| S2876 |
(+)-Dizocilpine (MK 801) Maleate
|
(+)-Dizocilpine (MK 801) Maleate is a potent, selective and non-competitive NMDA receptor antagonist with Kd of 37.2 nM in rat brain membranes.(+)-Dizocilpine (MK 801) Maleate can be used to induce animal models of Schizophrenia. |
-
Theranostics, 2025, 15(14):6901-6918
-
Aging -Albany NY), 2023, 15(12):5698-5712
-
Aging (Albany NY), 2023, 15(12):5698-5712
|
|
| S7072 |
NMDA (N-Methyl-D-aspartic acid)
|
NMDA(N-Methyl-D-aspartic acid)is a specific agonist for NMDA receptor mimicking the action of glutamate, the neurotransmitter which normally acts at that receptor. Phase 4. |
-
Theranostics, 2025, 15(14):6901-6918
-
Sci Rep, 2025, 15(1):17364
-
J Neurotrauma, 2025, 10.1177/08977151251374286
|
|
| S1438 |
Topiramate
|
Topiramate (MCN 4853, RWJ 17021) is a mutil-targeted inhibitor, including voltage-gated sodium channel and calcium channel, AMPA/kainate receptor and carbonic anhydrase, used to treat epilepsy. |
-
J Headache Pain, 2025, 26(1):182
-
Commun Biol, 2025, 8(1):28
-
Cell Rep, 2022, 40(5):111153
|
|
| S4091 |
Ifenprodil Tartrate
|
Ifenprodil is an atypical noncompetitive antagonist at the NMDA receptor, it interacts with high affinity at a homogeneous population of NMDA receptors in neonatal rat forebrain with IC50 of 0.3 μM. |
-
J Immunother Cancer, 2024, 12(11)e009805
-
Cancer Sci, 2022, 113(8):2716-2726
-
Cancer Res, 2021, canres.1017.2021
|
|
| S2043 |
Memantine HCl
|
Memantine HCl is an antagonist of NMDAR. It is also a CYP2B6 and CYP2D6 inhibitor for recombinant CYP2B6 and CYP2D6 with IC50 of 1.12 μM and 242.4 μM, Ki of 0.51 μM and 84.4 μM, respectively. |
-
Pharmaceuticals (Basel), 2023, 16(5)692
-
Front Genet, 2022, 13:942203
-
FASEB J, 2020, 10.1096/fj.202000534R
|
|
| S1334 |
Flupirtine maleate
|
Flupirtine maleate is the salt form of Flupirtine, which is a centrally acting non-opioid analgesia, is a selective neuronal potassium channel opener that also has NMDA receptor antagonist properties. |
-
Assay Drug Dev Technol, 2019, 17(7):310-321
-
Elife, 2015, 4
|
|
| S6266 |
(S)-Glutamic acid
|
(S)-Glutamic acid (L-Glutamic acid) is an endogenous, non-selective glutamate receptor agonist. |
-
Cell Biosci, 2024, 14(1):135
-
Cancer Sci, 2022, 113-6:1955-1967
-
CHEM ENG J, 2021, 10.1016/j.cej.2021.130083
|
|
| S4821 |
Glycine
|
Glycine (2-Aminoacetic acid, Aminoacetic acid, Glycocoll) is a non-essential, non-polar, non-optical, glucogenic amino acid that is primarily found in gelatin and silk fibroin. It is involved in the body's production of DNA, phospholipids and collagen, and in release of energy. |
-
J Invest Dermatol, 2022, S0022-202X(22)00096-3
-
Free Radic Res, 2022, 1-13
|
|
| S2251 |
(-)-Huperzine A (HupA)
|
(-)-Huperzine A is a potent, highly specific and reversible inhibitor of acetylcholinesterase (AChE) with Ki of 7 nM, exhibiting 200-fold more selectivity for G4 AChE over G1 AChE. Also acts as an NMDA receptor antagonist. Phase 4. |
-
Acta Pharmacol Sin, 2019, 10.1038/s41401-018-0206-4
|
|
| S6906 |
Capric acid
|
Capric acid (DA, Decanoic acid, Decylic acid), a component of medium-chain triclycerides occurring naturally in coconut oil and palm kernel oil, contributes to seizure control through direct AMPA receptor inhibition. Capric acid is also a modulating ligand for PPARs. Due to its specific melting range the product may be solid, liquid, a solidified melt or a supercooled melt.
