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[2-(4'R')苄基-5R-苯并咪唑的制备及药理活性。镇痛活性及对条件性回避反应的影响]

[Preparation and pharmacologic activity of 2-(4'R')benzyl-5R-benzimidazole. Analgesic activity and effect on conditioned avoidance response].

作者信息

Paglietti G, Pirisi M A, Loriga M, Grella G E, Sparatore F, Satta M, Manca P, Peana A

机构信息

Istituto di Chimica Farmaceutica e Tossicologica, Università di Sassari.

出版信息

Farmaco Sci. 1988 Mar;43(3):203-14.

PMID:3417006
Abstract

Several derivatives of 2-benzylbenzimidazole (dibazole) bearing substituents on positions 5 and 4' were prepared and tested, together with dibazole, for their activity on the acquisition of a conditioned avoidance response and for analgesic activity. Chlorpromazine and acetylsalicylic acid were used as standards. Analgesic activity was found for all these compounds, most of which proved more active than A.S.A. As regards the acquisition of a C.A.R., the 5-chloroderivatives exhibit a strong inhibitory activity, that for compound (VIII) is equal to that of chloropromazine, while dibazole and the 5-trifluormethylderivatives stimulate the acquisition.

摘要

制备并测试了几种在5位和4'位带有取代基的2-苄基苯并咪唑(双苯唑)衍生物,以及双苯唑,考察它们对条件性回避反应习得的活性和镇痛活性。以氯丙嗪和乙酰水杨酸作为标准对照。发现所有这些化合物均具有镇痛活性,其中大多数的活性比阿司匹林更强。关于条件性回避反应的习得,5-氯衍生物表现出强烈的抑制活性,化合物(VIII)的抑制活性与氯丙嗪相当,而双苯唑和5-三氟甲基衍生物则促进反应的习得。

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