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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
  • 本地全文:下载
  • 作者:Seiichi Kobashi ; Masayuki Takizawa ; Hajime Kubo
  • 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
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