NM441およびその活性本体のGABA受容体結合に及ぼす影響

• 堀 誠治

  聖マリアンナ医科大学難病治療研究センター臨床薬理部門

• 嶋田 甚五郎

  聖マリアンナ医科大学難病治療研究センター臨床薬理部門

書誌事項

タイトル別名

• Effect of NM441 and its active form on GABA receptor binding

抄録

New quinolones have been reported to have potent convulsant activity, and the concurrent administration of non-steroidal anti-inflammatory drugs (NSAIDs) has been reported to enhance this convulsant activity. We studied the effect of NM441, a newly developed quinolone, and NM394, an active metabolite of NM441, and its metabolites on the receptor binding of γ-aminobutyric acid (GABA), which is an inhibitory transmitter in the mammalian central nervous system (CNS). NM394 and NM441 inhibited GABA receptor binding in a concentration-dependent manner. The potency in the inhibition of the binding was between that of enoxacin and ciprofloxacin. In the presence of biphenylacetic acid (BPA), the inhibitory activity of NM394 was remarkably enhanced. The oxo-derivative and the ethylene-diamino-derivative inhibited GABA receptor binding, and their potencies were almost the same as NM394. But the inhibitory activity of the metabolites was little enhanced in the presence of BPA. These in vitro results suggest that NM394 induces convulsions through the inhibition of GABA receptor binding when it accumulates in the CNS, and that the concurrent administration of NSAIDs enhances the convulsant activity of NM394.

収録刊行物

• 日本化学療法学会雑誌

  日本化学療法学会雑誌 44 (Supplement1), 97-101, 1996

  公益社団法人 日本化学療法学会

キーワード

• キノロン薬
• 痙攣
• GABA受容体
• 非ステロイド系消炎薬
• NM441

詳細情報

• CRID: 1390001206289509376
• NII論文ID: 10007601311
• NII論文ID: 130004297781
• NII書誌ID: AN10472127
• DOI: 10.11250/chemotherapy1995.44.supplement1_97
• ISSN: 18845886
• ISSN: 13407007
• Web Site: https://search.jamas.or.jp/link/ui/1996196959
• 本文言語コード: ja
• データソース種別:
  • JaLC
  • CiNii Articles
• 抄録ライセンスフラグ: 使用不可