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抗炎剂10-甲胺-11-H-茚并-[1,2-b]喹啉-11-酮(MB432)的药理特性

Pharmacological properties of the antiinflammatory agent 10-methylamine-11-H-indeno-[1,2-b]quinolin-11-one (MB432).

作者信息

Chojnacka-Wójcik E, Naparzewska A

出版信息

Pol J Pharmacol Pharm. 1983;35(4):327-32.

PMID:6607462
Abstract

10-Methylamine-11-H-indeno [1,2-b] quinolin-11-one (MB432) was found to be a prostaglandin synthetase inhibitor, to display antiinflammatory activity in carrageenin edema and cotton pellet granuloma tests in rats, and to exert analgesic action in paw pressure test in rats and in the writhing test in mice. The therapeutic index (LD50/ED50) for antiinflammatory and analgesic effect of MB432 is higher than that of indomethacin (IND) and phenylbutazone (PHB). The acute toxicity of MB432 is low but the drug showed high ulcerogenic activity. The ratio of medium ulcerogenic to median antiinflammatory and analgesic doses of MB432 is comparable to that of PHB but higher than for IND.

摘要

10-甲胺基-11-H-茚并[1,2-b]喹啉-11-酮(MB432)被发现是一种前列腺素合成酶抑制剂,在大鼠角叉菜胶性水肿和棉球肉芽肿试验中显示出抗炎活性,并在大鼠爪压试验和小鼠扭体试验中发挥镇痛作用。MB432抗炎和镇痛作用的治疗指数(LD50/ED50)高于吲哚美辛(IND)和保泰松(PHB)。MB432的急性毒性较低,但该药物显示出高致溃疡活性。MB432的中度致溃疡剂量与中度抗炎和镇痛剂量之比与PHB相当,但高于IND。

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