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[奎尼丁立体异构体对心脏和循环系统的影响]

[Heart and circulatory effects of quinidine stereoisomers].

作者信息

Reuter N, Meyer F

出版信息

Arch Int Pharmacodyn Ther. 1976 Nov;224(1):152-63.

PMID:1015910
Abstract

Quinidine sulfate shows dose-related activity. On the cardio-vascular system of anaesthetized cats. It reduces heart rate, prolongs QRS and QT of the ECG, lowers peripheral blood pressure and depresses slightly myocardial contractility. Quinidine hydrochloride lowers blood pressure but alters the ECG only in very high doses. Epiquinidine has no blood pressure lowering activity. According to the Easson and Stedman hypothesis this may be the result of stereoselectivity of alpha-adrenergic receptors. Only very high doses of the epimer produce a transient decrease of blood pressure. The ECG-waves are, however, markedly altered. QT is prolonged only with epiquinine-epiquinidine-sulfate. The salts of epiquinidine tested are much better water-soluble than those of quinidine.

摘要

硫酸奎尼丁呈现出剂量相关的活性。在麻醉猫的心血管系统上,它会降低心率,延长心电图的QRS和QT间期,降低外周血压,并轻微抑制心肌收缩力。盐酸奎尼丁会降低血压,但仅在非常高的剂量下才会改变心电图。表喹尼丁没有降压活性。根据伊登和斯特德曼假说,这可能是α-肾上腺素能受体立体选择性的结果。只有非常高剂量的差向异构体才会导致血压短暂下降。然而,心电图波形会有明显改变。只有表奎宁-表喹尼丁-硫酸盐会延长QT间期。所测试的表喹尼丁盐比奎尼丁盐的水溶性要好得多。

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