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一种作为小鼠抗抑郁剂的2-氨基-2-恶唑啉衍生物。

A 2-amino-2-oxazoline derivative as an antidepressant in mice.

作者信息

Bourin M, Creuzet M H, Jarry C, Colombel M C

机构信息

Laboratoire de Pharmacologie, Faculté de Médecine, Nantes, France.

出版信息

Arzneimittelforschung. 1988 May;38(5):666-8.

PMID:3261982
Abstract

2-Amino-2-oxazolines are heterocyclic compounds with interesting pharmacological properties. Several derivatives of this chemical series were studied in psychopharmacological tests. One derivative 4,5-dihydro-5-[methyl(4-phenyl-1-piperazinyl)]-2-oxazolamine (COR 32-24), had an antidepressant profile. Its structure can be compared to trazodone in its phenylpiperazine group and to toloxatone in its oxazoline group. This molecule antagonized reserpine-induced hypothermia and ptosis, oxotremorine-induced hypothermia and high-dose apomorphine-induced hypothermia. It also potentiated yohimbine-induced sublethality and decreased the immobility of forced swimming. It had no monoamine oxidase inhibitory activity. These results suggest a profile close to that of viloxazine and to that of a classic antidepressant.

摘要

2-氨基-2-恶唑啉是具有有趣药理特性的杂环化合物。对该化学系列的几种衍生物进行了精神药理学测试。一种衍生物4,5-二氢-5-[甲基(4-苯基-1-哌嗪基)]-2-恶唑啉胺(COR 32-24)具有抗抑郁特性。其结构在苯基哌嗪基团方面可与曲唑酮相比较,在恶唑啉基团方面可与托洛沙酮相比较。该分子拮抗利血平诱导的体温过低和眼睑下垂、氧化震颤素诱导的体温过低以及高剂量阿扑吗啡诱导的体温过低。它还增强了育亨宾诱导的亚致死性,并减少了强迫游泳的不动时间。它没有单胺氧化酶抑制活性。这些结果表明其特性与维洛沙嗪和经典抗抑郁药的特性相近。

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