1. Others Neuronal Signaling Membrane Transporter/Ion Channel
  2. Isotope-Labeled Compounds GABA Receptor
  3. Alpidem-d14

Alpidem-d14Alpidem (HY-W013150) 的氘代物。Alpidem 是一种抗焦虑剂,为具有口服活性且可透过血脑屏障的 GABAA 受体配体,与含 α1β2γ2 亚基的 GABAA 受体结合的 IC50 为 17 nM,远高于与含 α5β2γ2 亚基的 GABAA 受体的结合活性 (IC50 of >10 μM)。Alpidem 可调控钙诱导的线粒体通透性转换,诱导谷胱甘肽耗竭和肝细胞坏死,增强 TNF-α 的毒性,抑制埋弹珠行为与自主活动,增强应激状态下啮齿类动物的摄食行为,并发挥抗惊厥作用。Alpidem 可用于焦虑、焦虑障碍及惊厥的相关研究。

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Alpidem-d<sub>14</sub>

Alpidem-d14 Chemical Structure

CAS No. : 1189962-23-9

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Alpidem-d14 is the deuterium labeled Alpidem (HY-W013150)[1]. Alpidem, an anxiolytic agent, is an orally active and brain-penetrant GABAA receptor ligand, binds to α1β2γ2 subunit-containing GABAA receptors (IC50 of 17 nM) over α5β2γ2 subunit-containing GABAA receptors (IC50 of >10 μM). Alpidem modulates calcium-induced mitochondrial permeability transition, induces glutathione depletion and hepatocyte necrosis, potentiates TNF-α toxicity, inhibits marble-burying and locomotor activity, enhances stressed rodent feeding behavior, and exerts anticonvulsant effects. Alpidem can be used for the research of anxiety, anxiety disorders, and convulsions.

产品应用

1. 该化合物可作为示踪剂。
2. 该化合物可作为 NMR、GC-MS 或 LC-MS 分析中的内标品,用于定量分析。

体外研究
(In Vitro)

氢、碳和其他元素的稳定重同位素已被掺入药物分子中,主要用作药物开发过程中定量的示踪剂。氘化因其可能影响药物的药代动力学和代谢特征而受到关注。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

分子量

418.42

Formula

C21H9D14Cl2N3O

CAS 号
非标记 CAS
中文名称

阿吡坦-d14

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
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产品名称:
Alpidem-d14
目录号:
HY-W013150S
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