glycine site of the nmda receptor

(R)-(+)-HA-966 ((+)-HA-966) is a partial agonist/antagonist of glycine site of the N-methyl-D-aspartate (NMDA) receptor complex. (R)-(+)-HA-966 selectively blocks the activation of the mesolimbic dopamine system by amphetamine, has the potential for neuro

7-Chlorokynurenic acid (7-chloro-4-hydroxy-2-carboxyquinoline) is an effecitve and selective antagonist of NMDA receptor with IC50 of 0.56 μM for the glycine B coagonist site. 7-Chlorokynurenic acid inhibits the reuptake of glutamate into synaptic vesicles with a Ki of 0.59 μM and shows antinociceptive actions after neuraxial delivery.

CGP 78608 hydrochloride is a specific antagonist at the glycine binding site of the NMDA receptor (IC50 = 6 nM). CGP 78608 hydrochloride exhibits anticonvulsant activity. CGP 78608 hydrochloride potentiates GluN1/GluN3A-mediated glycine currents (estimated EC50 = 26.3 nM).

AV-101 (4-Cl-KYN) , a prodrug antagonist at the glycine site of the NMDA receptor, has antidepressant activity and reduces levodopa-induced dyskinesia in MPTP monkeys.

Neboglamine (CR-2249, XY-2401) hydrochloride, an orally active positive modulator of the NMDA receptor glycine site, can be used in schizophrenia research [1].

1-Aminocyclopropane-1-carboxylic acid (ACC) is an intermediate in the synthesis of ethylene, the plant hormone responsible for biological processes ranging from seed germination to organ senescence. It is a small molecule agonist at the glycine modulatory site of the NMDA receptor (EC50 = 0.7-0.9 μM) in the presence of low levels (1 μM) of glutamate and as a competitive antagonist at the glutamate-binding site on NMDA receptors (EC50 = 81.6 nM) with high levels (10 μM) of glutamate.2 This compound has been reported to protect against neuron cell death in vivo models of ischemia by enabling moderate levels of NMDA receptor activation and attenuating any excess NMDA receptor signaling that may lead to neurotoxicity.

Indole-2-carboxylic acid is an indole carboxylic acid compound with multi-target biological activity, exhibiting neuroprotective, antiviral, and antioxidant properties. Indole-2-carboxylic acid is a competitive antagonist at the glycine site of the NMDA receptor (Ki = 15 μM). Indole-2-carboxylic acid specifically inhibits the potentiating effect of glycine on NMDA-gated currents, blocking the neurotoxicity caused by excessive NMDA receptor activation, and can be used in research on the treatment of neurodegenerative diseases and cerebral ischemic injury. Indole-2-carboxylic acid is also an HIV-1 integrase inhibitor; it interferes with the integration of viral DNA into the host genome and can be used in the development of anti-HIV drugs.

7-Chlorokynurenic acid sodium salt (7-CKA sodium salt) is a potent and selective antagonist of the glycine B coagonist site of the NMDA receptor (IC50: 0.56 μM) and a potent inhibitor of the reuptake of glutamate into synaptic vesicles (Ki: 0.59 μM).

L-689560 is widely used as a radiolabeled ligand in binding studies and used to study the roles of NMDA receptors in normal neurological processes as well as in diseases. At the GluN1 glycine binding site, L-689560 is an effective N-methyl-D-aspartate (NM

MDL 105519 is a selective, non-competitive antagonist at the glycine site of NMDA receptors. It inhibits cyclic GMP accumulation in brain slices, modulates Ca²⁺ and Na⁺-Ca²⁺ currents, and exhibits anxiolytic activity in rat models.

Boc-D-2,3-diaminopropionic acid (N-t-Boc-amino-D-alanine) is a derivative of an amino acid featuring a Boc protecting group. It is utilized in the synthesis of a powerful NMDA receptor glycine site agonist that exhibits specific activity towards the GluN2 subunit.

Gavestinel (GV 150526) is a non-competitive NMDA receptor antagonist that is potent, selective and orally active.Gavestinel binds to the glycine site of the NMDA receptor with a binding affinity (pKi value) of 8.5.Gavestinel is used in acute ischaemic stroke studies.

CGP-78608 is a glycine site-specific N-methyl-D-aspartate receptor antagonist prevents activation of the NMDA/NO/CGMP pathway by ammonia.

NMDA Receptor Antagonist 6 (Compound 13b) functions as an antagonist at the glycine-binding site of the NMDA receptor and demonstrates cytoneuroprotective efficacy. It safeguards PC12 cells from NMDA-induced damage and apoptosis [1].