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非诺维林(一种新型平滑肌运动调节剂)的药效学特征

Pharmacodynamic profile of fenoverine, a novel modulator of smooth muscle motility.

作者信息

De Santis D, Marrazzo R, Losasso C, Loffreda A, De Paola C, De Novellis V, Molinario L, Schiariti F, Marmo E

机构信息

Institute of Pharmacology and Toxicology, 1st Faculty of Medicine and Surgery, University of Naples, Italy.

出版信息

Drugs Exp Clin Res. 1989;15(1):37-42.

PMID:2743871
Abstract

Experimental research has documented that fenoverine is a depressant drug mostly active on the intestinal smooth muscle; however, it is also active on other tissues as well as on the genito-urinary tract. Fenoverine may be considered a synchronizer of smooth muscle effective in modulating the intracellular influx of calcium into the cell and its release from the intracellular pool. Fenoverine causes a reduction of the excitatory junction potential (EJP) in intestinal smooth muscle by stimulating parasympathetic efferent fibres without any change in the inhibitory junction potential (IJP). This also occurs in the presence of atropine. Fenoverine reduces the intracellular Ca2+ concentration by decreasing the calcium gradient across the cell membrane, as well as decreasing the release of Ca2+ from the intestinal pool more intensely than papaverine (but less intensely than nifedipine, verapamil or diltiazem). This phenomenon has been observed in the intestinal smooth muscle and also in the genito-urinary tract.

摘要

实验研究已证明,非诺维林是一种主要作用于肠道平滑肌的抑制性药物;然而,它对其他组织以及泌尿生殖道也有作用。非诺维林可被视为一种平滑肌同步剂,能有效调节细胞内钙离子流入细胞及其从细胞内储存库的释放。非诺维林通过刺激副交感传出纤维,使肠道平滑肌的兴奋性接头电位(EJP)降低,而抑制性接头电位(IJP)无任何变化。在阿托品存在的情况下也会出现这种情况。非诺维林通过降低细胞膜两侧的钙梯度来降低细胞内Ca2+浓度,并且比罂粟碱更强烈地减少肠道储存库中Ca2+的释放(但比硝苯地平、维拉帕米或地尔硫䓬的作用强度小)。这种现象在肠道平滑肌以及泌尿生殖道中均有观察到。

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