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Planta Med 1996; 62(6): 580-581
DOI: 10.1055/s-2006-957981
Letters

© Georg Thieme Verlag Stuttgart · New York

Kavain Inhibits Non-Stereospecifically Veratridine-Activated Na+ Channels

Johannes Gleitz, Norbert Gottner, Angela Ameri, Thies Peters (†)
  • University Clinics Ulm, Institute of Naturheilkunde, Helmholtzstr. 20, D-89081 Ulm, Germany
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Publication History

1996

1996

Publication Date:
04 January 2007 (online)

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Abstract

The action of the natural kava pyrone, (+)-kavain, and its synthetic racemate, (±)-kavain, on voltage-dependent Na+ channels was investigated, while considering their stereospecific properties, on veratridine-induced increases in cytosolic free Na+ and Ca2+ ([Na+]i, [Ca2+]i) and the release of endogenous glutamate from cerebrocortical synaptosomes. Both compounds dose-dependently suppressed the veratridine-induced increase in [Na+]i, [Ca2+]i and glutamate release with IC50 values (± S.D.) of 71 ± 22, 72 ± 7, 120 ± 37 µmol/l (+)-kavain and 77 ± 21, 90 ± 14, 92 ± 23 µmol/l (±)-kavain, respectively. As judged from the dose-dependency, IC50 values, velocity and time course of action, both kava pyrones were equally effective suggesting a non-stereospecific inhibition of veratridine-activated Na+ channels.

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