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  • 标题:Metabolism of Diltiazem. I. Structures of New Acidic and Basic Metabolites in Rat, Dog and Man
  • 本地全文:下载
  • 作者:Yoichi SUGAWARA ; Motoaki OHASHI ; Susumu NAKAMURA
  • 期刊名称:Biological and Pharmaceutical Bulletin
  • 印刷版ISSN:0918-6158
  • 电子版ISSN:1347-5215
  • 出版年度:1988
  • 卷号:11
  • 期号:4
  • 页码:211-223
  • DOI:10.1248/bpb1978.11.211
  • 出版社:The Pharmaceutical Society of Japan
  • 摘要:The metabolites of diltiazem in the urine of rats, dogs and man and rat bile were investigated. New metabolites including six acidic metabolites (A1-A6) and four basic metabolites (M9, MB, MC, MD) were isolated by high performance liquid chromatography and their structures were characterized by gas chromatography-mass spectrometry. Acidic metabolites A1, A2, A3, A4 and basic metabolite MD identified by comparing their properties with the synthetic compounds ; (+)-(2S, 3S)-2-(4-methoxyphenyl)-3-acetoxy-4-oxo-2, 3, 4, 5-tetrahydro-1, 5-benzothiazepin-5-acetic acid (A1), 3-deacetyl-A1 (A2), O-demethyl-A1 (A3), O-demethyl-3-deacetyl-A1 (A4) and N-didemethyl-diltiazem (MD). All acidic metabolites have a CH2COOH group which may be formed by oxidative deamination of the CH2CH2N (CH3)2 group of diltiazem.
  • 关键词:plasma
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