2. Membrane Transporter/Ion Channel Neuronal Signaling
  3. iGluR
  4. Rapastinel acetate

Rapastinel acetate  (Synonyms: GLYX-13 acetate)

目录号: HY-16728A
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Rapastinel acetate (GLYX-13 acetate)是一种N-methyl-D-aspartate (NMDA) 受体的调节剂，具有长效抗抑郁活性。Rapastinel acetate通过增强突触传递的长时程增强作用(LTP)来发挥其抗抑郁效果。Rapastinel acetate在海马体和内侧前额叶皮层的锥体神经元中，通过与NMDAR复合体的独特位点结合，瞬间增强NMDAR介导的电流。Rapastinel acetate在1 μmol/l浓度下显著增强了NMDAR介导的电流，而在10 μmol/l浓度时则显著降低电流。Rapastinel acetate的作用机制与细胞内钙失活位点的亲和力降低相关，这为增强由NMDAR介导的电导提供了理论基础。

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Rapastinel acetate Chemical Structure

Rapastinel acetate Chemical Structure

CAS No. : 491872-39-0

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Rapastinel acetate 相关抗体

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MCE 顾客使用本产品发表的 1 篇科研文献

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    Rapastinel acetate purchased from MCE. Usage Cited in: J Cell Mol Med. 2020 Aug;24(16):9287-9299.  [Abstract]

    Neurons are pre-treated with 25 μM propofol plus 20 μM Rapastinel, followed by TNF-α treatment (40 ng/mL, 2 h). The effect of propofol on TNF-α- induced intracellular calcium accumulation, phosphorylation of CaMK II and calpain-2, calpain activation, cathepsin B release and TrkB truncation is counteracted by Rapastinel.

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    AMPA Receptor NMDA Receptor Kainate Receptor

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    生物活性

    Rapastinel acetate (GLYX-13 acetate) is an N-methyl-D-aspartate (NMDA) receptor modulator with long-acting antidepressant activity. Rapastinel acetate exerts its antidepressant effects by enhancing long-term potentiation (LTP) of synaptic transmission. Rapastinel acetate transiently enhances NMDAR-mediated currents in pyramidal neurons in the hippocampus and medial prefrontal cortex by binding to unique sites on the NMDAR complex. Rapastinel acetate significantly enhanced NMDAR-mediated currents at a concentration of 1 μmol/l and significantly reduced the currents at a concentration of 10 μmol/l. The mechanism of action of Rapastinel acetate is related to the reduction of affinity to intracellular calcium inactivation sites, which provides a theoretical basis for enhancing conductance mediated by NMDAR[1].

    分子量

    473.52

    Formula

    C20H35N5O8
    CAS 号
    运输条件

    Room temperature in continental US; may vary elsewhere.
    储存方式

    Please store the product under the recommended conditions in the Certificate of Analysis.
    纯度 & 产品资料
    参考文献

    Rapastinel acetate 相关分类

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    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

    Keywords:

    Rapastinel491872-39-0GLYX-13GLYX13GLYX 13iGluRIonotropic glutamate receptorsInhibitorinhibitorinhibit

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