[Mechanism of blocking K+-channels with tetraethylammonium].
Using the patch-voltage-clamp method action of tetraethylammonium on the fast (30 pS) and slow K+ channels was investigated. The slow K+ channels were presented by two types: with whole (30 pS) and decreased (20 pS) conductance. In all cases tetraethylammonium decreased the current magnitude and modified the channel kinetic parameters. Apparent blocking constants determined from the current decreasing are as 8-50 and 4-12 mM for the slow K+ channels with whole and decreased conductance, respectively, and 0.05-0.08 mM--for the fast K+ channel. The potential dependency of the blocking constants correlates with that of the channel conductance. Probability of the channel open state for the slow K+ channels decreases, and that for the fast K+ channel increases under application of tetraethylammonium. It is concluded that there are two sites of tetraethylammonium binding: the first site is into the channel pore, and the second one--into the regulatory centre responsible for the channel kinetic behaviour. Blocking of general conductance of the slow channels is accompanied by proportional decrease of the channel substate conductances without change of their number and cooperatively. Block of the fast K+ channel occurs without change of the channel elementary conductance but with decrease of the number of the channel substates and reversible violation of the channel transition cooperativity. The data are discussed from the point of the hypothesis on the channel clustery organization.
D000200:Action Potentials / Q000187:drug effects; D000818:Animals; D066298:In Vitro Techniques; D007473:Ion Channels / Q000187:drug effects* / Q000502:physiology; D007700:Kinetics; D008195:Lymnaea; D009474:Neurons / Q000187:drug effects / Q000378:metabolism* / Q000502:physiology; D010539:Permeability; D011188:Potassium / Q000378:metabolism*; D013757:Tetraethylammonium Compounds / Q000494:pharmacology*
D007473:Ion Channels; D013757:Tetraethylammonium Compounds; D011188:Potassium
Mekhanizm blokirovaniia K+-kanalov tetraétilammoniem.