    Interaction Types & Directionality:
    antagonist (inhibitory)

    Interaction Info:

    PMIDs:
    7862741


    Sources:
    DrugBank

  • METHADONE   GRIN1

    Interaction Score: 0.15

    Interaction Types & Directionality:
    antagonist (inhibitory)

    Interaction Info:

    PMIDs:
    12405865 19717013 17139284 31368772 17016423


    Sources:
    DrugBank

  • FELBAMATE   GRIN1

    Interaction Score: 0.14

    Interaction Types & Directionality:
    antagonist (inhibitory)

    Interaction Info:
    Trial Name -
    Novel drug target Established target
    Mechanism of Interaction Glutamate [NMDA] receptor antagonist

    PMIDs:
    None found


    Sources:
    TdgClinicalTrial ChemblInteractions

  • DONEPEZIL   GRIN1

    Interaction Score: 0.13

    Interaction Types & Directionality:
    negative modulator (inhibitory)

    Interaction Info:

    PMIDs:
    20718745


    Sources:
    DrugBank

  • GW468816   GRIN1

    Interaction Score: 0.12

    Interaction Types & Directionality:
    antagonist (inhibitory)

    Interaction Info:
    Mechanism of Interaction Glutamate [NMDA] receptor antagonist
    Direct Interaction yes

    PMIDs:
    None found


    Sources:
    ChemblInteractions

  • AZD8108   GRIN1

    Interaction Score: 0.12

    Interaction Types & Directionality:
    antagonist (inhibitory)

    Interaction Info:
    Mechanism of Interaction Glutamate [NMDA] receptor antagonist
    Direct Interaction yes

    PMIDs:
    None found


    Sources:
    ChemblInteractions

  • DELUCEMINE   GRIN1

    Interaction Score: 0.12

    Interaction Types & Directionality:
    antagonist (inhibitory)

    Interaction Info:
    Direct Interaction yes
    Mechanism of Interaction Glutamate [NMDA] receptor antagonist

    PMIDs:
    None found


    Sources:
    ChemblInteractions

  • MEMANTINE HYDROCHLORIDE   GRIN1

    Interaction Score: 0.12

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    Mechanism of Interaction Glutamate [NMDA] receptor negative allosteric modulator
    Direct Interaction yes

    PMIDs:
    None found


    Sources:
    ChemblInteractions

  • KETAMINE HYDROCHLORIDE   GRIN1

    Interaction Score: 0.12

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    Direct Interaction yes
    Mechanism of Interaction Glutamate [NMDA] receptor negative allosteric modulator

    PMIDs:
    None found


    Sources:
    ChemblInteractions

  • LATREPIRDINE   GRIN1

    Interaction Score: 0.12

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    Trial Name Dimebon
    Novel drug target Established target

    PMIDs:
    None found


    Sources:
    TdgClinicalTrial

  • NEBOGLAMINE   GRIN1

    Interaction Score: 0.12

    Interaction Types & Directionality:
    positive modulator (activating)

    Interaction Info:
    Mechanism of Interaction Glutamate [NMDA] receptor positive allosteric modulator
    Direct Interaction yes

    PMIDs:
    None found


    Sources:
    ChemblInteractions

  • APIMOSTINEL   GRIN1

    Interaction Score: 0.12

    Interaction Types & Directionality:
    partial agonist (activating)

    Interaction Info:
    Mechanism of Interaction Glutamate [NMDA] receptor partial agonist
    Direct Interaction yes

    PMIDs:
    None found


    Sources:
    ChemblInteractions

  • AV-101   GRIN1

    Interaction Score: 0.12

    Interaction Types & Directionality:
    antagonist (inhibitory)

    Interaction Info:
    Mechanism of Interaction Glutamate [NMDA] receptor antagonist
    Direct Interaction yes

    PMIDs:
    None found


    Sources:
    ChemblInteractions

  • MEPERIDINE   GRIN1

    Interaction Score: 0.11

    Interaction Types & Directionality:
    antagonist (inhibitory)

    Interaction Info:

