glycine transporters

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。

Opiranserin 是一种非阿片类和非 NSAID 镇痛候选药物，是 2 型甘氨酸转运蛋白 (GlyT2) 和 5-羟色胺受体 2A (5HT2A) 的双重拮抗剂，IC50分别为 0.86 和 1.3 μM。它可用于术后疼痛的研究，对 rP2X3 有拮抗作用，IC50为0.87 μM。

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。

Opiranserin hydrochloride 是甘氨酸转运蛋白 2 型 (GlyT2) 和 5-羟色胺受体 2A (5HT2A) 的双重拮抗剂，IC50 分别为 0.86 和 1.3 μM。它显示对 rP2X3 的拮抗活性 (IC50=0.87 μM)。它正在开发为用于治疗术后疼痛的注射剂。

L-4FPG 是甘氨酸衍生物，抑制中性氨基酸转运蛋白 ASCT1 和 ASCT2。

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.

Butyryl-L-carnitine is a butyrate ester of carnitine. It is an inhibitor of intestinal transporters, blocking carnitine uptake by the carnitine transporter and glycine transport by the amino acid transporter in human retinal pigment epithelial (HRPE) cells (IC50s = 1.5 μM and 4.6 mM, respectively).

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

GT-0198 is a novel glycine transporter 2 inhibitor showed activity in a mouse model of neuropathic pain. GT-0198 inhibited the function of glycine transporter 2 (GlyT2) in human GlyT2-expressing HEK293 cells and did not bind various major transporters or receptors of neurotransmitters in a competitive manner. GT-0198 is considered to be a comparatively selective GlyT2 inhibitor. GT-0198 is a structurally novel GlyT2 inhibitor bearing a phenoxymethylbenzamide moiety with in vivo efficacy in behavioral models of neuropathic pain.