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

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Author(s)

Abstract

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.

Journal

  • Journal of Pharmacological Sciences

    Journal of Pharmacological Sciences 120(1), 54-58, 2012-09-20

    The Japanese Pharmacological Society

References:  15

Codes

  • NII Article ID (NAID)
    10031071961
  • NII NACSIS-CAT ID (NCID)
    AA11806667
  • Text Lang
    ENG
  • Article Type
    SHO
  • ISSN
    13478613
  • NDL Article ID
    023957424
  • NDL Call No.
    Z53-D199
  • Data Source
    CJP  NDL  J-STAGE 
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