NMDA Receptors

NMDA receptors are members of the ionotropic class of glutamate receptors, which also includes Kainate and AMPA receptors. NMDA receptors consist of NR1 subunits combined with NR2 (A-D) or NR3 (A-B) subunits. The ligand-gated channel is permeable to cations.

Products
Background
Literature
Gene Data

Agonists

Cat No Product Name / Activity
0186 cis-ACPD
Potent NMDA agonist. Also group II mGluR agonist
0213 D-Aspartic acid
NMDA agonist
0214 L-Aspartic acid
NMDA agonist
0216 L-Cysteinesulfinic acid
NMDA and mGlu agonist
3406 GLYX 13
NMDA receptor partial agonist; acts at the glycine site
0281 (R)-(+)-HA-966
NMDA partial agonist/antagonist; acts at glycine site
0197 Homoquinolinic acid
Selective, potent NMDA agonist
0285 Ibotenic acid
Non-selective NMDA agonist
2277 MNI-caged-D-aspartate
Caged D-aspartate; NMDA agonist
0114 NMDA
Selective NMDA agonist
0225 Quinolinic acid
Endogenous NMDA agonist and transmitter candidate
0959 Spermidine trihydrochloride
Agonist at polyamine site
0312 (RS)-(Tetrazol-5-yl)glycine
Highly potent NMDA receptor agonist

Antagonists

Cat No Product Name / Activity
0258 ACBC
NMDA antagonist, acts at glycine site
3693 DL-AP5 Sodium salt
Sodium salt of DL-AP5 (Cat. No. 0105)
0106 D-AP5
Potent, selective NMDA antagonist; more active form of DL-AP5 (Cat. No. 0105)
0105 DL-AP5
Potent, selective NMDA antagonist
0107 L-AP5
Potent, selective NMDA antagonist. Less active form of DL-AP5 (Cat. No. 0105)
0104 DL-AP7
Selective NMDA antagonist
0389 Arcaine sulfate
Competitive NMDA antagonist
0322 (R)-4-Carboxyphenylglycine
Moderately potent NMDA antagonist
4492 Cerestat
Potent and noncompetitive NMDA receptor antagonist
1469 CGP 37849
Potent and selective NMDA antagonist
1409 CGP 39551
Potent, selective and competitive NMDA antagonist
1493 CGP 78608 hydrochloride
Potent, selective glycine-site NMDA antagonist
1241 CGS 19755
Potent, competitive NMDA antagonist
3697 7-Chlorokynurenic acid sodium salt
Sodium salt of 7-Chlorokynurenic acid (Cat. No. 0237)
0237 7-Chlorokynurenic acid
NMDA antagonist, acts glycine site
0817 (2R,3S)-Chlorpheg
Weak NMDA antagonist
0190 CNQX
NMDA antagonist, acts glycine site. Also AMPA/kainate antagonist
2456 Co 101244 hydrochloride
Highly selective NR2B antagonist
4136 Conantokin G
NR2B-selective NMDA receptor antagonist
3125 Conantokin-R
Potent non-competitive NMDA receptor antagonist
3122 Conantokin-T
Non-competitive NMDA receptor antagonist
0247 (R)-CPP
Potent NMDA antagonist; more active enantiomer of (RS)-CPP (Cat. No. 0173)
0173 (RS)-CPP
Potent NMDA antagonist
1265 D-CPP-ene
Potent, competitive NMDA antagonist
3071 Dextromethorphan hydrobromide
NMDA receptor antagonist
0286 5,7-Dichlorokynurenic acid
Potent NMDA antagonist, acts at glycine site
3698 5,7-Dichlorokynurenic acid sodium salt
Sodium salt of 5,7-Dichlorokynurenic acid (Cat. No. 0286). Potent NMDA antagonist, acts at glycine site
0360 (±)-1-(1,2-Diphenylethyl)piperidine maleate
NMDA antagonist, acts ion channel site
4491 DQP 1105
Selective NR2C/NR2D receptor antagonist
2195 Eliprodil
Non-competitive NR2B-selective NMDA antagonist
0869 Felbamate
NMDA antagonist, acts glycine site
2867 Flupirtine maleate
Indirect NMDA receptor antagonist
2348 Gavestinel
Potent and selective glycine site antagonist; orally available and active in vivo
0282 (S)-(-)-HA-966
NMDA antagonist/partial agonist
2861 HU 211
NMDA receptor antagonist; also NF-κB inhibitor
0290 N-(4-Hydroxyphenylacetyl)spermine
Wasp toxin analog
0545 Ifenprodil hemitartrate
Non-competitive NMDA antagonist. Also σ ligand
2892 threo Ifenprodil hemitartrate
NR2B-selective NMDA antagonist; also σ agonist
3131 Ketamine hydrochloride
Non-competitive NMDA receptor antagonist
4379 (S)-(+)-Ketamine hydrochloride
NMDA receptor antagonist; enantiomer of ketamine hydrochloride (Cat. No. 3131)
0742 L-689,560
Very potent NMDA antagonist
0705 L-701,252
NMDA antagonist, acts glycine site
0907 L-701,324
NMDA antagonist; acts at glycine site
0840 Loperamide hydrochloride
NMDA antagonist, reduces Ca2+ flux
1521 LY 233053
Competitive NMDA receptor antagonist
1019 LY 235959
Competitive NMDA antagonist
0773 Memantine hydrochloride
NMDA antagonist; acts at ion channel site
0924 (+)-MK 801 maleate
Non-competitive NMDA antagonist; acts at ion channel site
0955 (-)-MK 801 maleate
NMDA antagonist, less active enantiomer
1970 Norketamine hydrochloride
Potent, non-competitive NMDA antagonist
4230 NPEC-caged-D-AP5
Caged D-AP5 (Cat.No. 0106); NMDA antagonist
5018 PEAQX tetrasodium salt
Potent NMDA receptor antagonist; NR2A selective
3277 Pentamidine isethionate
Antimicrobial that antagonizes NMDA receptors
2557 Phencyclidine hydrochloride
Non-competitive NMDA receptor antagonist
2273 PMPA (NMDA antagonist)
Competitive NMDA antagonist
2530 PPDA
Subtype-selective NR2C/NR2D antagonist
2274 PPPA
Competitive NR2A antagonist
4801 QNZ 46
NR2C/NR2D-selective NMDA receptor non-competitive antagonist
1622 Remacemide hydrochloride
NMDA antagonist; blocks ion channel and allosteric modulatory site
2005 Ro 04-5595 hydrochloride
NR2B-selective NMDA antagonist
1594 Ro 25-6981 maleate
NR2B-selective NMDA antagonist
3254 Ro 61-8048
NMDA antagonist; increases kynurenic acid levels
3343 Ro 8-4304 hydrochloride
NR2B-selective NMDA antagonist
1251 SDZ 220-040
Potent, competitive NMDA antagonist
1250 SDZ 220-581
Competitive NMDA antagonist
0635 Synthalin sulfate
Non-competitive NMDA antagonist
4154 TCN 201
Selective NR1/NR2A receptor antagonist
4163 TCN 213
NMDA antagonist; selective for NR2A over NR2B
4072 TCN 237 dihydrochloride
Highly potent and selective NR2B antagonist
2782 TCS 46b
Orally active, subtype-selective NR1A/NR2B antagonist
3322 ZD 9379
Brain penetrant NMDA antagonist; acts at glycine site

