glyt1

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

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.

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].

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

Org 25543 hydrochloride is a potent and selective glycine transporter type 2 (GlyT2) inhibitor (IC50 = 16 nM for hGlyT2). Displays no activity at GlyT1 or 56 other common biological targets (≥ 100 μM), in a glycine uptake assay in CHO cells.

Bitopertin R enantiomer (RG1678 R enantiomer) is the R-enantiomer of Bitopertin, a noncompetitive glycine reuptake inhibitor that inhibits glycine uptake at human GlyT1 (IC50: 25 nM).

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

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).

Tilapertin is an oral glycine transporter type-1 inhibitor.

glycine transporter 1 (GlyT1) inhibitor

DCCCyb is an orally bioavailable and selective GlyT1 Inhibitor. DCCCyb demonstrated excellent in vivo occupancy of GlyT1 transporters in rhesus monkeys as determined by the displacement of a PET tracer ligand.

GSK931145 is a positron emission tomography (PET) radioligand, it is suitable for quantifying glycine transporter (GlyT1) availability in the living brain.

Org-25935, a GlyT-1 inhibitor, is used potentially for the treatment of schizophrenia and alcohol dependence.

PF-03463275 is an orally available, CNS-penetrant inhibitor of SLC6A9, a GlyT1 glycine transporter.

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

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.

GSK-1018921 free base is a selective GlyT1 inhibitor.

Oleoyl-L-carnitine, a long-chain acylcarnitine, acts as a selective inhibitor of glycine transporter 2 (GlyT2; IC50 = 340 nM) while demonstrating significantly lesser affinity for GlyT1 (IC50 = >10,000 nM). Elevated plasma levels of this compound have been observed in patients suffering from chronic kidney disease or end-stage renal disease undergoing initial hemodialysis, correlating with an increased risk of cardiovascular mortality.