NMDA receptor 选择性拮抗剂

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.

D-Alanine

D-alanine (Ala, (R)-Alanine, Ba 2776, D-α-Alanine, NSC 158286) is an endogenous co-agonist at the glycine site of the N-methyl-d-aspartate (NMDA) receptor.

Deudextromethorphan (AVP-786)

Deudextromethorphan (AVP-786) is an active N-methyl-D-aspartate (NMDA) receptor antagonist.

Mephenesin

Mephenesin (Decontractyl, Cresoxydiol, Memphenesin, Mephedan) is centrally acting muscle relaxant, a topical analgesic and may be an NMDA receptor antagonist.

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.

6-Methoxy-2-naphthoic acid

6-Methoxy-2-naphthoic acid (6-Methoxy-2-naphthalenecarboxylic acid) is an modulator of NMDAR.

Tiletamine Hydrochloride

Tiletamine is a lipophilc and potent vetrinary anesthetic. It is also a NMDA receptor antagonist.

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.

(-)-Dizocilpine (MK 801) Maleate

(-)-Dizocilpine (MK 801, Dizocilpine, C13737) Maleate is a potent N-methyl-D-aspartate (NMDA) receptor antagonist with K_i of 30.5 nM.

(+)-Dizocilpine (MK 801) Maleate

(+)-Dizocilpine (MK 801) Maleate is a potent, selective and non-competitive NMDA receptor antagonist with K_d of 37.2 nM in rat brain membranes.

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.

NMDAR antagonist 1

NMDAR antagonist 1 is a potent and orally bioavailable NR2B-selective antagonist of NMDAR. It has neuroprotective activity.

Procaine HCl

Procaine (Novocaine) is an inhibitor of sodium channel, NMDA receptor and nAChR with IC50 of 60 μM, 0.296 mM and 45.5 μM, which is also an inhibitor of 5-HT3 with K_D of 1.7 μM.

Felbamate

Felbamate (Felbatol, ADD-03055,W-554) is an anticonvulsant drug used in the treatment of epilepsy; NMDAR antagonist.

Sarcosine

Sarcosine (N-methylglycine, Sarcosinic acid, Methylaminoacetic acid, Methylglycine) is a competitive inhibitor of the type I glycine transporter (GlyT1) and an N-methyl-D-aspartate receptor (NMDAR) co-agonist.

Kynurenic acid

Kynurenic acid (Quinurenic acid, Kynurenate), a natural metabolite of tryptophan via the kynurenine pathway, is a broad-spectrum excitatory amino acid antagonist; It proved to be an antagonist at NMDA, kainate and AMPA receptors.

Spermidine trihydrochloride

Spermidine (4-Azaoctamethylenediamine), a natural polyamine produced from putrescine and decarboxylated S-adenosylmethionine (dcSAM) by spermidine synthase, is a novel autophagy inducer and negatively modulates N-methyl-d-aspartate (NMDA).

Eliprodil (SL-820715)

Eliprodil (SL-820715) is a non-competitive NR2B-selective NMDA antagonist with IC50 value of 1 μM and is less potent for NR2A- and NR2C-containing receptors with IC50 > 100 μM.

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.

Riluzole (PK 26124)

Riluzole (PK 26124, RP-54274) is a glutamate release inhibitor with neuroprotective, anticonvulsant, anxiolytic and anesthetic qualities.

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.