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 is an antagonist of NMDA receptor (N-methyl-D-aspartate receptor).

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

NMDA-IN-1 is a potent and NR2B-selective NMDA antagonist with Ki of 0.85 nM. Its NR2B Ca2+ influx IC50 is 9.7 nM without activities on NR2A, NR2C, NR2D, hERG-channel and α1-adrenergic 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.

TCN-201 is a sulphonamide derivative that negatively modulates glycine binding to the GluN1 (glutamate receptor subunit) subunit of the receptor.

PEAQX is a potent and orally active NMDA antagonist with a 15-fold preference for human NMDA receptors with the 1A/2A (IC50=270 nM), rather than 1A/2B(29,600 nM).

Trans-crocetin sodium, also known as Transcrocetinate sodium or Sodium crocetinate, is potentially for the treatment of glioblastoma. Trans-crocetin improves amyloid-β degradation in monocytes from Alzheimer's Disease patients. trans-crocetin inhibit glutamatergic synaptic transmission in rat cortical brain slices. Crocetin inhibits invasiveness of MDA-MB-231 breast cancer cells via downregulation of matrix metalloproteinases.

NMDA and mGlu agonist.

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

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

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

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