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关于反式-2-氨基-3-羟基-1,2,3,4-四氢萘的一种N-取代哌嗪衍生物的抗心律失常活性。

On the antiarrhythmic activity of one N-substituted piperazine derivative of trans-2-amino-3-hydroxy-1, 2, 3, 4-tetrahydroanaphthalene.

作者信息

Staneva-Stoycheva D, Boyadjiev T, Raynova L, Mihaylova S, Tomov T

出版信息

Acta Physiol Pharmacol Bulg. 1979;5(3):51-8.

PMID:44072
Abstract

The antiarrhythmic activity of the compound N-(trans-3-hydroxy-1,2,3,4-tetrahydro-2-naphthyl)-N-(3-oxo-3-phenyl-2-methylpropyl)-piperazine hydrochloride, referred to as P11, is studied on anaesthesized cats and Wistar albino rats, as well as on non-anaesthesized rabbits. Four types of experimental arrhythmia are used--with BaCl2, with chloroform-adrenaline, with strophantine G and with aconitine. The compound P11 is introduced in doses of 0.25 and 0.50 mg/kg intravenously and 10 mg/kg orally. The compound manifests antiarrhythmic activity in all models of experimental arrhythmia used, causing greatest inhibition on the arrhythmia induced by chloroform-adrenaline (in 90 per cent) and with BaCl2 (in 84 per cent). The results obtained are associated with the beta-adrenoblocking and with the membrane-stabilizing action of the compound.

摘要

化合物N-(反式-3-羟基-1,2,3,4-四氢-2-萘基)-N-(3-氧代-3-苯基-2-甲基丙基)-哌嗪盐酸盐,简称P11,在麻醉猫、Wistar白化大鼠以及未麻醉的兔子身上研究了其抗心律失常活性。使用了四种类型的实验性心律失常模型——由氯化钡、氯仿-肾上腺素、毒毛旋花子苷G和乌头碱诱导的模型。化合物P11通过静脉注射以0.25和0.50mg/kg的剂量给药,口服给药剂量为10mg/kg。该化合物在所使用的所有实验性心律失常模型中均表现出抗心律失常活性,对氯仿-肾上腺素诱导的心律失常(90%)和氯化钡诱导的心律失常(84%)抑制作用最强。所得结果与该化合物的β-肾上腺素能阻滞作用和膜稳定作用有关。

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