[Inactivated sodium channels are blocked by the anti-arrhythmic cordaron].
The blocking action of the antiarrhythmic cordaron (amiodaron hydrochloride) on Na currents in the frog node of Ranvier was studied by the voltage-clamp technique. It was established that the degree of the cordaron-induced block can be reversibly increased by long-term (1 s and more) membrane depolarization. The time constants of both the development and recovery from the block caused by membrane depolarization are of the order of hundreds of seconds ("induced slow sodium inactivation"). The fraction of blocked channels rises to some limiting level with an increase in the magnitude of the depolarizing step, the region of strong voltage dependency being between -130 and -70 mv. The inhibition of outward potassium current by 7.10(-4) M cordaron does not exceed 15%. The time- and voltage-dependent block of Na channels is supposed to result from interaction of the antiarrhythmic with inactivated channels.
D000638:Amiodarone / Q000494:pharmacology*; D000818:Animals; D001001:Anura; D001572:Benzofurans / Q000494:pharmacology*; D007473:Ion Channels / Q000187:drug effects*; D008564:Membrane Potentials / Q000187:drug effects; D011188:Potassium / Q000378:metabolism; D011901:Ranvier's Nodes / Q000187:drug effects*; D012964:Sodium / Q000378:metabolism*
D001572:Benzofurans; D007473:Ion Channels; D012964:Sodium; D000638:Amiodarone; D011188:Potassium
Antiaritmik kordaron blokiruet inaktivirovannye natrievye kanaly.