    PMIDs:
    10735801


    Sources:
    DrugBank

  • AMANTADINE HYDROCHLORIDE   GRIN1

    Interaction Score: 0.11

    Interaction Types & Directionality:
    antagonist (inhibitory)

    Interaction Info:
    Direct Interaction yes
    Mechanism of Interaction Glutamate [NMDA] receptor antagonist

    PMIDs:
    None found


    Sources:
    ChemblInteractions

  • TRAMADOL   GRIN1

    Interaction Score: 0.09

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:

    PMIDs:
    15845694 31004280


    Sources:
    DrugBank

  • N-METHYL-D-ASPARTIC ACID (NMDA)   GRIN1

    Interaction Score: 0.09

    Interaction Types & Directionality:
    agonist (activating)

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

    PMIDs:
    None found


    Sources:
    GuideToPharmacology

  • NERAMEXANE MESYLATE   GRIN1

    Interaction Score: 0.09

    Interaction Types & Directionality:
    antagonist (inhibitory)

    Interaction Info:
    Mechanism of Interaction Glutamate [NMDA] receptor antagonist
    Direct Interaction yes

    PMIDs:
    None found


    Sources:
    ChemblInteractions

  • KETAMINE   GRIN1

    Interaction Score: 0.08

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    20361801


    Sources:
    DTC

  • PENTOBARBITAL   GRIN1

    Interaction Score: 0.08

    Interaction Types & Directionality:
    antagonist (inhibitory)

    Interaction Info:

    PMIDs:
    7862741


    Sources:
    DrugBank

  • ENFLURANE   GRIN1

    Interaction Score: 0.07

    Interaction Types & Directionality:
    antagonist (inhibitory)

    Interaction Info:

    PMIDs:
    11020764 8786535


    Sources:
    DrugBank

  • DEXANABINOL   GRIN1

    Interaction Score: 0.07

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    Trial Name dexanabinol, HU-211
    Novel drug target Established target

    PMIDs:
    None found


    Sources:
    TdgClinicalTrial

  • ACETYLCYSTEINE   GRIN1

    Interaction Score: 0.07

    Interaction Types & Directionality:
    activator (activating)

    Interaction Info:

    PMIDs:
    12183209


    Sources:
    DrugBank

  • PRASTERONE   GRIN1

    Interaction Score: 0.07

    Interaction Types & Directionality:
    agonist (activating)

    Interaction Info:

    PMIDs:
    9539798


    Sources:
    DrugBank

  • METHAMPHETAMINE   GRIN1

    Interaction Score: 0.07

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    23880023


    Sources:
    PharmGKB

  • NBQX   GRIN1

    Interaction Score: 0.06

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    TTD

  • MORPHINE   GRIN1

    Interaction Score: 0.05

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    12829326


    Sources:
    NCI

  • PHENOBARBITAL   GRIN1

    Interaction Score: 0.04

    Interaction Types & Directionality:
    antagonist (inhibitory)

    Interaction Info:

    PMIDs:
    7862741


    Sources:
    DrugBank

  • RALFINAMIDE   GRIN1

    Interaction Score: 0.04

    Interaction Types & Directionality:
    antagonist (inhibitory)

    Interaction Info:
    Direct Interaction yes
    Mechanism of Interaction Glutamate [NMDA] receptor antagonist

    PMIDs:
    None found


    Sources:
    ChemblInteractions

  • ORPHENADRINE HYDROCHLORIDE   GRIN1

    Interaction Score: 0.04

    Interaction Types & Directionality:
    antagonist (inhibitory)

    Interaction Info:
    Direct Interaction yes
    Mechanism of Interaction Glutamate [NMDA] receptor antagonist

    PMIDs:
    None found


    Sources:
    ChemblInteractions

  • ORPHENADRINE CITRATE   GRIN1

    Interaction Score: 0.04

    Interaction Types & Directionality:
    antagonist (inhibitory)

    Interaction Info:
    Mechanism of Interaction Glutamate [NMDA] receptor antagonist
    Direct Interaction yes

    PMIDs:
    None found


    Sources:
    ChemblInteractions

  • ARIPIPRAZOLE   GRIN1

    Interaction Score: 0.04

    Interaction Types & Directionality:
    ligand

    Interaction Info:

