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苄普地尔(1-[3-异丁氧基-2-(苄基苯基)氨基]丙基吡咯烷盐酸盐)——一种新型潜在抗心绞痛化合物的心血管药理学

Cardiovascular pharmacology of bepridil (1[3 isobutoxy 2 (benzylphenyl) amino] propyl pyrrolidine hydrochloride) a new potential anti-anginal compound.

作者信息

Cosnier D, Duchenne-Marullaz P, Rispat G, Streichenberger G

出版信息

Arch Int Pharmacodyn Ther. 1977 Jan;225(1):133-51.

PMID:849059
Abstract

In dogs intravenous bepridil (2.5 mg/kg) increased coronary sinus blood flow and PVO2. Arterial pressure was briefly lowered, and heart rate was slowed in animals with intact or denervated hearts, or after propranolol administration. Ventricular inotropism was reduced at higher doses. Bepridil (5 mg/kg i.v.) showed a partial antagonist activity on isoprenaline cardiovascular effects (or cardiac sympathetic stimulation effects) i.e. tachycardia, increase in left dP/dt max. and diastolic hypotension. The antitachycardia activity was particularly pronounced. It was found to be non-competitive. It was also found to be non-specific since glucagon, theophylline- and papaverine-induced tachycardia were also reduced. The continuous infusion of high doses of bepridil did not cause any disturbance in atrio-ventricular or intraventricular conduction. In rats, after 50 mg/kg/day p.o., bepridil did not alter myocardial noradrenaline levels.

摘要

在犬类中,静脉注射苄普地尔(2.5毫克/千克)可增加冠状窦血流量和混合静脉血氧分压。动脉压短暂降低,在心脏完整或去神经支配的动物中,或在给予普萘洛尔后,心率减慢。高剂量时心室收缩性降低。静脉注射苄普地尔(5毫克/千克)对异丙肾上腺素的心血管效应(或心脏交感神经刺激效应),即心动过速、左心室最大dp/dt增加和舒张期低血压,表现出部分拮抗活性。抗心动过速活性尤为明显。发现它是非竞争性的。还发现它是非特异性的,因为胰高血糖素、茶碱和罂粟碱诱导的心动过速也会降低。持续输注高剂量的苄普地尔不会引起房室或心室内传导的任何紊乱。在大鼠中,口服苄普地尔50毫克/千克/天后,不会改变心肌去甲肾上腺素水平。

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