Zolertine Hydrochloride

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].

Research Areas >> Cardiovascular Disease

Signaling Pathways >> GPCR/G Protein >> Adrenergic Receptor

α1A-adrenergic receptor:6.35 (pKi, in rabbit liver membrane)

α1B-adrenergic receptor:6.81 (pKi, in rat liver membrane)

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]。

[1]. Ibarra M, et al. The alpha-adrenoceptor antagonist, zolertine, inhibits alpha1D- and alpha1A-adrenoceptor-mediated vasoconstriction in vitro. J Auton Pharmacol. 2000 Jun;20(3):139-45.