|
-
Pharmaceuticals (Basel), 2023, 16(5)692
|
|
| S5032 |
Mephenesin
|
Mephenesin (Decontractyl, Cresoxydiol, Memphenesin, Mephedan) is centrally acting muscle relaxant, a topical analgesic and may be an NMDA receptor antagonist. |
-
Cell Rep Methods, 2023, 3(10):100599
|
|
| S4721 |
L-Glutamic acid monosodium salt
|
L-Glutamic acid monosodium salt (Monosodium glutamate, MSG) is the sodium salt of glutamic acid, found naturally in tomatoes, cheese and other foods. |
-
Heliyon, 2024, 10(1):e23945
-
Acta Biomater, 2022, 152:255-272
|
|
| S1998 |
D-Cycloserine
|
D-cycloserine (RO-1-9213) is an analog of the amino acid D-alanine, used as an antibiotic in the treatment of tuberculosis. |
|
|
| S1281 |
Aniracetam
|
Aniracetam (RO 13-5057) is a nootropics and neuroprotective drug. |
|
|
| S3624 |
Quinolinic acid
|
Quinolinic Acid (pyridine-2,3-dicarboxylic acid, QUIN), a neuroactive metabolite of the kynurenine pathway, is an agonist of N-methyl-D-aspartate (NMDA) receptor.
|
|
|
| S0509 |
NMDAR antagonist 1
|
NMDAR antagonist 1 is a potent and orally bioavailable NR2B-selective antagonist of NMDAR. It has neuroprotective activity. |
|
|
| S5129 |
D-Aspartic acid
|
D-Aspartic acid (D-Asp, Aminosuccinic acid, asparagic acid, asparaginic acid) is an endogenous amino acid occurring in several tissues and cells of both invertebrates and vertebrates. It can regulate testosterone synthesis and may act on a stimulatory receptor (NMDA). |
|
|
| E1246 |
D-AP5
|
D-AP5 (D-APV; D-2-Amino-5-phosphonovaleric acid) is a selective and competitive NMDA receptor antagonist that inhibits the glutamate binding site of NMDA receptors. |
|
|
| E0484 |
CNQX
|
CNQX (6-cyano-7-nitroquinoxaline-2,3-dione) is an AMPA and kainate receptor antagonist with IC50 values are 0.3 μM and 1.5 μM for AMPA and kainate receptors, respectively. CNQX is also an antagonist at the glycine modulatory site on the NMDA receptor complex (IC50 = 25 μM). CNQX shows neuroprotective effects in models of ischemia and inhibits seizure-like activity in hippocampal neurons. |
|
|
| S4957 |
Linalool
|
Linalool (Phantol), a monoterpene compound commonly found as major component of essential oils of several aromatic species, is a competitive antagonist of NMDA receptors. |
|
|
| S3070 |
Piracetam
|
Piracetam (UCB 6215) is a cyclic derivative of the neurotransmitter gamma-aminobutyric acid (GABA), used in treatment of a wide range of cognitive disorders. |
|
|
| S6804 |
CX546
|
CX546, a prototypical ampakine agent, is a selective positive AMPA receptor modulator. |
|
|
| S4745 |
L-Phenylalanine
|
L-Phenylalanine is an essential amino acid and a competitive antagonist against NMDAR glycine- and glutamate-binding sites with a Kb of 573 μM. It is widely used in food flavor and pharmaceutical production. |
|
|
| S6907 |
Rapastinel (GLYX-13)
|
Rapastinel (GLYX-13, BV-102, TPPT-amide) is a partial agonist of N-methyl-D-aspartate receptor (NMDAR) that targeting a glycine site. Rapastinel has long-lasting antidepressant effects. |
|
|
| S6224 |
(R)-Serine
|
(R)-Serine is the R-enantiomer of serine, which is used in the biosynthesis of proteins. |
|
|
| E1050 |
PEAQX
|
PEAQX (NVP-AAM077) is an effective and orally available human NMDA antagonist, which shows preference in excess of 100-fold for hNMDA 1A/2A (IC50=of 270 nM) over hNMDA 1A/2B receptors (IC50=29,600 nM). |
|
|
| S5669 |
Isoxsuprine hydrochloride
|
Isoxsuprine hydrochloride is a beta-adrenergic agonist with vasodilator activity. |
|
|
| S5664 |
Orphenadrine Hydrochloride
|
Orphenadrine Hydrochloride is an uncompetitive NMDAR antagonist, H1 receptor antagonist and nonselective mAChR antagonist with muscle relaxant activity. |
|
|
| S9686 |
NBQX (FG9202)
|
NBQX (FG9202, NNC 079202) is a highly selective and competitive antagonist of AMPA receptor (AMPAR) with anti-epileptic effect. |
|
|
| S6803 |
1-BCP
|
1-BCP (Piperonylic acid piperidide) is a memory-enhancing agent that enhances AMPA-induced currents. |
|
|
| S4280 |
Meclofenoxate (Centrophenoxine) HCl
|
Meclofenoxate (Centrophenoxine) HCl is an anti-aging drug used to treat the symptoms of senile dementia and Alzheimer's disease, and also inhibits the activity of cholinephosphotransferase.
