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具有潜在抗焦虑活性的双环[2.2.2]辛-7-烯-2,3,5,6-四羧酸二亚胺的N,N'-双氨基烷基取代衍生物的合成。

Synthesis of N,N'-bis-aminoalkyl-substituted derivatives of bicyclo[2.2.2]oct-7-ene-2,3,5,6-tetracarboxydiimide with potential anxiolytic activity.

作者信息

Turło J, Zawadowski T

机构信息

Katedra i Zakład Chemii Medycznej, Akademia Medyczna w Warszawie, Polska (Poland).

出版信息

Farmaco. 1996 Dec;51(12):815-8.

PMID:9050215
Abstract

In continuation of the search for discovering new antipsychotic and anxiolytic agents with a reduced production of extrapyramidala side-effects, a series of N,N'-bis-aminoalkyl derivatives of bicyclo[2.2.2]oct-7-ene tetracarboxydiimide was prepared. Evaluation of these compounds in vitro revealed a very low affinity for 5-HT1A receptor.

摘要

为了继续寻找具有减少锥体外系副作用的新型抗精神病和抗焦虑药物，制备了一系列双环[2.2.2]辛-7-烯四羧酸二酰亚胺的N,N'-双氨基烷基衍生物。对这些化合物的体外评估显示其对5-HT1A受体的亲和力非常低。

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