Vincamine and vincanol (cas 19877-89-5) are potent blockers of voltage-gated Na + channels

Add time:09/25/2019    Source:infona.pl

The effects of three vinca derivatives on [ 3 H]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 (cas 19877-89-5) reduced [ 3 H]batrachotoxin binding with IC 5 0 values of 0.34, 1.9 and 10.7 μM, blocked Na + currents with IC 5 0 values of 44, 72 and 40 μM, and protected cortical cultures against veratridine-induced cell death with IC 5 0 values of 0.49, 26 and 33 μM, respectively. Upon i.p. administration, vinpocetine, vincamine and vincanol attenuated maximal electric shock-induced convulsions in a dose-dependent manner with ED 5 0 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.

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