GlyT1

Glycine transporters (GlyTs) are members of the Na⁺/Cl^--dependent transporter family, whose activities and subcellular distributions are regulated by phosphorylation and interactions with other proteins. GlyTs comprise glycine transporter type 1 (SLC6A9; GlyT1) and glycine transporter type 2 (SLC6A5; Glyt2). Both GlyTs exist in multiple splice variants. GlyTs that regulate levels of brain glycine, an inhibitory neurotransmitter with co-agonist activity for NMDA receptors (NMDARs), have been considered to be important targets for the treatment of brain disorders with suppressed NMDAR function such as schizophrenia.

GlyT1 and GlyT2 are expressed on both astrocytes and neurons, but their expression pattern in brain tissue is foremost related to neurotransmission. GlyT2 is markedly expressed in brainstem, spinal cord and cerebellum, where it is responsible for glycine uptake into glycinergic and GABAergic terminals. GlyT1 is abundant in neocortex, thalamus and hippocampus, where it is expressed in astrocytes, and involved in glutamatergic neurotransmission. GlyT1 and GlyT2, which are located in glial cells and neurons, respectively play important roles by clearing synaptically released glycine or supplying glycine to glycinergic neurons to regulate glycinergic neurotransmission. Thus, inhibition of GlyTs could be used to modify pain signal transmission in the spinal cord.

GlyT1 相关产品（17）

货号	产品名	Cas	产品描述
PC12233	ALX 5407 hydrochloride	200006-08-2	Gly T1抑制剂,ALX-5407 is a potent, selective, orally active inhibitor of GlyT1 glycine transporter with IC50 of 3 nM.
PL01829	ASP2535	374886-51-8	ASP-2535 是一种高效、有口服活性、选择性的，脑渗透性和中心活性的 GlyT1 抑制剂。ASP-2535 能改善精神分裂症和阿尔茨海默病动物模型的认知障碍。
PC11863	Bitopertin	845614-11-1	甘氨酸再摄取抑制剂（GlyT1）,Bitopertin 是一种有效的非竞争性glycine reuptake 抑制剂，抑制甘氨酸摄取，IC50 为 25 nM。
PL01649	Bitopertin (R enantiomer)	845614-12-2	Bitopertin R enantiomer (RG1678 R enantiomer; RO4917838 R enantiomer) 是 Bitopertin 的R型对映体。Bitopertin是非竞争性甘氨酸重吸收 (GlyT1) 抑制剂。
PL02041	GlyT1 Inhibitor 1	1820934-93-7	GlyT1 Inhibitor 1 是一种有效的选择性 GlyT1 抑制剂，抑制 rGlyT1， IC50 为 38 nM。
PL03798	Iclepertin	1421936-85-7	Iclepertin (BI-425809) 是一种有效、选择性且具有口服活性的甘氨酸转运蛋白 1 (GlyT1) 抑制剂。Iclepertin 对 GlyT2 无活性。Iclepertin 可用于阿尔茨海默病和精神分裂症研究。
PC12340	LY 2365109 hydrochloride	868265-28-5	甘氨酸转运蛋白1（GlyT1）抑制剂,LY2365109 is a potent and selective GlyT1 inhibitors with IC50 value of 15.8 nM.
PL01062	LY2365109 hydrochloride	1779796-27-8	LY2365109 hydrochloride 是一种高效、选择性的 GlyT1 抑制剂，抑制过表达 hGlyT1 细胞摄取谷氨酸的 IC50 值为 15.8 nM.
PL01401	N-Arachidonylglycine	179113-91-8	N-Arachidonylglycine (NA-Gly) 是内源性大麻素类 anandamide (AEA) 的羧基类似物，是一种 GPR18 激动剂 (EC50 = 44.5 nM)。与 AEA 不同，N-Arachidonylglycine 在 CB1 和 CB2 受体上均无活性。N-Arachidonylglycine 可抑制 GLYT2 (IC50 = 5.1 μM)。 N-Arachidonylglycine 也是子宫内膜细胞迁移的有效激活剂。
PL01739	Opiranserin hydrochloride	1440796-75-7	Opiranserin (VVZ-149) hydrochloride，一种非阿片类药物和非甾体抗炎止痛药，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。Opiranserin hydrochloride 对 rP2X3 有拮抗作用 (IC50=0.87 μM)。Opiranserin hydrochloride 可用于术后疼痛的研究。
PC12036	Org 25543 hydrochloride	495076-64-7	GlyT2抑制剂,A potent, highly selective glycine transporter 1 (GlyT2) inhibitor with IC50 of 16 nM with negligible affinity for GlyT1..
PL01594	PF-03463275	1173239-39-8	PF-03463275 是一种中枢神经系统渗透性、具有口服活性、选择性、竞争性甘氨酸转运蛋白-1 (GlyT1) 可逆抑制剂，Ki 为 11.6 nM。PF-03463275 有可能用于精神分裂症的研究。
PL01165	Sarcosine-15N		Sarcosine-<sup>15</sup>N 是带有 <sup>15</sup>N 标记的 Sarcosine。Sarcosine (N-Methylglycine) 是一种內源性氨基酸，是竞争性的甘氨酸转运蛋白-1 (GlyT1) 抑制剂和甘氨酸受体协同激动剂。Sarcosine 通过增加甘氨酸的浓度增强 NMDA 受体的功能。Sarcosine 通常用于精神分裂症的研究。
PC12313	Sarcosine.	107-97-1	GlyT1的内源性抑制剂,Sarcosine 1型甘氨酸转运蛋白 (GlyT) 抑制剂和甘氨酸结合位点的N-甲基-D-天冬氨酸 (NMDA) 受体共激动剂。
PL01593	SSR504734	615571-23-8	SSR504734 是一种具有口服活性、选择性和可逆性的 GlyT1 抑制剂 (hGlyT1，rGlyT1，mGlyT1 IC50 分别为 18、15 和 38 nM)。SSR504734 表现出抗精神分裂、抗焦虑和抗抑郁的活性。
PL03139	Stearoyl-L-carnitine chloride	32350-57-5	Stearoyl-L-carnitine chloride 是一种内源性的长链酰基肉碱。Stearoyl-L-carnitine chloride 是一种效力较弱的 GlyT2 抑制剂。Stearoyl-L-carnitine chloride 在浓度高达 3 μM 时可抑制 16.8％的甘氨酸响应。
PL03140	Stearoyl-L-carnitine-d3 (chloride)	2245711-27-5	Stearoyl-L-carnitine-d3 (chloride) 是 Stearoyl-L-carnitine chloride 的氘代物。Stearoyl-L-carnitine chloride 是一种内源性的长链酰基肉碱。Stearoyl-L-carnitine chloride 是一种效力较弱的 GlyT2 抑制剂。Stearoyl-L-carnitine chloride 在浓度高达 3 μM 时可抑制 16.8％的甘氨酸响应。