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一种具有类似胺碘酮血流动力学特征的潜在抗心绞痛苯并[b]噻吩。

A potentially antianginal benzo [b]thiophene with an amiodarone-like haemodynamic profile.

作者信息

Charlier R, Bauthier J, Richard J

出版信息

Arzneimittelforschung. 1975 Jan;25(1):46-52.

PMID:238543
Abstract

L 9146 or 2-methyl-3(3,5 dimethyl-4-gamma-di-n-butylaminopropoxy-benzoyl)-benzo [b] thiophene is a substance belonging to the amiodarone series which induces in the anaesthetized dog a decrease of myocardial oxygen consumption which is mainly due to slowing of the heart rate and reduction in systemic blood pressure. L 9146 also enhances coronary blood flow. L 9146 has also antiadrenergic properties since catecholamine-induced hypertension, tachycardia and increase of myocardial oxygen consumption are markedly antagonized; these antiacrenergic effects are not due to a competitive blockade of the beta-adrenoceptors. L 9146 does not decrease cardiac output, but increases it appreciably in the initial phase of its action. Several findings indicate that when the intensity of certain properties is considered, l9146 is more active than aniodarone since only half the dose used with aniodarone is required to achieve a given level of action. The overall haemodynamic properties of L 9146, which are similar to those of amiodarone, are considered to be potentially valuable for the long-term treatment of angina pectoris.

摘要

L 9146或2-甲基-3(3,5-二甲基-4-γ-二正丁基氨基丙氧基-苯甲酰基)-苯并[b]噻吩是一种属于胺碘酮系列的物质,它能使麻醉犬的心肌耗氧量降低,这主要是由于心率减慢和全身血压降低所致。L 9146还能增加冠状动脉血流量。L 9146还具有抗肾上腺素能特性,因为儿茶酚胺引起的高血压、心动过速和心肌耗氧量增加会受到明显拮抗;这些抗肾上腺素能作用并非由于β-肾上腺素能受体的竞争性阻断。L 9146不会降低心输出量,但其在作用初期会明显增加心输出量。多项研究结果表明,从某些特性的强度来看,L 9146比胺碘酮更具活性,因为达到给定作用水平所需的剂量仅为胺碘酮的一半。L 9146的整体血流动力学特性与胺碘酮相似,被认为对心绞痛的长期治疗具有潜在价值。

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