glyt1 inhibitor 1

GlyT1 Inhibitor 1 is a selective and potent GlyT1 inhibitor, inhibiting rGlyT1, used in research on neurological disorders.

SSR504734 is an orally active, selective, and reversible inhibitor of human, rat, and mouse GlyT1 (IC50 = 18, 15, and 38 nM, respectively). SSR504734 exhibits activity in schizophrenia, anxiety, and depression models [1].

ASP2535 is a potent, selective, orally bioavailable, brain-permeable, and centrally-active glycine transporter-1 (GlyT1) inhibitor that can improve cognitive impairment in animal models of schizophrenia and Alzheimer's disease[1].

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

glycine transporter 1 (GlyT1) inhibitor

SSR504734 is a novel potent glycine transporter 1 (GlyT1) inhibitor.

Iclepertin (BI-425809) is an orally active and selective inhibitor of glycine transporter protein 1 (GlyT1).Iclepertin is used for the treatment of central nervous system disorders such as Alzheimer;s disease. Iclepertin is used for central nervous system disorders such as Alzheimer;s disease, schizophrenia and cognitive disorders.

Potent and selective inhibitor of the glial glycine transporter GlyT1b (IC50 = 6.9 nM). Displays negligible activity at GlyT-2, adrenoreceptors, dopamine, 5HT receptors and noradrenaline, dopamine, 5HT and GABA transporters (pIC50 in vivo. Chue et al (2013) Glycine reuptake inhibition as a new therapeutic approach in schizophrenia: focus on the glycine transporter 1 (GlyT1). Curr.Pharm.Des. 19 1311 PMID:23194655 |Brown et al (2001) Discovery and SAR of org 24598-a selective glycine uptake inhibitor. Bioorg.Med.Chem.Lett. 11 2007 PMID:11454468 |Williams et al (2003) Development of a scintillation proximity assay for analysis of Na+/Cl- -dependent neurotransmitter transporter activity. Anal. Biochem. 321 31 PMID:12963052

PF-03463275 is an orally active and selective reversible inhibitor of competitive glycine transporter protein-1 (GlyT1) with a Ki of 11.6 nM.PF-03463275 has CNS permeability and may be used to ameliorate cognitive deficits associated with schizophrenia.

Bitopertin (Paliflutine) (RG1678, RO-4917838) is a potent inhibitor of glycine transporter 1 (GlyT1), with Ki of 8.1 nM for human hGlyT1b and IC50 of 22-25 nM in Chinese hamster ovary cells.