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新型抗高血压药2-(2-氯-对甲苯胺基)-2-咪唑啉硝酸盐(可乐定)的药理特性。I. 对血压和心率的作用

Pharmacological properties of 2-(2-chloro-p-toluidino)-2-imidazoline-nitrate (Tolonidine), a new antihypertensive agent. I. Action on blood pressure and heart rate.

作者信息

Cosnier D, Duchene-Marullaz P, Grimal J, Rispat G, Streichenberger G

出版信息

Arzneimittelforschung. 1975 Oct;25(10):1557-61.

PMID:1243037
Abstract

Tolonidine, 2-(2-chloro-p-toluidino)-2-imidazoline-nitrate, a substance structurally related to clonidine, was studied for its effects on blood pressure and heart rate in anesthetized or conscious, normotensive or hypertensive animals (mainly dogs). In all cases, blood pressure was lowered by tolonidine. Initial short-lasting hypertension was observed after each i.v. administration. Heart rate was markedly lowered irrespective of the experimental process. Comparison with clonidine, guanethidine and mecamylamine in hypertensive anesthetized or unanesthetized animals made it possible to place tolonidine with respect to these reference antihypertensive drugs. A close relationship essentially appears between the effects of both derivatives of imidazoline: tolonidine and clonidine, tolonidine being, however, active at higher doses. The analysis of these results will appear at the end of a series of three articles.

摘要

托洛尼定,即2-(2-氯-对甲苯胺基)-2-咪唑啉硝酸盐,是一种结构上与可乐定相关的物质,已在麻醉或清醒的正常血压或高血压动物(主要是狗)身上研究了其对血压和心率的影响。在所有情况下,托洛尼定都能降低血压。每次静脉注射后均观察到最初短暂的高血压。无论实验过程如何,心率均显著降低。在高血压麻醉或未麻醉动物中与可乐定、胍乙啶和美加明进行比较,使得确定托洛尼定相对于这些参考抗高血压药物的地位成为可能。咪唑啉的两种衍生物——托洛尼定和可乐定的作用之间基本上存在密切关系,然而,托洛尼定在更高剂量时才具有活性。这些结果的分析将在三篇系列文章的最后呈现。

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