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福斯高林对肌肉细胞的作用会受到激素、钙离子和钙拮抗剂的影响。

The action of forskolin on muscle cells is modified by hormones, calcium ions and calcium antagonists.

作者信息

Lindner E, Metzger H

出版信息

Arzneimittelforschung. 1983;33(10):1436-41.

PMID:6316992
Abstract

Forskolin, a drug isolated from the Indian plant Coleus forskohlii, exerts its actions on cells by directly activating the catalytic subunit of adenylatecyclases. The primary effect on heart muscles is the positive inotropic one, at higher forskolin concentrations, an acceleration of the pacemaker activity can be observed. External Ca2+ is required for this augmentation of contraction, verapamil, prenylamine and tetrodotoxin depress these effects. The action of forskolin and digitalis glycosides are to a certain degree additive. Incubation of rat heart slices with forskolin depresses the membrane bound Na+K+-ATPase activity. In smooth muscle cells, forskolin lowers the contractions, evoked by K+, norepinephrine and by angiotensin II. The results are discussed in respect to a forskolin induced enlargement of the Ca2+-uptake of heart muscle cells and a lowering of the Ca2+-sensitivity of the contractile system of smooth muscle cells.

摘要

福斯高林是一种从印度植物毛喉鞘蕊花中分离出的药物,它通过直接激活腺苷酸环化酶的催化亚基对细胞发挥作用。对心肌的主要作用是正性肌力作用,在较高浓度的福斯高林作用下,可观察到起搏活动加速。这种收缩增强需要细胞外钙离子,维拉帕米、普尼拉明和河豚毒素可抑制这些作用。福斯高林和洋地黄糖苷的作用在一定程度上是相加的。用福斯高林孵育大鼠心脏切片可降低膜结合的钠钾-ATP酶活性。在平滑肌细胞中,福斯高林可降低由钾离子、去甲肾上腺素和血管紧张素II引起的收缩。结合福斯高林诱导心肌细胞钙摄取增加和平滑肌细胞收缩系统钙敏感性降低的情况对结果进行了讨论。

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