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

GlyT (甘氨酸转运蛋白)

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.

GlyT 相关产品 (15):

目录号 产品名 作用方式 纯度
  • HY-10809
    Bitopertin Inhibitor 99.68%
    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。
  • HY-101037
    Sarcosine Inhibitor
    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。
  • HY-10716A
    PF-03463275 Inhibitor 99.57%
    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。
  • HY-100416A
    LY2365109 hydrochloride Inhibitor 99.32%
    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.
  • HY-112432
    GlyT1 Inhibitor 1 Inhibitor 98.35%
    GlyT1 Inhibitor 1 是一种有效的选择性 GlyT1 抑制剂,抑制 rGlyT1 IC50 为 38 nM。
  • HY-103332
    N-Arachidonylglycine Inhibitor
    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。
  • HY-138935
    Iclepertin Inhibitor
    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。
  • HY-130466
    Stearoyl-L-carnitine chloride Inhibitor ≥99.0%
    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。
  • HY-10809A
    Bitopertin (R enantiomer) 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。
  • 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。
  • HY-110176
    ASP2535 Inhibitor 99.70%
    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。
  • HY-107526
    NFPS Inhibitor
    NFPS 是一种选择性,非竞争性甘氨酸转运蛋白-1 (GlyT1) 抑制剂,对 hGlyT1 和 rGlyT1 的 IC50 分别为 2.8 nM 和 9.8 nM。NFPS 通过 glyR alpha1 亚基在瞬时局灶性脑缺血和再灌注的大鼠模型中发挥神经保护作用。
  • HY-111029
    ALX-1393 Inhibitor
    ALX-1393 是一种选择性 GlyT2 抑制剂, 对大鼠急性疼痛模型中的热,机械和化学刺激具有抗伤害作用。
  • HY-19887
    Tilapertin Inhibitor
    Tilapertin 是甘氨酸转运蛋白 1 型 (GlyT1) 的口服抑制剂。
  • HY-101334
    MPDC Inhibitor
    MPDC 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。
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