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藜芦碱和BDF 9148对大鼠右心室动作电位及收缩性的影响。

The effects of veratridine and BDF 9148 on the action potentials and contractility of the rat right ventricle.

作者信息

Doggrell S A, Bishop B E, Brosch S

机构信息

Department of Pharmacology and Clinical Pharmacology, School of Medicine, University of Auckland, New Zealand.

出版信息

Gen Pharmacol. 1995 May;26(3):593-601. doi: 10.1016/0306-3623(94)00221-8.

DOI:10.1016/0306-3623(94)00221-8
PMID:7789734
Abstract
  1. The effects of veratridine, BDF 9148 and lignocaine on the action potentials and contractile force of the electrically-driven rat right ventricle have been determined. 2. Veratridine at 10(-7)-10(-6) M and BDF 9148 at 10(-7)-10(-5) M had no effect on the threshold potential or amplitude but prolonged the ventricular action potentials. 3. In contractility studies, veratridine at 10(-7)-10(-6) M augmented the cardiac stimulation responses and the augmenting effects with 3 x 10(-7) and 10(-6) M were greater at 2 than 4 Hz. In the presence of veratridine at 3 x 10(-6) M, the ventricle would not pace. 4. BDF 9148 at 10(-7)-10(-5) M augmented the cardiac stimulation responses and the augmenting effects with 10(-7) and 3 x 10(-7) M were greater at 2 than 4 Hz and the effect was maximal at 3 x 10(-7) M and submaximal at 10(-5) M. The effects of BDF 9148 at 10(-5) were not readily reversible. 5. Lignocaine at 10(-4) M had no effect on the ventricular action potential duration but decreased the threshold potential and amplitude and also reduced the cardiac stimulation force responses. In the presence of lignocaine, the augmenting effects of veratridine and BDF 9148 on ventricular force were reduced. 6. In summary this study has shown that BDF 9148 prolongs the action potential and augments the contractile force responses of the rat right ventricle by a lignocaine-sensitive mechanism. BDF 9148 or similar drugs may have potential as positive inotropes in the treatment of heart failure.
摘要
  1. 已测定藜芦定、BDF 9148和利多卡因对电驱动大鼠右心室动作电位和收缩力的影响。2. 10(-7)-10(-6)M的藜芦定和10(-7)-10(-5)M的BDF 9148对阈电位或幅度无影响,但延长了心室动作电位。3. 在收缩性研究中,10(-7)-10(-6)M的藜芦定增强了心脏刺激反应,3×10(-7)和10(-6)M时的增强作用在2Hz比4Hz时更大。在3×10(-6)M的藜芦定存在下,心室不会起搏。4. 10(-7)-10(-5)M的BDF 9148增强了心脏刺激反应,10(-7)和3×10(-7)M时的增强作用在2Hz比4Hz时更大,且在3×10(-7)M时作用最大,在10(-5)M时作用次最大。10(-5)M的BDF 9148的作用不易逆转。5. 10(-4)M的利多卡因对心室动作电位持续时间无影响,但降低了阈电位和幅度,还降低了心脏刺激力反应。在利多卡因存在下,藜芦定和BDF 9148对心室力的增强作用减弱。(6)总之,本研究表明BDF 9148通过一种利多卡因敏感机制延长动作电位并增强大鼠右心室的收缩力反应。BDF 9148或类似药物在治疗心力衰竭方面可能有作为正性肌力药的潜力。

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