Ligand-sets

Cat No Product Name / Activity
1825 Mixed NMDA Receptor Tocriset™
Selection of 5 mixed NMDA receptor ligands (Cat. Nos. 0114, 0312, 0106, 0924 and 1241)
1823 NMDA Receptor - Glycine Site Tocriset™
Selection of 5 NMDA receptor (glycine site) ligands (Cat. Nos. 0219, 0281, 0742, 1493 and 0237)

Other

Cat No Product Name / Activity
1238 CCMQ
Used to characterize NR2B-containing NMDA receptors
4105 CIQ
Potentiator of NMDA receptors containing NR2C/NR2D
0219 Glycine
Endogenous potentiator, co-transmitter
6095 2S,6S-Hydroxynorketamine hydrochloride
Ketamine metabolite; decreases D-serine (a NMDA co-agonist); antidepressant
1636 IEM 1460
Open-channel blocker of NMDA currents. Also blocks AMPA currents
2224 MNI-caged-NMDA
Caged NMDA
2213 N20C hydrochloride
Non-competitive NMDA receptor open-channel blocker
2851 Nefiracetam
Cognitive enhancer; potentiates NMDA currents
5996 (R)-Norketamine hydrochloride
NMDA receptor modulator; metabolite of Ketamine hydrochloride (Cat. No.3131).
6112 (S)-Norketamine hydrochloride
NMDA receptor modulator; metabolite of Ketamine hydrochloride (Cat. No.3131)
5376 Pregnenolone sulfate sodium salt
NMDA Potentiator
0226 D-Serine
Potentiator, acts at glycine site
0958 Spermine tetrahydrochloride
Modulator at polyamine site

NMDA receptors are members of the ionotropic class of glutamate receptors, which also includes Kainate and AMPA receptors. NMDA receptors consist of NR1 subunits combined with one or more NR2 (A-D) or NR3 (A-B) subunits. The ligand-gated channel is permeable to cations including Ca2+, and at resting membrane potentials NMDA receptors are inactive due to a voltage-dependent blockade of the channel pore by Mg2+.

External sources of pharmacological information for NMDA Receptors :

    Literature for NMDA Receptors

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    NMDA Receptor Gene Data

    Gene Species Gene Symbol Gene Accession No. Protein Accession No.
    GluN1 Human GRIN1 NM_021569 Q05586
    Mouse Grin1 NM_008169 P35438
    Rat Grin1 NM_017010 P35439
    GluN2A Human GRIN2A NM_000833 Q12879
    Mouse Grin2a NM_008170 P35436
    Rat Grin2a NM_012573 Q00959
    GluN2B Human GRIN2B NM_000834 Q13224
    Mouse Grin2b NM_008171 Q01097
    Rat Grin2b NM_012574 Q00960
    GluN2C Human GRIN2C NM_000835 Q14957
    Mouse Grin2c NM_010350 Q01098
    Rat grin2c NM_012575 Q00961
    GluN2D Human GRIN2D NM_000836 O15399
    Mouse Grin2d NM_008172 Q03391
    Rat Grin2d NM_022797 Q62645
    GluN3A Human GRIN3A NM_133445 Q8TCU5
    Mouse Grin3a NM_001033351 NP_001028523
    Rat Grin3a AF073379 Q9R1M7
    GluN3B Human GRIN3B NM_138690 O60391
    Mouse Grin3b NM_130455 Q91ZU9
    Rat Grin3b NM_133308 Q8VHN2