glycine site

1-Aminocyclobutanecarboxylic acid (ACBC) is a NMDA receptor partial agonist. 1-Aminocyclobutanecarboxylic acid act at the glycine site, NR1[1].

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).

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

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.

Rapastinel acetate is a modulator of N-methyl-D-aspartate (NMDA) receptor and a partial agonist of glycine site long-lasting antidepressant effects.

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.

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

Rapastinel Trifluoroacetate (GLYX-13 Trifluoroacetate) is an NMDA receptor modulator with partial agonist properties at the glycine site.

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

5,7-Dichlorokynurenic acid (5,7-dichlorokynurenic acid sodium) is an NMDA receptor antagonist.

HA-966 HCl is an NMDA receptor complex glycine site antagonist.

RPR104632 is a novel and potent antagonist located at the NMDA glycine site with neuroprotective activity.

GV-196771 selectively antagonize the glycine-binding site of the NMDA ionophore.

Obestatin is a 23 amino acid peptide hormone with a conserved C-terminal glycine residue and amidation site that is formed by cleavage of the ghrelin and obestatin prepropeptide.1It binds to the orphan receptor GPR39 (Kd= 1 nM) and stimulates cAMP production in CHO and HEK293 cells overexpressing human GPR39. Obestatin inhibits contraction of isolated mouse jejunum muscle strips induced by ghrelin .In vivo, obestatin (12.5-1,000 nmol/kg) suppresses food intake in a time- and dose-dependent manner and reduces body weight gain and gastric emptying in mice. Obestatin (0.22 g per animal) also reduces food intake and glucose response without affecting plasma insulin responses in fasted high-fat diet fed mice.2 1.Zhang, J.V., Ren, P.C., Avsian-Kretchmer, O., et al.Obestatin, a peptide encoded by the ghrelin gene, opposes ghrelin's effects on food intakeScience310(5750)996-999(2005) 2.Subasinghage, A.P., Green, B.D., Flatt, P.R., et al.Metabolic and structural properties of human obestatin {1-23} and two fragment peptidesPeptides31(9)1697-1705(2010)

MDL 100748 is a glycine site antagonist of NMDA receptor.

HA-966 trihydrate is an NMDA receptor complex glycine site antagonist.

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].

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.

FN-A208 is an active peptide combining A208 from murine laminin a1 with the fibronectin active site GRGDS, linked by a glycine spacer. This compound self-assembles into amyloid-like fibrils and facilitates fibroblast cell adhesion through actin stress fiber formation, suggesting its use as a bioadhesive in tissue regeneration and engineering. FN-A208 targets IKVAV receptors and integrins, but its function can be inhibited by EDTA.

H-Arg-Gly-Asp-Cys-OH is a tetrapeptide that contains the arginine-glycine-aspartate (RGD) motif, a sequence that acts as a recognition site for various adhesion proteins.1It inhibits the binding of fibrinogen to endothelial cells and ADP-stimulated platelets with IC50values of 320 and 35 μM, respectively.2Implantation of titanium rods coated with H-Arg-Gly-Asp-Cys-OH increases bone formation in rat femurs.3H-Arg-Gly-Asp-Cys-OH has been conjugated to polyethylenimine to improve gene transfection efficiency.4 1.Park, H.S., Kim, C., and Kang, Y.K.Preferred conformations of RGDX tetrapeptides to inhibit the binding of fibrinogen to plateletsBiopolymers63(5)298-313(2002) 2.Tranqui, L., Andrieux, A., Hudry-Clergeon, G., et al.Differential structural requirements for fibrinogen binding to platelets and to endothelial cellsJ. Cell Biol.108(6)2519-2527(1989) 3.Ferris, D.M., Moodie, G.D., Dimond, P.M., et al.RGD-coated titanium implants stimulate increased bone formation in vivoBiomaterials20(23-24)2323-2331(1999) 4.Kunath, K., Merdan, T., Hegener, O., et al.Integrin targeting using RGD-PEI conjugates for in vitro gene transferJ. Gene Med.5(7)588-599(2003)

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.

GW-468816 is a glycine site NMDA receptor antagonist.

ACEA1011 is a glycine site NMDA receptor antagonist. It may have analgesic effects.

RGD-4C, an arginine-glycine-aspartic acid peptide (ACDCRGDCFC), exhibits integrin binding activity. The primary integrin recognition site in extracellular matrix proteins, the Arg-Gly-Asp (RGD) sequence, allows peptides with this sequence to mimic matrix proteins' recognition specificity. As an αv-integrin ligand, RGD-4C can be conjugated with bioactive molecules to demonstrate antitumor effects in animal models [1] [2] [3].

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).

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

GV-196771A A novel NMDA receptor glycine site antagonist with potent antinociceptive activity.

L-701252, a potent glycine site NMDA receptor antagonist, exhibits an inhibition concentration (IC50) of 420 nM. Additionally, it offers marginal neuroprotection against global cerebral ischemia.