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[四氢喹啉和四氢异喹啉的制备及其镇痛活性]

[Preparation and analgesic activity of tetrahydroquinolines and tetrahydroisoquinolines].

作者信息

Ferranti A, Garuti L, Giovanninetti G, Gaggi R, Roncada P, Nardi P

出版信息

Farmaco Sci. 1987 Apr;42(4):237-49. doi: 10.1002/chin.198744211.

Abstract

A series of 1,2,3,4-tetrahydroquinolines and of 1,2,3,4-tetrahydroisoquinolines were synthesised and evaluated for analgesic activity by both hot-plate and acetic acid writhing methods in rats. Te most potent compound was 2-methyl-1,2,3,4-tetrahydro-5-quinolinol (IV i) which was shown to be 1/8 and 1/50 as active as morphine according to the employed assay. The analgesic activity was shown to be associated to a not selective action on the CNS.

摘要

合成了一系列1,2,3,4-四氢喹啉和1,2,3,4-四氢异喹啉,并通过热板法和醋酸扭体法在大鼠身上评估了它们的镇痛活性。最有效的化合物是2-甲基-1,2,3,4-四氢-5-喹啉醇(IV i),根据所采用的试验,其活性分别为吗啡的1/8和1/50。结果表明,镇痛活性与对中枢神经系统的非选择性作用有关。

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