1. Signaling Pathways
  2. Membrane Transporter/Ion Channel
    Neuronal Signaling
  3. GlyT

GlyT (甘氨酸转运蛋白)

Glycine transporters

甘氨酸转运蛋白 (GlyTs) 是 Na+/Cl- 依赖性转运蛋白家族的成员,其活性和亚细胞分布受磷酸化和与其他蛋白质的相互作用调节。GlyTs 包括甘氨酸转运蛋白 1 型 (SLC6A9;GlyT1) 和甘氨酸转运蛋白 2 型 (SLC6A5;Glyt2)。两种 GlyTs 都存在于多种剪接变体中。调节脑甘氨酸水平的 GlyTs 是一种具有 NMDA 受体 (NMDARs) 共激动剂活性的抑制性神经递质,被认为是治疗 NMDAR 功能受抑制的脑部疾病(如精神分裂症)的重要靶点。

GlyT1 和 GlyT2 在星形胶质细胞和神经元上均有表达,但它们在脑组织中的表达模式主要与神经传递有关。GlyT2在脑干、脊髓和小脑中大量表达,负责将甘氨酸摄取到甘氨酸能和GABA能终末神经元中。GlyT1在大脑皮层、丘脑和海马中含量丰富,在星形胶质细胞中表达,参与谷氨酸能神经传递。GlyT1和GlyT2分别位于神经胶质细胞和神经元中,通过清除突触释放的甘氨酸或向甘氨酸能神经元提供甘氨酸来调节甘氨酸能神经传递,发挥重要作用。因此,抑制GlyTs可用于改变脊髓中的疼痛信号传递。

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.

Cat. No. Product Name Effect Purity Chemical Structure
  • HY-113202S1
    Stearoyl-L-carnitine-d9 chloride Inhibitor
    Stearoyl-L-carnitine-d9 chloride 是 Stearoyl-L-carnitine chloride 的氘代物。Stearoyl-L-carnitine chloride 是一种脂肪酯脂质分子,是一种内源性代谢物 (endogenous metabolite)。Stearoyl-L-carnitine chloride 可用作 PKC 抑制剂。Stearoyl-L-carnitine chloride 在 β 细胞中积聚,导致 2 型糖尿病小鼠的胰岛素合成停止和能量缺乏。Stearoyl-L-carnitine chloride 抑制大鼠和兔血浆中的卵磷脂胆固醇酰基转移酶 (LCAT)。Stearoyl-L-carnitine chloride 可作为帕金森病的代谢组学生物标志物。Stearoyl-L-carnitine chloride 是一种效力较弱的 GlyT2 抑制剂。
    Stearoyl-L-carnitine-d<sub>9</sub> chloride
  • HY-111162
    GSK494581A Inhibitor
    GSK494581A 是人类 GPR55 的特异性配体 (pEC50 为 6.8),也是一种甘氨酸转运蛋白亚型 1 (GlyT1) 抑制剂。GSK494581A 可能通过与GPR55 结合来调控疼痛信号传导、骨形态发生以及血管内皮细胞形成。
    GSK494581A
  • HY-113202S
    Stearoyl-L-carnitine-d3 Inhibitor
    Stearoyl-L-carnitine-d3 是 Stearoylcarnitine 的氘代物。Stearoylcarnitine 是一种脂肪酯脂质分子,是一种内源性代谢物 (endogenous metabolite)。Stearoylcarnitine 可用作 PKC 抑制剂。Stearoylcarnitine 在 β 细胞中积聚,导致 2 型糖尿病小鼠的胰岛素合成停止和能量缺乏。Stearoylcarnitine 抑制大鼠和兔血浆中的卵磷脂胆固醇酰基转移酶 (LCAT)。Stearoylcarnitine 可作为帕金森病的代谢组学生物标志物。Stearoylcarnitine 是一种效力较弱的 GlyT2 抑制剂。
    Stearoyl-L-carnitine-d<sub>3</sub>
  • HY-101334A
    MPDC hydrochloride Inhibitor
    MPDC hydrochloride 是竞争性的、前脑突触体中的、Na+ 依赖的、高亲和力的谷氨酸转运体抑制剂。
    MPDC hydrochloride
  • HY-122666
    Org 25935 Inhibitor
    Org 25935 是一种有效且具有选择性的甘氨酸转运蛋白 1 (GlyT1) 抑制剂,IC50 为 100 nM。Org 25935 可在大鼠中降低乙醇摄入和乙醇嗜好,但不影响水的摄入。Org 25935 可用于研究酒精依赖或滥用。
    Org 25935
  • HY-19887
    Tilapertin Inhibitor
    Tilapertin 是甘氨酸转运蛋白 1 型 (GlyT1) 的口服抑制剂。
    Tilapertin
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