    PMIDs:
    26346901


    Sources:
    DrugBank

  • ACAMPROSATE CALCIUM   GRIN1

    Interaction Score: 0.04

    Interaction Types & Directionality:
    antagonist (inhibitory)

    Interaction Info:
    Mechanism of Interaction Glutamate [NMDA] receptor antagonist
    Direct Interaction yes

    PMIDs:
    None found


    Sources:
    ChemblInteractions

  • GLUTAMIC ACID   GRIN1

    Interaction Score: 0.03

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    17662248


    Sources:
    DrugBank

  • GLYCINE   GRIN1

    Interaction Score: 0.03

    Interaction Types & Directionality:
    agonist (activating)

    Interaction Info:
    Specific Binding Site for Interaction glycine site
    Specific Action of the Ligand Agonist
    Endogenous Drug? True

    PMIDs:
    None found


    Sources:
    GuideToPharmacology

  • HALOPERIDOL   GRIN1

    Interaction Score: 0.02

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    27023437


    Sources:
    PharmGKB

  • Ensembl: ENSG00000176884

    • Version: 101_38

    Alternate Names:
    GRIN1 Ensembl Gene Name

    Gene Info:
    Gene Biotype PROTEIN_CODING

    Publications:

  • TdgClinicalTrial: Q05586

    • Version: January-2014

    Alternate Names:
    GRIN1 Gene Symbol

    Gene Info:
    Target Class Receptors
    Target Subclass TC:1.A.10.1.6

    Publications:

  • TEND: Q05586

    • Version: 01-August-2011

    Alternate Names:
    Q05586 Uniprot Accession
    GRIN1 Gene Symbol
    2902 Entrez Gene Id

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

    Publications:

  • RussLampel: ENSG00000176884

    • Version: 26-July-2011

    Alternate Names:
    ENSG00000176884 Ensembl Gene Id
    GLUTAMATE [NMDA] RECEPTOR SUBUNIT ZETA 1 PRECURSOR (N-METHYL-D- ASPARTATE RECEPTOR SUBUNIT NR1). [SOURCE:UNIPROT/SWISSPROT;ACC:Q05586] Description
    GRIN1 Display Id

    Gene Info:
    Human Readable Name DRUGGABLE GENOME

    Gene Categories:
    DRUGGABLE GENOME

    Publications:

  • HopkinsGroom: Q05586

    • Version: 11-September-2012

    Alternate Names:
    GRIN1 Uniprot Gene Name
    GLUTAMATE [NMDA] RECEPTOR SUBUNIT ZETA-1 Uniprot Protein Name
    2902 Entrez Gene Id

    Gene Info:
    Interpro Type Domain
    Uniprot Status Swiss-Prot
    Interpro Acc IPR001320

    Gene Categories:
    DRUGGABLE GENOME

    Publications:

  • TdgClinicalTrial: Q12879

    • Version: January-2014

    Alternate Names:
    GRIN2A Gene Symbol
    GRIN1 Gene Symbol

    Gene Info:
    Target Class Receptors
    Target Subclass TC:1.A.10.1

    Publications:

  • GuideToPharmacology: 2902

    • Version: 29-September-2020

    Alternate Names:
    4584 HUGO Gene ID
    4584 HUGO Gene Symbol
    glutamate ionotropic receptor NMDA type subunit 1 HUGO Gene Name

    Gene Info:
    GuideToPharmacology Gene Category Name Ionotropic glutamate receptors
    GuideToPharmacology Gene Category ID 75

    Gene Categories:
    ION CHANNEL

    Publications:

  • PharmGKB: GRIN1

    • Version: 18-August-2020

    Alternate Names:
    PA28978 PharmGKB ID

    Gene Info:

    Publications:
    Porcelli S et al., 2016, Possible biomarkers modulating haloperidol efficacy and/or tolerability., Pharmacogenomics
    Chanasong R et al., 2013, Genetic variation of GRIN1 confers vulnerability to methamphetamine-dependent psychosis in a Thai population., Neurosci Lett

