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吗啡新衍生物的药理活性

Pharmacological activity of new derivatives of morphine.

作者信息

Spyraki C, Papaïoannou G, Tsatsas G, Varonos D

出版信息

Arzneimittelforschung. 1980;30(3):467-70.

PMID:7387757
Abstract

Three new derivatives of morphine: O3-(beta-isopropylaminoethyl) ether of morphine (T .3289), O3, O6-[N,N'-bis(methylcarbamate] ester of morphine (T .3298) and beta-dimethylamino-ethyl-ether of dihydromorphinone (T .3403) were tested for their action on CNS. A detailed study of pain threshold, motor activity, conditioned behavior and noradrenaline levels in brain was carried out. The compounds T .3289 and T .3298 exhibited analgesic action. The spontaneous activity of rats was decreased by T .3289 and increased by T .3298. The conditioned avoidance response was decreased and the brain nor-adrenaline levels were altered.

摘要

三种新的吗啡衍生物

吗啡的O3-(β-异丙基氨基乙基)醚(T.3289)、吗啡的O3,O6-[N,N'-双(甲基氨基甲酸酯)]酯(T.3298)和二氢吗啡酮的β-二甲基氨基乙醚(T.3403),对它们在中枢神经系统的作用进行了测试。对痛阈、运动活性、条件行为和脑中去甲肾上腺素水平进行了详细研究。化合物T.3289和T.3298表现出镇痛作用。T.3289使大鼠的自发活动降低,而T.3298使其增加。条件回避反应降低,脑中去甲肾上腺素水平发生改变。

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