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

GlyT (甘氨酸转运蛋白)

Glycine transporters

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-10809A
    Bitopertin (R enantiomer)

    比拓喷丁 (R型对映体)

    Inhibitor
    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。
    Bitopertin (R enantiomer)
  • HY-109067
    Opiranserin Antagonist
    Opiranserin (VVZ-149),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 对 rP2X3 有拮抗作用 (IC50=0.87 μM)。Opiranserin 可用于术后疼痛的研究。
    Opiranserin
  • HY-130466S
    Stearoyl-L-carnitine-d3 chloride Inhibitor
    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。
    Stearoyl-L-carnitine-d<sub>3</sub> chloride
  • HY-14568
    DCCCyB Inhibitor
    DCCCyB 是一种可口服的、有效的、选择性的 GlyT1 抑制剂。DCCCyB 在恒河猴体内表现出优异的 GlyT1 转运蛋白占有率。
    DCCCyB
  • HY-107527
    Org 25543 hydrochloride Inhibitor
    Org 25543 h ydrochloride是一种选择性且不可逆的 GlyT2 抑制剂 (IC50: 16 nM)。Org 25543 hydrochloride 具有镇痛作用。Org 25543 hydrochloride 可改善小鼠部分坐骨神经结扎损伤后的机械性异常性疼痛。
    Org 25543 hydrochloride
  • HY-10712
    Org-24598 Inhibitor
    Org-24598 是一种甘氨酸转运蛋白1 GlyT-1 抑制剂。Org-24598 可以抑制 [3H]CHIBA-3007 与大鼠体内脑膜的特异性结合 Ki 为 16.9 nM。
    Org-24598
  • 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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