Kynurenic acid, an endogenous tryptophan metabolite, is a broad-spectrum antagonist targeting NMDA, glutamate, α7 nicotinic acetylcholine receptor. Kynurenic acid is also a selective ligand of the GPR35 receptor.

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

MDL-29951 is a glycine antagonist of NMDA receptor activation (Ki=0.14 mM, [3H]glycine binding) in vitro and in vivo.

Spermidine, a precursor of spermine, is a polyamine derived from putrescine and could help stabilize some membranes and nucleic acid structures.

Mephenesin is a centrally acting muscle relaxant which may work as an NMDA receptor antagonist.

Rislenemdaz, also known as MK-0657, is a NR2B-selective NMDA antagonist potentially for the treatment of Parkinson's disease.

Budipine is an uncompetitive NMDAR antagonist used as an antiparkinson agent.

Rapastinel is a putative NMDAR functional glycine-site partial agonist.

NMDAR antagonist 1 is a NR2B-selective NMDAR antagonist.

7-Chlorokynurenic acid is an antagonist of NMDA receptor acting at the glycine site. It can also act as competitive inhibitor of L-glutamate transport into synaptic vesicles.

CIQ is a subunit-selective potentiator of NMDA receptors containing the NR2C or NR2D subunit.

D-AP5（D-APV）是一种选择性和竞争性的NMDA受体拮抗剂，其Kd为1.4 μM。D-AP5抑制了NMDA受体的谷氨酸位点的谷氨酸结合。

L-701324 is an orally active and long acting anticonvulsant with high affinity and selectivity for the glycine site on the NMDA receptor.

Gavestinel is a selective antagonist acting at the strychnine-insensitive glycine binding site of the NMDA receptor-channel complex with Kd of 0.8 nM.

Eliprodil can antogonize GluN2B-selective NMDA in a non-competitive manner with IC50 value of 1 μM. It is also a σ1 ligand with Ki value of 0.013 μM.

PEAQX 是一种强效且口服活性的 NMDA 拮抗剂，对人 NMDA 受体的 1A/2A（IC50 = 270 nM）具有 15 倍的优先性，而对 1A/2B 的 IC50 为 29,600 nM。

Traxoprodil a selective antagonist of the NR2B subunit of the NMDA receptor.

Dizocilpine maleate (MK-801 maleate)是一种高效、选择性和非竞争性的NMDA受体拮抗剂，在大鼠脑膜中的Kd为37.2 nM。

Radiprodil is a selective antagonist of NMDA NR2B that used in treatment of neuropathic pain.

Ibotenic acid has agonist activity at both the N-methyl-D-aspartate (NMDA) and trans-ACPD or metabolotropic quisqualate (Qm) receptor sites.