glyt1

Sarcosine (Methylglycine) 是 I 型甘氨酸转运蛋白 (GlyT1) 的竞争性抑制剂和 N-甲基-D-天冬氨酸受体 (NMDAR) 共激动剂，通过增加甘氨酸的浓度增强 NMDA 受体的功能，可用于精神分裂症的研究。

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

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

Tilapertin is an oral glycine transporter type-1 inhibitor.

Iclepertin (BI-425809) 是一种具有口服活性和选择性的甘氨酸转运蛋白 1 (GlyT1) 抑制剂。Iclepertin 可用于阿尔茨海默病.精神分裂和认知障碍等中枢神经系统疾病。

PF-03463275 是一种具有口服活性和选择性的竞争性甘氨酸转运蛋白-1 (GlyT1) 可逆抑制剂，Ki 为 11.6 nM。PF-03463275 具有中枢神经系统渗透性，可用于改善与精神分裂症相关的认知障碍。

Bitopertin (Paliflutine) 是一种有效的甘氨酸转运蛋白 1 (GlyT1) 抑制剂，对人 hGlyT1b 的 Ki 为 8.1 nM。

GlyT1 Inhibitor 1 是一种具有选择性和高效性的 GlyT1 抑制剂，抑制 rGlyT1，可用于研究神经系统疾病。

LY2365109 hydrochloride 是高选择性GlyT1抑制剂，抑制过表达 hGlyT1 细胞摄取谷氨酸的IC50值为 15.8 nM.

SSR504734 是一种具有口服活性、选择性和可逆性的 GlyT1抑制剂 (hGlyT1，rGlyT1，mGlyT1IC50分别为 18、15 和 38 nM)。SSR504734 在精神分裂症、焦虑症和抑郁症模型中表现出活性。

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

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

Org 25543 hydrochloride 是一种有效的选择性甘氨酸转运蛋白 2 型 (GlyT2) 抑制剂（hGlyT2 的 IC50 = 16 nM）。在 CHO 细胞的甘氨酸摄取测定中，对 GlyT1 或 56 种其他常见生物靶标 (≥ 100 μM) 没有显示活性。

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

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.

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

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

GSK-1018921 free base is a selective GlyT1 inhibitor.

Oleoyl-L-carnitine是一种长链酰基肉碱，也是一种糖苷转运体2（GlyT2；IC50 = 340 nM）的抑制剂，对GlyT2比对GlyT1（IC50 = >10,000 nM）具有选择性。慢性肾脏病或接受初始血液透析的终末期肾脏病患者的血浆中Oleoyl-L-carnitine水平增高，这与心血管死亡率相关。