文章基本信息

标题：Antinociceptive Effects of 1-Acyl-4-dialkylaminopiperidine and 1-Alkyl-4-dialkylaminopiperidine in Mice: Structure–Activity Relation Study of Matrine-Type Alkaloids
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作者：Seiichi Kobashi ; Hajime Kubo ; Takayasu Yamauchi 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：2002
卷号：25
期号：8
页码：1030-1034
DOI：10.1248/bpb.25.1030
出版社：The Pharmaceutical Society of Japan
摘要：We previously reported that (+)-matrine and (+)-allomatrine have antinociceptive properties mediated mainly through the activation of κ-opioid receptors. 1-Acyl-4-dialkylaminopiperidines were synthesized as the simplest derivatives of matrine, and the structure–activity relations were examined by the acetic acid-induced abdominal contraction test. The antinociceptive potencies of 1-alkyl-4-dialkylaminopiperidines were significantly lower than those of the corresponding 1-acyl-4-dialkylaminopiperidines. These findings suggest that the amide group of (+)-matrine is an essential functional group that influences antinociceptive potency.
关键词：structure activity relationship;antinociception;matrine