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[对中枢神经系统有活性的 1,4 - 二取代 1,3 - 二氢 - 2H - 1,5 - 苯并及氯苯并二氮杂䓬 - 2 - 酮]

[1,4-Disubstituted 1,3-dihydro-2H-1,5-benzo- and chlorobenzodiazepin-2-ones with activity on the central nervous system].

作者信息

Savelli F, Boido A, Mulè A, Piu L, Alamanni M C, Pirisino G, Satta M, Peana A

机构信息

Istituto di Scienze Farmaceutiche, Università di Genova.

出版信息

Farmaco. 1989 Feb;44(2):125-40.

PMID:2775411
Abstract

In pursuing the study on pyridodiazepinone derivatives, in order to verify the variation of biological activity induced by replacement of the heteroaromatic with an aromatic nucleus and by the introduction of chlorine on the benzene ring, a series of 1-[(dialkylamino)alkyl]-4-phenyl-1,3-dihydro-2H-1,4-benzodiazepin- 2-ones and of 7-chloro-analogues were prepared. Some benzodiazepinones and their 7-chloro-analagous were subjected to pharmacological experimentation in order to evaluate and compare their effect upon mice with regard to exploratory activity, motor coordination and spontaneous motility. In addition their anti-strychnine, anti-cardiazole, anti-amphetamine and anti-reserpine activities were also evaluated.

摘要

在进行吡啶并二氮杂䓬酮衍生物的研究过程中,为了验证用芳环取代杂芳环以及在苯环上引入氯原子所引起的生物活性变化,制备了一系列1-[(二烷基氨基)烷基]-4-苯基-1,3-二氢-2H-1,4-苯并二氮杂䓬-2-酮及其7-氯类似物。对一些苯并二氮杂䓬酮及其7-氯类似物进行了药理实验,以评估和比较它们对小鼠在探索活动、运动协调性和自发运动方面的影响。此外,还评估了它们的抗士的宁、抗戊四氮、抗苯丙胺和抗利血平活性。

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