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胆碱酯酶抑制剂加兰他敏的镇痛作用研究。

Study of the analgesic effects of galanthamine, a cholinesterase inhibitor.

作者信息

Cozanitis D A, Friedmann T, Fürst S

出版信息

Arch Int Pharmacodyn Ther. 1983 Dec;266(2):229-38.

PMID:6667067
Abstract

The effects of galanthamine, an alkaloidal anticholinesterase agent whose chemical structure bears similarity to codeine, was studied in various animal and isolated organ tests. Antinociceptive activity of galanthamine given subcutaneously was detected and compared to physostigmine and morphine in the rat hot plate test. Naloxone partially blocked the effect of galanthamine but not that of physostigmine. Both cholinesterase inhibitors provided analgesia in the mouse acetic acid writhing test. They potentiated the effect of morphine in the rat hot plate test but inhibited the barbiturate anaesthesia potentiation of morphine in the rat. While galanthamine provided analgesia in the intact animal, it failed to produce opiate-like activity in such isolated organs as longitudinal muscle strip of the guinea-pig ileum, mouse vas deferens, and cat nictitating membrane.

摘要

加兰他敏是一种化学结构与可待因相似的生物碱类抗胆碱酯酶药,对其在各种动物及离体器官试验中的作用进行了研究。在大鼠热板试验中检测了皮下注射加兰他敏的抗伤害感受活性,并与毒扁豆碱和吗啡进行比较。纳洛酮部分阻断了加兰他敏的作用,但未阻断毒扁豆碱的作用。两种胆碱酯酶抑制剂在小鼠醋酸扭体试验中均产生镇痛作用。它们在大鼠热板试验中增强了吗啡的作用,但在大鼠中抑制了巴比妥类麻醉对吗啡的增强作用。虽然加兰他敏在完整动物中产生镇痛作用,但在诸如豚鼠回肠纵肌条、小鼠输精管和猫瞬膜等离体器官中未能产生阿片样活性。

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