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β-肾上腺素能受体拮抗剂与缺氧心肌中肌酸磷酸激酶的释放

Beta-adrenoceptor antagonists and the release of creatine phosphokinase from hypoxic heart muscle.

作者信息

Nayler W G, Grau A, Yepez C

出版信息

Cardiovasc Res. 1977 Jul;11(4):344-52. doi: 10.1093/cvr/11.4.344.

Abstract

The ability of several beta-adrenoceptor antagonists with partial agonist activity (dl-oxprenolol, dl-acebutolol and dl-practolol) to attenuate the release of CPK that occurs during hypoxia (pO2 less than 0.8 kPa [6 MMHg]) has been studied and compared with the protection provided by dl-propranolol. dl-propranolol attenuated the hypoxic-induced release of CPK. The activity resided in the l isomer. dl-oxprenolol, acebutolol, and practolol were either less effective than propranolol in preventing CPK release, or they exacerbated the release. The protective effect of dl-propranolol extended to the hypoxic hyperthyroid heart but not to hearts that were perfused under aerobic (pO2 greater than 80 kPa [600 mmHg]) Ca2+-free conditions.

摘要

已研究了几种具有部分激动剂活性的β-肾上腺素受体拮抗剂(消旋氧烯洛尔、消旋醋丁洛尔和消旋普拉洛尔)减轻缺氧(pO2小于0.8 kPa [6 mmHg])期间CPK释放的能力,并与消旋普萘洛尔提供的保护作用进行了比较。消旋普萘洛尔减轻了缺氧诱导的CPK释放。活性存在于左旋异构体中。消旋氧烯洛尔、醋丁洛尔和普拉洛尔在预防CPK释放方面要么比普萘洛尔效果差,要么会加剧释放。消旋普萘洛尔的保护作用扩展到缺氧的甲状腺功能亢进心脏,但不适用于在有氧(pO2大于80 kPa [600 mmHg])无钙条件下灌注的心脏。

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