|
|
|
| E5887New |
Osavampator
|
Osavampator (TAK-653, NBI-1065845) is a positive allosteric modulator (PAM) of AMPA receptors. It enhances glutamate-induced calcium influx in CHO cells expressing human AMPA receptors with an EC50 of 3.3 µM and potentiates AMPA receptor-mediated currents in rat primary hippocampal neurons with an EC50 of 4.4 µM. |
|
|
| S7072 |
NMDA (N-Methyl-D-aspartic acid)
|
NMDA(N-Methyl-D-aspartic acid)is a specific agonist for NMDA receptor mimicking the action of glutamate, the neurotransmitter which normally acts at that receptor. Phase 4. |
-
Theranostics, 2025, 15(14):6901-6918
-
Sci Rep, 2025, 15(1):17364
-
J Neurotrauma, 2025, 10.1177/08977151251374286
|
|
| S6266 |
(S)-Glutamic acid
|
(S)-Glutamic acid (L-Glutamic acid) is an endogenous, non-selective glutamate receptor agonist. |
-
Cell Biosci, 2024, 14(1):135
-
Cancer Sci, 2022, 113-6:1955-1967
-
CHEM ENG J, 2021, 10.1016/j.cej.2021.130083
|
|
| S4721 |
L-Glutamic acid monosodium salt
|
L-Glutamic acid monosodium salt (Monosodium glutamate, MSG) is the sodium salt of glutamic acid, found naturally in tomatoes, cheese and other foods. |
-
Heliyon, 2024, 10(1):e23945
-
Acta Biomater, 2022, 152:255-272
|
|
| S3624 |
Quinolinic acid
|
Quinolinic Acid (pyridine-2,3-dicarboxylic acid, QUIN), a neuroactive metabolite of the kynurenine pathway, is an agonist of N-methyl-D-aspartate (NMDA) receptor.
