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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概要
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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-dialkylaminopiperidiaes 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.
- 公益社団法人日本薬学会の論文
- 2002-08-01
著者
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Kubo H
New Product Research Laboratories Ii Daiichi Pharmaceutical Company Ltd.
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KOBASHI Seiichi
Faculty of Medicinal Chemistry; Hoshi University
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KUBO Hajime
Faculty of Medicinal Chemistry; Hoshi University
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YAMAUCHI Takayasu
Faculty of Medicinal Chemistry; Hoshi University
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HIGASHIYAMA Kimio
Faculty of Medicinal Chemistry; Hoshi University
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HIGASHIYAMA Kimio
Institute of Medicinal Chemistry, Hoshi University
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Yamauchi T
Faculty Of Medicinal Chemistry; Hoshi University
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Higashiyama Kimio
Institute Of Medicinal Chemistry Hoshi University
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Higashiyama K
Faculty Of Pharmaceutical Sciences Okayama University
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