  • DrugBank: BE0004956

    • Version: 5.1.7

    Alternate Names:
    GRIN1 DrugBank Gene Name
    Q05586 UniProt Accession
    2902 Entrez Gene Id

    Gene Info:

    Publications:
    Hara et al., 2005, The effects of tramadol and its metabolite on glycine, gamma-aminobutyric acidA, and N-methyl-D-aspartate receptors expressed in Xenopus oocytes., Anesth. Analg.
    Barakat A, 2019, Revisiting Tramadol: A Multi-Modal Agent for Pain Management., CNS Drugs
    Ludolph et al., 2010, Atomoxetine acts as an NMDA receptor blocker in clinically relevant concentrations., Br. J. Pharmacol.

  • DrugBank: BE0000365

    • Version: 5.1.7

    Alternate Names:
    GRIN1 DrugBank Gene Name
    Q05586 UniProt Accession
    2902 Entrez Gene Id

    Gene Info:

    Publications:
    Miglio et al., 2007, Stimulation of N-methyl-D-aspartate receptors modulates Jurkat T cell growth and adhesion to fibronectin., Biochem. Biophys. Res. Commun.
    Yamakura et al., 2000, N-methyl-D-aspartate receptor channel block by meperidine is dependent on extracellular pH., Anesth. Analg.
    Kotermanski et al., 2009, Memantine binding to a superficial site on NMDA receptors contributes to partial trapping., J. Physiol. (Lond.)

  • DrugBank: BE0004852

    • Version: 5.1.7

    Alternate Names:
    GRIN1 DrugBank Gene Name
    Q05586 UniProt Accession
    2902 Entrez Gene Id

    Gene Info:

    Publications:
    Cheng G et al., 2000, Enflurane directly depresses glutamate AMPA and NMDA currents in mouse spinal cord motor neurons independent of actions on GABAA or glycine receptors., Anesthesiology
    Dildy-Mayfield et al., 1996, Anesthetics produce subunit-selective actions on glutamate receptors., J. Pharmacol. Exp. Ther.
    Robinson DM et al., 2006, Memantine: a review of its use in Alzheimer's disease., Drugs

  • NCI: GRIN1

    • Version: 14-September-2017

    Alternate Names:

    Gene Info:

    Publications:
    Zhu et al., 2003, Region-specific changes in NMDA receptor mRNA induced by chronic morphine treatment are prevented by the co-administration of the competitive NMDA receptor antagonist LY274614., Brain Res. Mol. Brain Res.

  • DTC: GRIN1

    • Version: 02-September-2020

    Alternate Names:

    Gene Info:

    Publications:
    Frølund S et al., 2010, Assessment of structurally diverse philanthotoxin analogues for inhibitory activity on ionotropic glutamate receptor subtypes: discovery of nanomolar, nonselective, and use-dependent antagonists., J Med Chem
    Rook Y et al., 2010, Bivalent beta-carbolines as potential multitarget anti-Alzheimer agents., J Med Chem

  • ChemblInteractions: NMDAR1

    • Version: chembl_23

    Alternate Names:
    NMDAR1 GENE_SYMBOL
    GRIN1 GENE_SYMBOL
    Glutamate receptor ionotropic, NMDA 1 UNIPROT

    Gene Info:

    Publications:

  • HingoraniCasas: ENSG00000176884

    • Version: 31-May-2017

    Alternate Names:
    ENSG00000176884 Gene Symbol
    GRIN1 Ensembl Id

    Gene Info:

    Gene Categories:
    DRUGGABLE GENOME

    Publications:

  • Pharos: GRIN1

    • Version: 03-September-2020

    Alternate Names:
    Glutamate receptor ionotropic, NMDA 1 Gene Name
    Q05586 UniProt ID

    Gene Info:

    Gene Categories:
    ION CHANNEL

    Publications:

  • GO: GRIN1

    • Version: 05-September-2020

    Alternate Names:
    NMDAR1 GO Gene Synonym

    Gene Info:

    Gene Categories:
    CELL SURFACE

    Publications:

  • TTD: Glutamate receptor ionotropic NMDA 1

    • Version: 2020.06.01

    Alternate Names:
    NMDAR1 TTD Gene Abbreviation
    T62276 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.

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