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1-[2-羟基-3-(4-苯基-1-哌嗪基)丙基]-2-吡咯烷酮(MG-1(R,S))及其对映异构体的抗心律失常和降压活性。

Antiarrhythmic and hypotensive activities of 1-[2-hydroxy-3-(4-phenyl-1-piperazinyl)propyl]-pyrrolidin-2-one (MG-1(R,S)) and its enantiomers.

机构信息

Department of Pharmacodynamics, Laboratory of Pharmacological Screening, Faculty of Pharmacy, Medical College, Jagiellonian University, Medyczna 9, PL 30-688 Kraków, Poland.

出版信息

Pharmacol Rep. 2011;63(2):455-63. doi: 10.1016/s1734-1140(11)70512-6.

Abstract

The compound MG-1(R,S), (1-[2-hydroxy-3(4-phenyl-1-piperazinyl)propyl]-pyrrolidin-2-one, and its enantiomers were tested for electrocardiographic, antiarrhythmic and hypotensive activities. The racemic mixture (MG-1(R,S)) and its S-enantiomer significantly decreased systolic and diastolic blood pressure and possessed antiarrhythmic activity. The S-enantiomer displayed the greatest effect. The R-enantiomer did not show antiarrhythmic or hypotensive activity. The results suggest that the antiarrhythmic and hypotensive effects of these compounds are related to their adrenolytic properties.

摘要

化合物 MG-1(R,S),即 1-[2-羟基-3(4-苯基-1-哌嗪基)丙基]-吡咯烷-2-酮及其对映异构体,被测试了其心电图、抗心律失常和降压活性。外消旋混合物(MG-1(R,S))及其 S-对映异构体显著降低了收缩压和舒张压,具有抗心律失常活性。S-对映异构体显示出最大的效果。R-对映异构体没有显示出抗心律失常或降压活性。结果表明,这些化合物的抗心律失常和降压作用与其肾上腺能阻断特性有关。

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