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

Zolertine hydrochloride 是一种 α-肾上腺素受体 (α-adrenoceptor) 拮抗剂,在大鼠肝脏 (α1B-adrenoceptors) 和兔肝脏 (α1A-adrenoceptors) 膜中的 pKi 分别为 6.81 和 6.35。

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Zolertine hydrochloride Chemical Structure

Zolertine hydrochloride Chemical Structure

CAS No. : 7241-94-3

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生物活性

Zolertine hydrochloride is an α-adrenoceptor antagonist with a pKi of 6.81 in rat liver (α1B-adrenoceptors) and 6.35 in rabbit liver (α1A-adrenoceptors) membranes[1].

IC50 & Target[1]

α1A-adrenergic receptor

6.35 (pKi, in rabbit liver membrane)

α1B-adrenergic receptor

6.81 (pKi, in rat liver membrane)

体外研究
(In Vitro)

在大鼠的颈动脉和主动脉中,Zolertine hydrochloride 竞争性地抗拮抗了去甲肾上腺素诱导的收缩反应,得到的 pA2 值分别为:WKY 7.48±0.18,SHR 7.43±0.13;以及 WKY 7.57±0.24,SHR 7.40±0.08。在一些血管中,Zolertine hydrochloride 表现为非竞争性拮抗剂,因为 Schild 图的斜率小于 1。Zolertine hydrochloride 的 pKb 估值在肠系膜动脉中为 WKY 6.98±0.16,SHR 6.81±0.18;在尾动脉中为 WKY 5.73±0.11,SHR 5.87±0.25;在兔主动脉中为 6.65±0.09[1]
与 α1A-肾上腺素受体相比,Zolertine hydrochloride 对 α1D-肾上腺素受体的亲和力更高,而对 α1B-肾上腺素受体的亲和力居中[1]

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

分子量

294.78

Formula

C13H19ClN6

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

Zolertine hydrochloride 相关分类

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Help & FAQs
  • 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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