METABOLISM OF IDEBENONE (CV-2619), A NEW CEREBRAL METABOLISM IMPROVING AGENT : ISOLATION AND IDENTIFICATION OF METABOLITES IN THE RAT AND DOG

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概要

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• Metabolic studies of idebenone (CV-2619), a new cerebral metabolism improving agent, in the rat and dog by thin-layer chromatography, gas-liquid chromatography-mass spectrometry and fast atom bombardment-mass spectrometry led to characterization of the following metabolites : the parent compound, 6-(9-carboxynonyl)-2,3-dimethoxy-5-methyl-1,4-benzoquinone (QS-10), 6-(7-carboxyheptyl)-2,3-dimethoxy-5-methyl-1,4-benzoquinone (QS-8), 6-(5-carboxypentyl)-2,3-dimethoxy-5-methyl-1,4-benzoquinone (QS-6), 6-(3-carboxypropyl)-2,3-dimethoxy-5-methyl-1,4-benzoquinone (QS-4), 1- or 4-phenyl sulfate of the hydroquinone derivatives fo CV-2619 and QS-4,and 1- and 4-phenyl glucuronides of the hydroquinone derivative of QS-10. These results indicated that CV-2619 was metabolized by oxidation of the side chain followed by β-oxidation of form successively QS-10,QS-8,QS-6 and QS-4,and reduction of the quinone ring and subsequent conjugation yielding the sulfates and glucuronides of the hydroquinone derivatives of CV-2619,QS-10,QS-8,QS-6 and QS-4.

• 公益社団法人日本薬学会の論文

著者

• Torii Hiroshi

  Drug Safety Evaluation Laboratories Central Research Division Takeda Chemical Industries Ltd.

• KOBAYASHI Tadamasa

  Department of Microbiology, School of Pharmaceutical Sciences, University of Shizuoka

• YOSHIDA Kiyoshi

  Drug Analysis and Pharmacokinetics Research Laboratories, Pharmaceutical Development Division, Taked

• Tanayama S

  Takeda Chemical Ind. Ltd. Osaka Jpn

• Tanayama Shigeharu

  Drug Analysis And Pharmacokinetics Research Laboratories Pharmaceutical Development Division Takeda

• Kobayashi T

  Department Of Microbiology School Of Pharmaceutical Sciences University Of Shizuoka

• Yoshida K

  National Research Lab. Metrology Ibaraki

• KOBAYASHI TAKUO

  Drug Safety Evaluation Laboratories, Central Research Division, Takeda Chemical Industries. Ltd.

• MITANI MASAYOSHI

  Drug Safety Evaluation Laboratories, Central Research Division, Takeda Chemical Industries, Ltd.

• Mitani Masayoshi

  Drug Safety Evaluation Laboratories Central Research Division Takeda Chemical Industries Ltd.

• Yoshida Kiyoshi

  Drug Analysis And Pharmacokinetics Research Laboratories Pharmaceutical Development Division Takeda

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• Enantioselective determination of pazinaclone, a new isoindoline anxiolytic, and its active metabolite in rat plasma by high-performance liquid chromatography
• DISPOSITION OF IDEBENONE (CV-2619), A NEW CEREBRAL METABOLISM IMPROVING AGENT, IN RATS AND DOGS
• METABOLISM OF IDEBENONE (CV-2619), A NEW CEREBRAL METABOLISM IMPROVING AGENT : ISOLATION AND IDENTIFICATION OF METABOLITES IN THE RAT AND DOG

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