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  4. KRM-II-81

KRM-II-81是一种γ?氨基丁酸A型（GABAA）受体配体，具有镇痛、抗焦虑和抗癫痫活性。KRM-II-81表现出对α2/3亚单位选择性的GABAA受体正变构调节作用。KRM-II-81在口服给药后能够减轻由福尔马林诱导的疼痛反应。KRM-II-81显著减轻了慢性脊神经结扎引起的痛觉行为。KRM-II-81的分析表明，其血浆和脑内浓度与镇痛效果呈正相关。KRM-II-81对GABA电流的增强作用显示其在镇痛机制中具有关键作用。KRM-II-81在呼吸抑制方面的效果较弱，显示其安全性和耐受性。

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KRM-II-81 Chemical Structure

KRM-II-81 Chemical Structure

CAS No. : 2014348-91-3

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KRM-II-81 相关抗体

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  • 生物活性

  • 纯度 & 产品资料

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生物活性

KRM-II-81 is a gamma-aminobutyric acid type A (GABAA) receptor ligand with analgesic, anxiolytic and anti-epileptic activities. KRM-II-81 exhibits positive allosteric modulation of GABAA receptors selective for the α2/3 subunit. KRM-II-81 reduces formalin-induced pain response after oral administration. KRM-II-81 significantly reduces pain behavior induced by chronic spinal nerve ligation. Analysis of KRM-II-81 showed that its plasma and brain concentrations were positively correlated with analgesic effects. The enhancement effect of KRM-II-81 on GABA current shows its key role in the analgesic mechanism. KRM-II-81 was less effective in respiratory depression, demonstrating its safety and tolerability[1].

分子量

351.36

Formula

C21H13N5O
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

KRM-II-81 相关分类

  • 摩尔计算器

  • 稀释计算器

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浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
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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:

KRM-II-812014348-91-3OthersInhibitorinhibitorinhibit

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产品名称：
KRM-II-81
目录号：
HY-116275
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