title: Estimation of rate constants of drug binding to open channels of cardiac transient outward current.
abstract: An improved approach to the evaluation of the rate constants of drugs binding to the open channel underlying the transient outward potassium current I(t0) is described. It is based on an analysis of a quantitative model formulated by a set of twelve differential equations. The rate constants are calculated from the time constants resulting from an approximation of the time course of apparent inactivation of the recorded I(t0) by two exponentials in the absence and by three exponentials in the presence of a blocking agent. The model study confirmed significantly higher accuracy in comparison with the existing electrophysiological method.
authors.affiliation: Department of Physiology, Masaryk University, Brno, Czech Republic. simurda@med.muni.cz
authors.forename: Jiří
authors.initials: J
authors.lastname: Simurda
authors.forename: Milena
authors.initials: M
authors.lastname: Simurdová
mesh_terms: D001665:Binding Sites; D002462:Cell Membrane / Q000187:drug effects / Q000502:physiology*; D003198:Computer Simulation; D015640:Ion Channel Gating / Q000187:drug effects / Q000502:physiology; D007700:Kinetics; D008564:Membrane Potentials / Q000502:physiology*; D008955:Models, Cardiovascular; D032383:Myocytes, Cardiac / Q000187:drug effects / Q000502:physiology*; D011188:Potassium / