[2-(4' r ')苄基- 5r -苯并咪唑和2-(4'-吡啶基)- 5r -苯并咪唑的制备及药理活性。]镇痛活性及其对条件回避反应的影响[j]。

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
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引用次数: 0

摘要

制备了16种2-(4' r ')苯基- 5r -苯并咪唑和2-(4'-吡啶基)- 5r -苯并咪唑,并与2-苯基苯并咪唑一起测定了它们在大鼠身上获得条件回避反应的活性和小鼠的镇痛活性,并与氯丙嗪和乙酰水杨酸进行了比较。一些化合物强烈抑制C.A.R的获得,其中2-(4′-烷氧基)苯并咪唑(XVI)和(XVII)明显超过氯丙嗪。镇痛活性也普遍存在于所检查的化合物中;在5位上含有三氟甲基或乙酰基的化合物表现出比乙酰水杨酸更高的活性。去调节和镇痛活动彼此不相关。
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[Preparation and pharmacologic activity of 2-(4'R')benzyl-5R-benzimidazole and 2-(4'-pyridinyl)-5R-benzimidazoles. Analgesic activity and effect on conditioned avoidance response].

Sixteen 2-(4'R')phenyl-5R-benzimidazoles and two 2-(4'-pyridinyl)-5R-benzimidazoles were prepared and tested, together with 2-phenylbenzimidazole, for their activity on the acquisition of a conditioned avoidance response in rats and for analgesic activity in mice, and compared with chlorpromazine and acetylsalicylic acid. Several compounds inhibit strongly the acquisition of a C.A.R., with 2-(4'-alkoxy)phenylbenzimidazoles (XVI) and (XVII) clearly exceeding chlorpromazine. Analgesic activity is also generally present in the examined compounds; those bearing in the position 5 a trifluoromethyl or an acetyl group exhibit an activity higher than that of acetylsalicylic acid. Deconditioning and analgesic activities are not correlated with each other.

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