Inhibition by Pregnenolone Sulphate, a Metabolite of the Neurosteroid Pregnenolone, of Voltage-Gated Sodium Channels Expressed in Xenopus Oocytes

Takafumi Horishita; Susumu Ueno; Nobuyuki Yanagihara; Yuka Sudo; Yasuhito Uezono; Dan Okura; Takeyoshi Sata

doi:10.1254/jphs.12106SC

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Inhibition by Pregnenolone Sulphate, a Metabolite of the Neurosteroid Pregnenolone, of Voltage-Gated Sodium Channels Expressed in Xenopus Oocytes

Takafumi Horishita, Susumu Ueno, Nobuyuki Yanagihara, Yuka Sudo, Yasuhito Uezono, Dan Okura, Takeyoshi Sata

著者情報

キーワード: pregnenolone sulphate, voltage-gated sodium channel, neuroprotection

ジャーナルフリー早期公開

論文ID: 12106SC

DOI https://doi.org/10.1254/jphs.12106SC

この記事には本公開記事があります。

The final version of this article is now available: Vol. 120 (2012), No. 1 pp. 54-58

詳細

抄録

Neurosteroids are known as allosteric modulators of the ligand-gated ion channel superfamily. Voltage-gated sodium channels (Na_v) play an important role in mediating excitotoxic damages. Here we report the effects of neurosteroids on the function of Na_v, using voltage-clamp techniques in Xenopus oocytes expressed with the Na_v1.2 α subunit. Pregnenolone sulphate, but not pregnenolone, inhibited sodium currents (I_Na) at 3 – 100 μmol/L. The suppression of I_Na 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_v via increased inactivation, which may contribute to the neuroprotection.

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