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标题：Antinociceptive Effects of N-Acyloctahydropyrido[3,2,1-ij][1,6]naphthyridine in Mice: Structure–Activity Relation Study of Matrine-Type Alkaloids Part II
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作者：Seiichi Kobashi ; Masayuki Takizawa ; Hajime Kubo 等
期刊名称：Biological and Pharmaceutical Bulletin
印刷版ISSN：0918-6158
电子版ISSN：1347-5215
出版年度：2003
卷号：26
期号：3
页码：375-379
DOI：10.1248/bpb.26.375
出版社：The Pharmaceutical Society of Japan
摘要：N -Acyloctahydropyrido[3,2,1- ij ][1,6]naphthyridines were synthesized as derivatives of matrine-type alkaloids, and the structure–activity relations were examined by the acetic acid-induced abdominal contraction test. The antinociceptive potencies of N -acyloctahydropyrido[3,2,1- ij ][1,6]naphthyridines were significantly lower than those of (+)-matrine. The antinociceptive effects of N -benzyloctahydropyrido[3,2,1- ij ][1,6]naphthyridines are approximately 5.6 to 6.5 times less than those of N -benzoyloctahydropyrido[3,2,1- ij ][1,6]naphthyridine. These findings suggest that the amide group of matrine-type alkaloids is an essential functional group that influences antinociceptive potency. The antinociceptive effect of 4c was markedly antagonized by pretreatment with Naloxone, and that of 3c partially so.
关键词：structure–activity relationship;antinociception;matrine