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普萘洛尔的d-和l-光学异构体对心室颤动阈值的影响。

The effects of the d- and l-optical isomers of propranolol on the ventricular fibrillation threshold.

作者信息

Spear J F, Moore E N, Ricciutti M

出版信息

Eur J Cardiol. 1978 Apr-May;7(2-3):117-24.

PMID:668750
Abstract

The minimum current required to induce ventricular fibrillation was determined in 22 sodium pentobarbital anesthetized open chest dogs in the presence of the d- or l-isomers of propranolol at concentrations of 0.2, 0.5, and 1.0 mg/kg. The hearts were paced from the right atrium at a constant basic cycle length of 350 msec and the current was delivered during the vulnerable period to the right ventricle as a 120 msec train of 4 msec square wave pulses at 100 Hz. The l-isomer of propranolol increased the ventricular fibrillation threshold (VFT) above control values at all concentrations; the maximum increase ranged from 17.8 to greater than 420.8% change from control. In contrast, the d-isomer caused only a small increase in the ventricular fibrillation threshold with the maximum increase ranging between 14.0 and 65.2% change from control. The maximum increase in VFT for the racemic mixture of propranolol was 44.7 to greater than 500.0% above control and was similar to the l-isomer alone. Since the beta-blocking potency of the l-isomer is 100 times the potency of the d-isomer we conclude that propranolol's action in increasing the ventricular fibrillation threshold is dependent on its beta-blocking effect.

摘要

在22只戊巴比妥钠麻醉的开胸犬中,分别在存在浓度为0.2、0.5和1.0mg/kg的普萘洛尔d-异构体或l-异构体的情况下,测定诱发心室颤动所需的最小电流。以350毫秒的恒定基本周期长度从右心房对心脏进行起搏,并在易损期向右心室输送电流,输送方式为以100Hz频率、持续120毫秒的4毫秒方波脉冲序列。普萘洛尔的l-异构体在所有浓度下均使心室颤动阈值(VFT)高于对照值;最大增幅范围为相对于对照变化17.8%至大于420.8%。相比之下,d-异构体仅使心室颤动阈值有小幅增加,最大增幅范围为相对于对照变化14.0%至65.2%。普萘洛尔外消旋混合物的VFT最大增幅高于对照44.7%至大于500.0%,且与单独的l-异构体相似。由于l-异构体的β受体阻滞效能是d-异构体的100倍,我们得出结论,普萘洛尔增加心室颤动阈值的作用取决于其β受体阻滞效应。

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