DGIdb - GRIN1 Gene Record

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:

Trial Name	memantine
Novel drug target	Established target
Trial Name	Namenda

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

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

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

Trial Name	neramexane mesylate
Novel drug target	Established target

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

Trial Name	dimiracetam, NT-11624
Novel drug target	Established target

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

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

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

binder
antagonist (inhibitory)

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

Trial Name	dexanabinol, HU-211
Novel drug target	Established target

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

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

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

GRIN1	DrugBank Gene Name
Q05586	UniProt Accession
2902	Entrez Gene Id

NMDAR1	GENE_SYMBOL
GRIN1	GENE_SYMBOL
Glutamate receptor ionotropic, NMDA 1	UNIPROT

Glutamate receptor ionotropic, NMDA 1	Gene Name
Q05586	UniProt ID

GRIN1 Gene Record

GRIN1 2902 Druggable Genome

Alternate Names:

Gene Info:

Gene Categories: Category Details

Publications:

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 2843389 2170997 10592235 2556198

Sources: DrugBank

Interaction Types & Directionality: blocker (inhibitory)

Interaction Info:

PMIDs: 22261381

Sources: DrugBank

Interaction Types & Directionality: antagonist (inhibitory)

Interaction Info:

PMIDs: 16340185

Sources: DrugBank

Interaction Types & Directionality: ligand

Interaction Info:

PMIDs: None found

Sources: DrugBank

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 10592235

Sources: DrugBank

Interaction Types & Directionality: antagonist (inhibitory)

Interaction Info: Novel drug target Established target Trial Name -

PMIDs: 17139284 17016423 8788072

Sources: TEND TdgClinicalTrial DrugBank

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

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

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 20873775

Sources: DTC

Interaction Types & Directionality: antagonist (inhibitory)

Interaction Info:

PMIDs: 22346357 18540918

Sources: DrugBank

Interaction Types & Directionality: antagonist (inhibitory)

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

PMIDs: None found

Sources: ChemblInteractions

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info:

PMIDs: 22716121 7636857

Sources: DrugBank

Interaction Types & Directionality: antagonist (inhibitory)

Interaction Info:

PMIDs: 3365283

Sources: DrugBank

Interaction Types & Directionality: antagonist (inhibitory)

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

PMIDs: None found

Sources: ChemblInteractions

Interaction Types & Directionality: antagonist (inhibitory)

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

PMIDs: None found

Sources: ChemblInteractions

Interaction Types & Directionality: antagonist (inhibitory)

Interaction Info:

PMIDs: 7624018

Sources: DrugBank

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

Interaction Types & Directionality: antagonist (inhibitory)

Interaction Info:

PMIDs: 23825891

Sources: DrugBank

Interaction Types & Directionality: n/a

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

Interaction Types & Directionality:

n/a

PMIDs:
2843389 2170997 10592235 2556198

Sources:
DrugBank

Interaction Types & Directionality:

blocker (inhibitory)

PMIDs:
22261381

Sources:
DrugBank

Interaction Types & Directionality:

antagonist (inhibitory)

PMIDs:
16340185

Sources:
DrugBank

Interaction Types & Directionality:

ligand

PMIDs:
None found

Sources:
DrugBank

Interaction Types & Directionality:

n/a

PMIDs:
10592235

Sources:
DrugBank

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Novel drug target Established target

Trial Name -

PMIDs:
17139284 17016423 8788072

Sources:
TEND TdgClinicalTrial DrugBank

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

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

Interaction Types & Directionality:

n/a

PMIDs:
20873775

Sources:
DTC

Interaction Types & Directionality:

antagonist (inhibitory)

PMIDs:
22346357 18540918

Sources:
DrugBank

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Mechanism of Interaction Glutamate NMDA receptor; GRIN1/GRIN2B antagonist

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions

Interaction Types & Directionality:

inhibitor (inhibitory)

PMIDs:
22716121 7636857

Sources:
DrugBank

Interaction Types & Directionality:

antagonist (inhibitory)

PMIDs:
3365283

Sources:
DrugBank

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Mechanism of Interaction Glutamate NMDA receptor; GRIN1/GRIN2B antagonist

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Glutamate NMDA receptor; GRIN1/GRIN2B antagonist

PMIDs:
None found

Sources:
ChemblInteractions

Interaction Types & Directionality:

antagonist (inhibitory)

PMIDs:
7624018

Sources:
DrugBank

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

Interaction Types & Directionality:

antagonist (inhibitory)

PMIDs:
23825891

Sources:
DrugBank

Interaction Types & Directionality:

n/a

Interaction Info:

Trial Name neramexane mesylate

Novel drug target Established target

PMIDs:
None found

Sources:
TdgClinicalTrial

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
TTD

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Mechanism of Interaction Glutamate NMDA receptor; GRIN1/GRIN2B antagonist

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions

Interaction Types & Directionality:

n/a

PMIDs:
20361801

Sources:
DTC

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Glutamate [NMDA] receptor negative allosteric modulator

PMIDs:
29392371

Sources:
DrugBank ChemblInteractions

Interaction Types & Directionality:

partial agonist (activating)