Inhibition by Pregnenolone Sulphate, a Metabolite of the Neurosteroid Pregnenolone, of Voltage-Gated Sodium Channels Expressed in <I>Xenopus</I> Oocytes
スポンサーリンク
概要
- 論文の詳細を見る
Neurosteroids are known as allosteric modulators of the ligand-gated ion channel superfamily. Voltage-gated sodium channels (Na<SUB>v</SUB>) play an important role in mediating excitotoxic damages. Here we report the effects of neurosteroids on the function of Na<SUB>v</SUB>, using voltage-clamp techniques in <I>Xenopus</I> oocytes expressed with the Na<SUB>v</SUB>1.2 <I>α</I> subunit. Pregnenolone sulphate, but not pregnenolone, inhibited sodium currents (I<SUB>Na</SUB>) at 3 – 100 <I>μ</I>mol/L. The suppression of I<SUB>Na</SUB> by pregnenolone sulphate was due to increased inactivation with little change in activation. These findings suggest that pregnenolone sulphate, a metabolite of pregnenolone, suppresses the function of Na<SUB>v</SUB> via increased inactivation, which may contribute to the neuroprotection.
著者
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Yanagihara Nobuyuki
Department Of Phamacology University Of Occupational And Environmental Health
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Sudo Yuka
Cancer Pathophysiology Div. National Cancer Center Res. Inst. Jpn
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Ueno Susumu
Department Of Phamacology University Of Occupational And Environmental Health
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Sata Takeyoshi
Department Of Anesthesiology School Of Medicine University Of Occupational And Environmental Health
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Uezono Yasuhito
Cancer Pathophysiology Division National Cancer Center Research Institute
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Horishita Takafumi
Department Of Anesthesiology University Of Occupational And Environmental Health
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Okura Dan
Department of Anesthesiology, School of Medicine, University of Occupational and Environmental Health, Japan
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OKURA Dan
Department of Anesthesiology, School of Medicine, University of Occupational and Environmental Health
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Yanagihara Nobuyuki
Department of Pharmacology, School of Medicine, University of Occupational and Environmental Health, Japan
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Uezono Yasuhito
Cancer Pathophysiology Division, National Cancer Center Research Institute, Japan
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Sudo Yuka
Cancer Pathophysiology Division, National Cancer Center Research Institute, Japan
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Sata Takeyoshi
Department of Anesthesiology, School of Medicine, University of Occupational and Environmental Health, Japan
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