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A23187:一种直接增强心肌收缩力的钙离子载体(38704)。

A23187: a calcium ionophore that directly increases cardiac contractility (38704).

作者信息

Holland D R, Steinberg M I, Armstrong W M

出版信息

Proc Soc Exp Biol Med. 1975 Apr;148(4):1141-5.

PMID:1093199
Abstract

The effect of the calcium ionophore A23187 on contractility in guinea pig left atria was studied. This ionophore increased both the force of contraction and the rate of tension development in a concentration dependent manner. The positive inotropic effect of A23187 is not mediated by activation of beta-receptors or by the release of endogenous catecholamines since neither propranolol nor pretreatment with reserpine altered the inotropic effect of this agent. Our studies of the dependence of contractile force on external calcium indicate that A23187 enhances the response of atrial muscle to external calcium ions. Since A23187 is known to facilitate the movement of calcium across biological membranes, we believe the ionophore may be acting either by increasing calcium influx across the myocardial cell membrane or by facilitating calcium release from sarcoplasmic reticulum.

摘要

研究了钙离子载体A23187对豚鼠左心房收缩性的影响。该离子载体以浓度依赖性方式增加收缩力和张力发展速率。A23187的正性肌力作用不是由β受体激活或内源性儿茶酚胺释放介导的,因为普萘洛尔和利血平预处理均未改变该药物的正性肌力作用。我们对收缩力对外源钙依赖性的研究表明,A23187增强了心房肌对外源钙离子的反应。由于已知A23187可促进钙跨生物膜的转运,我们认为该离子载体可能通过增加钙跨心肌细胞膜的内流或促进肌浆网释放钙来发挥作用。

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