1. GPCR/G Protein Neuronal Signaling
  2. Adrenergic Receptor
  3. RWJ52353 hydrochloride

RWJ-52353 hydrochloride 是口服有效、高选择性的 α2D 肾上腺素能受体的激动剂 (Ki: 1.5 nM),具有潜在镇痛作用。RWJ-52353 hydrochloride 在大鼠和小鼠的腹部测试实验中均表现出镇痛活性,并改善小鼠在热板实验和甩尾实验中的焦躁情况。RWJ-52353 hydrochloride 还调节有机阳离子转运蛋白 (OCT) 亚型,抑制 rOCT1 和 rOCT2 的 IC50s 分别为 100 μM 和 20 μM;同时激活 rOCT3,影响细胞中 [3H]-1-甲基-4-苯基吡啶鎓 ([3H]MPP) 转运。

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RWJ52353 hydrochloride Chemical Structure

RWJ52353 hydrochloride Chemical Structure

CAS No. : 245744-13-2

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查看 Adrenergic Receptor 亚型特异性产品:

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

RWJ-52353 hydrochloride is an orally potent, highly selective α2D adrenergic receptor agonist (Ki: 1.5 nM) with potential analgesic effects. RWJ-52353 hydrochloride demonstrated analgesic activity in abdominal tests in rats and mice, and improved agitation in mice in the hot plate test and tail flick test. RWJ-52353 hydrochloride also regulates the organic cation transporter (OCT) subtype, inhibiting rOCT1 and rOCT2 with IC50s of 100 μM and 20 μM respectively; it also activates rOCT3, affecting [3H]-1- in cells. Methyl-4-phenylpyridinium ([3H]MPP) transport[1][2].

IC50 & Target

Ki: 1.5 nM (α2D AR), 254 nM (α2A AR), 621 nM (α2B AR), 443 nM (α1 AR)[1]
IC50: 100 μM (rOCT1), 20 μM (rOCT2)[2]

体内研究
(In Vivo)

RWJ-52353 (30 mg/kg; po; 单剂量) hydrochloride 在诱导引起的小鼠腹部疼痛模型具有抑制作用,抑制率达到 100%[1]
RWJ-52353 在诱导引起的大鼠和小鼠的腹部疼痛模型中的 ED50s 分别为 15.1 mg/kg (po) 和 11.6 mg/kg (po)[1]
RWJ-52353 还能够减轻小鼠在热板实验 (48°C) 和甩尾实验中的痛苦程度,ED50s 分别为 25.9 mg/kg (po) 和 100.2 mg/kg (po)[1]

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

分子量

238.74

Formula

C11H11ClN2S

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

RWJ52353 hydrochloride 相关分类

  • 摩尔计算器

  • 稀释计算器

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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.

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RWJ52353 hydrochloride
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HY-103216A
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