glycine receptor

Urethane (Ethylurethane) was an antineoplastic agent .Now is used for other medicinal purposes.

Halothane (Anestan) is a nonflammable, halogenated, hydrocarbon anesthetic that provides relatively rapid induction with little or no excitement. Analgesia may not be adequate. NITROUS OXIDE is often given concomitantly. Because halothane may not produce sufficient muscle relaxation, supplemental neuromuscular blocking agents may be required.

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).

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

UK-240455 is a potent and selective N-methyl-D-aspartic acid (NMDA) glycine receptor antagonist with neuroprotective effects and improvements in motor function in Parkinson's disease models, making it a potential candidate for Parkinson's disease treatment.

PAOPA is a novel dopamine D2 receptor modulator and L-proline-L-leucine-glycine amide (PLG) peptide mimetic that prevents and reverses behavioral and biochemical abnormalities in preclinical animal models of schizophrenia sensitized to amphetamine. PAOPA has been used in the study of schizophrenia and extrapyramidal dysfunction.

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

Alanine is a nonessential amino acid made in the body from the conversion of the carbohydrate pyruvate or the breakdown of DNA and the dipeptides carnosine and anserine. D-Alanine ((R)-Alanine) is a weak GlyR (inhibitory glycine receptor) and PMBA agonist, with an EC50 of 9 mM for GlyR.

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

Cycloleucine is an antagonist of NMDA receptor associated glycine receptor with a Ki of 600 μM. Cycloleucine is also a competitive inhibitor of S-adenosyl-methionine mediated methylation with anxiolytic and cytostatic effects.

glycine (2-Aminoacetic acid) is a non-essential amino acid. It is found primarily in gelatin and silk fibroin and used therapeutically as a nutrient. It is also a fast inhibitory neurotransmitter.

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

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

Org 25543 is the development of an N-Acyl amino acid that selectively inhibits the glycine transporter 2 to produce analgesia in a rat model of chronic pain.

TCN 213 is an antagonist of NMDA receptor that has a selective for NR1 NR2A over NR1 NR2B

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).

Ifenprodil (RC61-91) is an inhibitor of the NMDA receptor, specifically of GluN1 (glycine-binding NMDA receptor subunit 1) and GluN2B (glutamate-binding NMDA receptor subunit 2) subunits. Additionally, Ifenprodil inhibits GIRK channels and interacts with alpha1 adrenergic, serotonin, and sigma receptors.

N-Oleoyl Glycine, a Lipoamino Acid, Stimulates Adipogenesis Associated With Activation of CB1 Receptor and Akt Signaling Pathway in 3T3-L1 Adipocyte

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 an effective antagonist of glycine binding to the NMDA receptor.