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

Il Farmaco; edizione scientifica Pub Date : 1988-03-01
G Paglietti, M A Pirisi, M Loriga, G E Grella, F Sparatore, M Satta, P Manca, A Peana
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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.

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[2-(4'R')苄基- 5r -苯并咪唑的制备及其药理活性。]镇痛活性及其对条件回避反应的影响[j]。
制备了几种具有5′和4′取代基的2-苄基苯并咪唑(二唑)衍生物,并与二唑一起对其获得条件回避反应的活性和镇痛活性进行了测试。以氯丙嗪和乙酰水杨酸为标准品。所有这些化合物都具有镇痛活性,其中大多数比A.S.A.更有活性。至于C.A.R的获得,5-氯衍生物表现出很强的抑制活性,化合物(VIII)的抑制活性与氯丙嗪相当,而二唑和5-三氟甲基衍生物则刺激获得。
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