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司替普利对温血动物离体心肌等长肌电图和动作电位的影响。

Influence of stenopril on the isometric myogram and the action potential of isolated myocardium of warm-blooded animals.

作者信息

Spassov G, Mileva S

出版信息

Acta Physiol Pharmacol Bulg. 1981;7(3):26-33.

PMID:7340394
Abstract

The effect of the original Bulgarian drug Stenopril (1-phenyl-2/1-phenylpropyl-/3/-amino/propane hydrochloride) on the papillary muscle of guinea-pig right ventricle was studied in vitro. The isometric myogram and the transmembrane cellular activity were recorded. At low Stenopril concentrations (1-5 x 10(-6)M) three effects were observed: weak positive inotropic effect, phasic response (initial increase and subsequent decrease of the amplitude of the contractions) and weak negative inotropic effect. Concentrations of 10(-5) and 10(-4)M inhibit the contractile activity of the myocardium. The changes in the action potentials at the low concentrations are small. At the higher concentrations the Stenopril-negative inotropy is accompanied by lowering of the plateau and extension of the potential at the expense of the late repolarization, as well as decrease of the repolarization velocity. In a number of experiments the excitability decreased until the appearance of local responses. Isoprenaline (10(-6)M) completely restores the Stenopril-inhibited electrical and contractile activity of the drug. It is assumed that Stenopril influences the inward calcium current, similar to the calcium antagonists, and that it also inactivates the Na-permeability of the membrane.

摘要

研究了原产于保加利亚的药物司替普利(1-苯基-2/1-苯丙基/-3/-氨基/丙烷盐酸盐)对豚鼠右心室乳头肌的体外作用。记录了等长肌电图和跨膜细胞活性。在低司替普利浓度(1-5×10⁻⁶M)下观察到三种效应:微弱的正性肌力作用、相位反应(收缩幅度先增加后降低)和微弱的负性肌力作用。10⁻⁵和10⁻⁴M的浓度抑制心肌的收缩活性。低浓度时动作电位的变化较小。在较高浓度时,司替普利的负性肌力作用伴随着平台期降低和以晚期复极化时间延长为代价的电位延长,以及复极化速度降低。在一些实验中,兴奋性降低直至出现局部反应。异丙肾上腺素(10⁻⁶M)可完全恢复司替普利抑制的该药物的电活动和收缩活性。推测司替普利与钙拮抗剂类似,影响内向钙电流,并且它还使膜的钠通透性失活。

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