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Vincamine and vincanol are potent blockers of voltage-gated Na+ channels.

Abstract：

:The effects of three vinca derivatives on [3H]batrachotoxin binding in rat cortical synaptosomes, on the inhibition of whole-cell Na+ currents evoked in voltage-clamped cortical neurones of the rat, on the protection against veratridine-induced cell death in cortical cultures and on the maximal electroshock-induced seizures in mice were compared. Vinpocetine, vincamine and vincanol reduced [3H]batrachotoxin binding with IC50 values of 0.34, 1.9 and 10.7 microM, blocked Na+ currents with IC50 values of 44.72 and 40 microM, and protected cortical against veratridine-induced cell death with IC50 values of 0.49, 26 and 33 microM, respectively. Upon i.p. administration, vinpocetine, vincamine and vincanol attenuated maximal electric shock-induced convulsions in a dose-dependent manner with ED50 values of 27, 15.4 and 14.6 mg/kg, respectively. The present findings indicate that the three vinca derivatives are potent blockers of voltage-gated Na+ channels, a mechanism that may contribute at least in part to the pharmacological/therapeutic benefit of these drugs.

journal_name

Eur J Pharmacol

journal_title

European journal of pharmacology

authors

Erdo SA,Molnár P,Lakics V,Bence JZ,Tömösközi Z

doi

10.1016/s0014-2999(96)00542-0

subject

Has Abstract

pub_date

1996-10-24 00:00:00

pages

69-73

issue

1-2

eissn

0014-2999

issn

1879-0712

pii

S0014-2999(96)00542-0

journal_volume

314

pub_type

杂志文章

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