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Vincamine and vincanol are potent blockers of voltage-gated Na+ channels
- Source :
- European Journal of Pharmacology. 314:69-73
- Publication Year :
- 1996
- Publisher :
- Elsevier BV, 1996.
-
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.
- Subjects :
- Male
Patch-Clamp Techniques
Vinca
Vincamine
Pharmacology
Sodium Channels
Rats, Sprague-Dawley
Mice
chemistry.chemical_compound
Vinpocetine
medicine
Animals
Patch clamp
Vinca Alkaloids
Antihypertensive Agents
Cells, Cultured
Veratridine
Cell Death
Voltage-gated ion channel
biology
Alkaloid
Brain
biology.organism_classification
Rats
Mechanism of action
chemistry
Batrachotoxin
medicine.symptom
Ion Channel Gating
medicine.drug
Subjects
Details
- ISSN :
- 00142999
- Volume :
- 314
- Database :
- OpenAIRE
- Journal :
- European Journal of Pharmacology
- Accession number :
- edsair.doi.dedup.....d6c82c999f89be0a9e8cd7a483b00fa5