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紫铆因及其半合成衍生物的一些药理学研究。

Some pharmacological investigations of embelin and its semisynthetic derivatives.

作者信息

Gupta O P, Ali M M, Ray Ghatak B J, Atal C K

出版信息

Indian J Physiol Pharmacol. 1977 Jan-Mar;21(1):31-9.

PMID:873589
Abstract

Embelin, obtained from Embolin ribes was condensed with different primary amines. Depending on the conditions of reaction, disalts or diimines were formed. Ten such disalts and fourteen diimines were developed. Embelin and all its disalts showed analgesic activity whereas all the diimines derivatives were inactive. The disalt, 2:5 disobutyl amine embelin showed maximum action. Analgesic effect was noticed only after intraperitoneal administration but not after subcutaneous, intramuscular or oral administration. The compounds cause some local irritation. The possibility of peritoneal irritation rendering the animals unresponsive to experimental pain seems to deserve consideration. However, analgesic effect could be seen in dogs and cats after intravenous injection. Embelin and its disalt, 2:5 isobutyl amine embelin also exhibited antipyretic and antiinflammatory activities.

摘要

从酸藤子中提取的紫铆因与不同的伯胺进行缩合反应。根据反应条件,生成了二元盐或二亚胺。共制备了10种此类二元盐和14种二亚胺。紫铆因及其所有二元盐均显示出镇痛活性,而所有二亚胺衍生物均无活性。二元盐2:5二丁胺紫铆因的作用最强。仅腹腔注射后可观察到镇痛效果,皮下、肌肉或口服给药后则无此效果。这些化合物会引起一些局部刺激。腹膜刺激导致动物对实验性疼痛无反应的可能性似乎值得考虑。然而,静脉注射后在犬和猫中可观察到镇痛效果。紫铆因及其二元盐2:5异丁胺紫铆因还具有解热和抗炎活性。

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