GlyT1 Inhibitor

Bitopertin is a potent, noncompetitive glycine reuptake inhibitor, inhibits glycine uptake at human GlyT1 with a concentration exhibiting IC50 of 25 nM.

Sarcosine (N-Methylglycine), an endogenous amino acid, is a competitive glycine transporter type I (GlyT1) inhibitor and N-methyl-D-aspartate (NMDA) receptor co-agonist. Sarcosine increases the glycine concentration, resulting in an indirect potentiation of the NMDA receptor. Sarcosine is commonly used for the research of schizophrenia.

Iclepertin (BI-425809) is a potent, selective and orally active glycine transporter 1 (GlyT1) inhibitor. Iclepertin is inactive against GlyT2. Iclepertin can be used for Alzheimer disease and schizophrenia research.

Sarcosine-d₃ is the deuterium labeled Sarcosine. Sarcosine (N-Methylglycine), an endogenous amino acid, is a competitive glycine transporter type I (GlyT1) inhibitor and N-methyl-D-aspartate (NMDA) receptor co-agonist. Sarcosine increases the glycine concentration, resulting in an indirect potentiation of the NMDA receptor. Sarcosine is commonly used for the research of schizophrenia.

PF-03463275 is a centrally penetrant, orally available, selective, and competitive GlyT1 (glycine transporter-1) reversible inhibitor, with a K_i of 11.6 nM. PF-03463275 has the potential for Schizophrenia research.

Org 24461 is a selective and brain-penetrant GlyT-1 inhibitor. Org 24461 blocks glycine uptake, reuptake, reverse operation, [³H]glycine efflux and release. Org 24461 enhances NMDA receptor function, modulates striatal monoamine/glutamate levels, and reverses PCP-induced behavioral and electrographic abnormalities. Org 24461 can be used for the research of retinal hypoxia/ischemia, and schizophrenia.

GlyT1 Inhibitor 1 is a potent and selective GlyT1 inhibitor with an IC₅₀ of 38 nM for rGlyT1. Antipsychotic activity.

SSR504734 is an orally active, selective and reversible inhibitor of human, rat, and mouse GlyT1 (IC₅₀=18, 15, and 38 nM, respectively). SSR504734 shows anti-schizophrenia, anti-anxiety and anti-depression activities.

LY2365109 hydrochloride is a potent and selective GlyT1 inhibitor, with an IC₅₀ of 15.8 nM for glycine uptake in cells over-expressing hGlyT1a.

NFPS is a selective, non-competitive glycine transporter-1 (GlyT1) inhibitor with IC₅₀s of 2.8 nM and 9.8 nM for hGlyT1 and rGlyT1, respectively. NFPS exerts neuroprotection via glyR alpha1 subunit in the rat model of transient focal cerebral ischaemia and reperfusion.

Sarcosine-¹⁵N is the ¹⁵N-labeled Sarcosine. Sarcosine (N-Methylglycine), an endogenous amino acid, is a competitive glycine transporter type I (GlyT1) inhibitor and N-methyl-D-aspartate (NMDA) receptor co-agonist. Sarcosine increases the glycine concentration, resulting in an indirect potentiation of the NMDA receptor. Sarcosine is commonly used for the research of schizophrenia.

Tilapertin is an oral inhibitor of glycine transporter type-1 (GlyT1).

TASP0315003 is a glycine transporter 1 (GlyT1) inhibitor. TASP0315003 potentiates NMDA receptor function by increasing synaptic glycine levels. TASP0315003 can improve cognitive dysfunction and the negative symptoms of schizophrenia without having undesirable central nervous system side effects. TASP0315003 can be used for the research of neurological disease.

PF-03463275 hydrochloride is a centrally penetrant, orally available, selective, and competitive GlyT1 (glycine transporter-1) reversible inhibitor, with a K_i of 11.6 nM. PF-03463275 hydrochloride has the potential for Schizophrenia research.

GSK494581A is a specific ligand for human GPR55 (pEC₅₀ of 6.8) and also acts as an inhibitor of glycine transporter subtype 1 (GlyT1). GSK494581A may regulate pain signaling, bone morphogenesis, and vascular endothelial cell formation by binding to GPR55.

Org 25935 is a potent and selective glycine transporter 1 protein (GlyT1) inhibitor with an IC₅₀ value of 100 nM. Org 25935 can decrease ethanol (EtOH) intake and EtOH preference in rats, whereas water intake is unaffected. Org 25935 can be used for researching alcohol dependence or abuse.