|
|
|
| S3070 |
Piracetam
|
Piracetam (UCB 6215) is a cyclic derivative of the neurotransmitter gamma-aminobutyric acid (GABA), used in treatment of a wide range of cognitive disorders. |
|
|
| S6907 |
Rapastinel (GLYX-13)
|
Rapastinel (GLYX-13, BV-102, TPPT-amide) is a partial agonist of N-methyl-D-aspartate receptor (NMDAR) that targeting a glycine site. Rapastinel has long-lasting antidepressant effects. |
|
|
| S6224 |
(R)-Serine
|
(R)-Serine is the R-enantiomer of serine, which is used in the biosynthesis of proteins. |
|
|
| S5669 |
Isoxsuprine hydrochloride
|
Isoxsuprine hydrochloride is a beta-adrenergic agonist with vasodilator activity. |
|
|
| S6803 |
1-BCP
|
1-BCP (Piperonylic acid piperidide) is a memory-enhancing agent that enhances AMPA-induced currents. |
|
|
| S2876 |
(+)-Dizocilpine (MK 801) Maleate
|
(+)-Dizocilpine (MK 801) Maleate is a potent, selective and non-competitive NMDA receptor antagonist with Kd of 37.2 nM in rat brain membranes.(+)-Dizocilpine (MK 801) Maleate can be used to induce animal models of Schizophrenia. |
- Theranostics, 2025, 15(14):6901-6918
- Aging -Albany NY), 2023, 15(12):5698-5712
- Aging (Albany NY), 2023, 15(12):5698-5712
|
|
| S4091 |
Ifenprodil Tartrate
|
Ifenprodil is an atypical noncompetitive antagonist at the NMDA receptor, it interacts with high affinity at a homogeneous population of NMDA receptors in neonatal rat forebrain with IC50 of 0.3 μM. |
- J Immunother Cancer, 2024, 12(11)e009805
- Cancer Sci, 2022, 113(8):2716-2726
- Cancer Res, 2021, canres.1017.2021
|
|
| S2043 |
Memantine HCl
|
Memantine HCl is an antagonist of NMDAR. It is also a CYP2B6 and CYP2D6 inhibitor for recombinant CYP2B6 and CYP2D6 with IC50 of 1.12 μM and 242.4 μM, Ki of 0.51 μM and 84.4 μM, respectively. |
- Pharmaceuticals (Basel), 2023, 16(5)692
- Front Genet, 2022, 13:942203
- FASEB J, 2020, 10.1096/fj.202000534R
|
|
| S1334 |
Flupirtine maleate
|
Flupirtine maleate is the salt form of Flupirtine, which is a centrally acting non-opioid analgesia, is a selective neuronal potassium channel opener that also has NMDA receptor antagonist properties. |
- Assay Drug Dev Technol, 2019, 17(7):310-321
- Elife, 2015, 4
|
|
| S5032 |
Mephenesin
|
Mephenesin (Decontractyl, Cresoxydiol, Memphenesin, Mephedan) is centrally acting muscle relaxant, a topical analgesic and may be an NMDA receptor antagonist. |
- Cell Rep Methods, 2023, 3(10):100599
|
|
| S0509 |
NMDAR antagonist 1
|
NMDAR antagonist 1 is a potent and orally bioavailable NR2B-selective antagonist of NMDAR. It has neuroprotective activity. |
|
|
| E1246 |
D-AP5
|
D-AP5 (D-APV; D-2-Amino-5-phosphonovaleric acid) is a selective and competitive NMDA receptor antagonist that inhibits the glutamate binding site of NMDA receptors. |
|
|
| E0484 |
CNQX
|
CNQX (6-cyano-7-nitroquinoxaline-2,3-dione) is an AMPA and kainate receptor antagonist with IC50 values are 0.3 μM and 1.5 μM for AMPA and kainate receptors, respectively. CNQX is also an antagonist at the glycine modulatory site on the NMDA receptor complex (IC50 = 25 μM). CNQX shows neuroprotective effects in models of ischemia and inhibits seizure-like activity in hippocampal neurons. |
|
|
| S4957 |
Linalool
|
Linalool (Phantol), a monoterpene compound commonly found as major component of essential oils of several aromatic species, is a competitive antagonist of NMDA receptors. |
|
|
| S4745 |
L-Phenylalanine
|
L-Phenylalanine is an essential amino acid and a competitive antagonist against NMDAR glycine- and glutamate-binding sites with a Kb of 573 μM. It is widely used in food flavor and pharmaceutical production. |
|
|
| E1050 |
PEAQX
|
PEAQX (NVP-AAM077) is an effective and orally available human NMDA antagonist, which shows preference in excess of 100-fold for hNMDA 1A/2A (IC50=of 270 nM) over hNMDA 1A/2B receptors (IC50=29,600 nM). |
|
|
| S5664 |
Orphenadrine Hydrochloride
|
Orphenadrine Hydrochloride is an uncompetitive NMDAR antagonist, H1 receptor antagonist and nonselective mAChR antagonist with muscle relaxant activity. |
|
|
| S9686 |
NBQX (FG9202)
|
NBQX (FG9202, NNC 079202) is a highly selective and competitive antagonist of AMPA receptor (AMPAR) with anti-epileptic effect. |
|
|