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  • 标题:INHIBITORY EFFECT OF MOLECULAR MOIETY IN PAPAVERINE STRUCTURE ON CYCLIC AMP-PHOSPHODIESTERASE OF SMOOTH AND CARDIAC MUSCLES
  • 本地全文:下载
  • 作者:MASAYASU KIMURA ; ISAMI WAKI ; IKUKO KIMURA
  • 期刊名称:Biological and Pharmaceutical Bulletin
  • 印刷版ISSN:0918-6158
  • 电子版ISSN:1347-5215
  • 出版年度:1978
  • 卷号:1
  • 期号:3
  • 页码:145-152
  • DOI:10.1248/bpb1978.1.145
  • 出版社:The Pharmaceutical Society of Japan
  • 摘要:Inhibitory effects on low Km cyclic AMP-phosphodiesterase (PDE) obtained from guinea-pig ileum and rat cardiac muscle were studied using papaverine (Pap) and its related moiety compounds which were classified into group I : isoquinoline derivatives, group II : 2-veratrylpyridine derivatives and group III : 1-veratryl-veratrylamine derivatives. 3, 4-Dimethyl-2-veratryl-pyridine (P-3, 4M) belonging to group II was more effective than 1-methyl-6, 7-dimethoxy-isoquinoline (IQ) belonging to group I, but not so as Pap. Compounds in group III were little effective inhibitors. Pap and P-3, 4M seemed to be a competitive type and IQ to be a non-competitive type of compound. In the steric configuration of Pap molecule, an aphorphine type compound was more effective than a berberine type compound. Barium chloride did not exert any antagonistic effect upon low Km cyclic AMP-PDE inhibited by Pap. Potentiation effects on dose-relaxation curve induced by cyclic AMP in guinea-pig taenia coli fell into the order of Pap>P-3, 4M>IQ, being parallel with the potency order of cyclic AMP-PDE inhibition.
  • 关键词:cardiac muscle
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