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安匹托林一些稠合类似物的合成与镇痛活性

Synthesis and analgesic activity of some condensed analogs of anpirtoline.

作者信息

Rádl S, Kovárová L, Hezky P, Vosátka V, Königová O, Proska J, Krejcí I

机构信息

Research Institute of Pharmacy and Biochemistry, Prague, Czech Republic.

出版信息

Arch Pharm (Weinheim). 1999 Jun;332(6):208-12. doi: 10.1002/(sici)1521-4184(19996)332:6<208::aid-ardp208>3.0.co;2-0.

Abstract

New condensed derivatives of anpirtoline, in which the pyridine ring is replaced with quinoline, isoquinoline, quinazoline, and phthalazine nuclei, have been synthesized. Their receptor binding profiles (5-HT1A, 5-HT1B) and analgesic activity (hot plate, acetic acid induced writhing) have been studied. The analgesic activity of compounds 7d, 8b, 8c, and 8e are at least comparable to that of the clinically used drugs flupirtine and tramadol under the same conditions.

摘要

已合成了安吡托林的新型缩合衍生物,其中吡啶环被喹啉、异喹啉、喹唑啉和酞嗪核取代。研究了它们的受体结合谱(5-HT1A、5-HT1B)和镇痛活性(热板法、醋酸诱导扭体法)。在相同条件下,化合物7d、8b、8c和8e的镇痛活性至少与临床使用的药物氟吡汀和曲马多相当。

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