新penem薬ritipenem (ritipenem acoxilの活性本体) の痙攣誘発作用と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
  • 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

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  • Convulsant activity of ritipenem (an active form of ritipenem acoxil) and its effect on GABA receptor binding

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Since β-lactams have been reported to induce convulsions, we studied the convulsant activity of ritipenem (RIPM), an active form of ritipenem acoxil (RIPM-AC), and its effect on the receptor binding of γ-aminobutyric acid (GABA), an inhibitory transmitter in the central nervous system. Intraventricular injection of imipenem (IPM), cefazolin (CEZ) and cephaloridine (CER) induced convulsions in mice in a dose-dependent manner, whereas RIPM did not induce convulsion up to 200 nmol/brain. These β-lactams inhibited GABA receptor binding in a concentration-dependent manner. The order of inhibitory activity was IPM>CEZ>CER≥RIPM. These in vivo and in vitro results suggest that RIPM might have weaker convulsant activity than IPM, CEZ and CER.

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