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BAY K 8644是一种钙通道激动剂,在体外可抑制肾素分泌。

BAY K 8644, a calcium channel agonist, inhibits renin secretion in vitro.

作者信息

Churchill P C, Churchill M C

出版信息

Arch Int Pharmacodyn Ther. 1987 Jan;285(1):87-97.

PMID:2437873
Abstract

These experiments were designed to characterize the renin secretory effects of BAY K 8644, a dihydropyridine derivative which acts as a Ca channel agonist. The rat renal cortical slice preparation was used. BAY K 8644 produced a concentration-dependent inhibition of basal renin secretion. Although the inhibitory effect was not blocked by nifedipine or by methoxyverapamil in concentrations which effectively block the renin secretory effects of K-depolarization, higher concentrations did block. Moreover, chelating extracellular Ca2+ with EGTA also blocked the inhibitory effect. These observations are consistent with the hypothesis that the inhibitory effect is mediated by Ca2+ influx. Collectively, the results add to the growing evidence that Ca2+ is an inhibitory second messenger in the renin secretory process.

摘要

这些实验旨在表征BAY K 8644(一种作为钙通道激动剂的二氢吡啶衍生物)对肾素分泌的影响。采用大鼠肾皮质切片制备物。BAY K 8644对基础肾素分泌产生浓度依赖性抑制作用。尽管硝苯地平或甲氧基维拉帕米在有效阻断钾去极化对肾素分泌作用的浓度下并不能阻断这种抑制作用,但更高浓度时则可阻断。此外,用乙二醇双四乙酸(EGTA)螯合细胞外钙离子也可阻断这种抑制作用。这些观察结果与下述假说一致,即这种抑制作用是由钙离子内流介导的。总体而言,这些结果进一步证明了钙离子是肾素分泌过程中的一种抑制性第二信使,相关证据越来越多。

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