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吗啡丙酯的抗伤害感受活性:重新评估

Antinociceptive activity of propionyl esters of morphine: a reevaluation.

作者信息

Whitehouse L W, Paul C J, Gottschling K H, Lodge B A, By A W

机构信息

Bureau of Drug Research, Health and Welfare Canada, Ottawa, Ontario.

出版信息

J Pharm Sci. 1990 Apr;79(4):349-50. doi: 10.1002/jps.2600790416.

DOI:10.1002/jps.2600790416
PMID:2352148
Abstract

The antinociceptive activity of the propionyl homologues of 3-O- and 6-O-acetyl- and 3,6-O-diacetylmorphine was re-investigated using materials of unequivocally established structure. Testing was in male Wistar rats at 60 min following subcutaneous administration by the rat tail-flick method. Results indicate that the antinociceptive activity of 3-O-propionylmorphine was similar to that of 3-O-acetylmorphine. 6-O-Propionylmorphine and 3,6-O-dipropionylmorphine had similar antinociceptive activity and, like 6-O-acetylmorphine, 6-O-propionylmorphine may be the pharmacologically active principle responsible for the antinociceptive activity of its disubstituted homologue.

摘要

使用结构明确的材料,对3-O-和6-O-乙酰基以及3,6-O-二乙酰吗啡的丙酰基同系物的抗伤害感受活性进行了重新研究。通过大鼠甩尾法,在雄性Wistar大鼠皮下给药60分钟后进行测试。结果表明,3-O-丙酰吗啡的抗伤害感受活性与3-O-乙酰吗啡相似。6-O-丙酰吗啡和3,6-O-二丙酰吗啡具有相似的抗伤害感受活性,并且与6-O-乙酰吗啡一样,6-O-丙酰吗啡可能是其双取代同系物抗伤害感受活性的药理活性成分。

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