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具有潜在抗抑郁活性的二取代四氢咔唑的合成。

Synthesis of disubstituted tetrahydrocarbazoles with potential antidepressive activity.

作者信息

Giancaspro G I, Pizzorno M T, Albonico S M, Bindstein E, Garofalo A, Zeichen R

机构信息

Iquimefa-Conicet-Facultad de Farmacia y Bioquimica Universidad de Buenos Aires, Argentina.

出版信息

Farmaco. 1989 May;44(5):483-93.

PMID:2789627
Abstract

A new series of disubstituted tetrahydrocarbazoles were synthesized. They are tested for antidepressive activity by the Porsolt's forced swimming test (one of the acute stress methods) and by the prevention of reserpine induced hypothermia and ptosis in mice. 3-Morpholino-1-[N-(6-methoxy-1,2,3,4- tetrahydrocarbozolyl)2-propanol, fumarate (XI) was demonstrated to be the most promising compound of this series. Besides, this series did not present the most common adverse effects of the conventional tricyclic-antidepressants (loss of locomotor coordination, ataxia and anticholinergic activity).

摘要

合成了一系列新的二取代四氢咔唑。通过波索尔特强迫游泳试验(一种急性应激方法)以及预防小鼠利血平诱导的体温过低和眼睑下垂来测试它们的抗抑郁活性。3-吗啉代-1-[N-(6-甲氧基-1,2,3,4-四氢咔唑基)]-2-丙醇富马酸盐(XI)被证明是该系列中最有前景的化合物。此外,该系列没有表现出传统三环抗抑郁药最常见的不良反应(运动协调丧失、共济失调和抗胆碱能活性)。

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