Application of LC-NMR for Characterization of Rat Urinary Metabolites of Zonampanel Monohydrate (YM872)

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概要

• 論文の詳細を見る

• Zonampanel monohydrate (YM872) has a potent and selective antagonistic effect on the glutamate receptor subtype, α-amino-3-hydroxy-5-methylisoxazole-4-propionic acid (AMPA) receptor. Metabolic fingerprinting in rat urine after a single intravenous administration of ^<14>C-labeled YM872 (^<14>C-YM872) revealed the presence of two metabolites, Rl and R2. The two metabolites were semi-purified by preparative HPLC from rat urine after a single intravenous administration of non-labeled YM872, and their structures were elucidated by various instrumental analyses involving LC-NMR. The results showed that R1 and R2 have a hydroxyamino group and an amino group at the C-7 position of the quinoxalinedione skeleton, respectively. Therefore, the proposed metabolic pathway of YM872 in rats involves the reduction of the nitro group to a hydroxyamino group and then subsequent reduction to an amino group.

• 公益社団法人日本薬学会の論文
• 2004-11-01

著者

• SUZUMURA KEN-ICHI

  Analysis & Metabolism Laboratories, Institute for Drug Discovery Research, Yamanouchi Pharmaceutical

• FUNATSU MASASHI

  Analysis & Metabolism Laboratories, Institute for Drug Discovery Research, Yamanouchi Pharmaceutical

• IMAI Harumitsu

  Drug Metabolism Laboratories, Institute for Drug Development Research, Yamanouchi Pharmaceutical Co,

• Hashimoto T

  Faculty Of Pharmaceutical Sciences Hokuriku University

• 橋本 忠

  北陸大・薬

• Sohda Kin-ya

  Institute For Drug Discovery Research Yamanouchi Pharmaceutical Co. Ltd.

• Sohda Kin-ya

  Drug Metabolism Laboratories Drug Development Division Yamanouchi Pharmaceutical Co. Ltd.

• KAMIMURA Hidetaka

  Drug Metabolism Research Laboratories, Drug Discovery Research, Astellas Pharma Inc.

• Imai Harumitsu

  Drug Metabolism Laboratories Drug Development Division Yamanouchi Pharmaceutical Co. Ltd.

• MINEMATSU Tsuyoshi

  Drug Metabolism Laboratories, Drug Development Division, Yamanouchi Pharmaceutical Co., Ltd.

• HASHIMOTO Tadashi

  Drug Metabolism Laboratories, Drug Development Division, Yamanouchi Pharmaceutical Co., Ltd.

• SUZUKI Katsuhiro

  Drug Metabolism Laboratories, Drug Development Division, Yamanouchi Pharmaceutical Co., Ltd.

• USUI Takashi

  Drug Metabolism Laboratories, Drug Development Division, Yamanouchi Pharmaceutical Co., Ltd.

• Funatsu Masashi

  Analysis Research Analysis & Metabolism Laboratories Institute For Drug Discovery Research

• Suzumura Ken-ichi

  Analysis Research Analysis & Metabolism Laboratories Institute For Drug Discovery Research

• Hashimoto Tadashi

  Faculty Of Pharmaceutical Sciences Hokuriku University

• Minematsu Tsuyoshi

  Drug Metabolism Laboratories Drug Development Division Yamanouchi Pharmaceutical Co. Ltd.

• Usui Takashi

  Drug Metabolism Laboratories Drug Development Division Yamanouchi Pharmaceutical Co. Ltd.

• Suzuki K

  Drug Metabolism Laboratories Drug Development Division Yamanouchi Pharmaceutical Co. Ltd.

• Hashimoto T

  Hokuriku Univ. Kanazawa Jpn

• Suzumura K

  Yamanouchi Pharmaceutical Co. Ltd. Ibaraki Jpn

• Hashimoto Toshihiro

  Fac. Of Pharmaceutical Sciences Tokushima Bunri Univ.

• Usui T

  Drug Metabolism Research Laboratories Astellas Pharma Inc.

• Kamimura Hidetaka

  Drug Metabolism Research Laboratories Astellas Pharma Inc.

• Kamimura Hidetaka

  Drug Metabolism Department Product Development Laboratories Yamanouchi Pharmaceutical Co. Ltd.

• Hashimoto Tadashi

  Drug Metabolism Laboratories Drug Development Division Yamanouchi Pharmaceutical Co. Ltd.

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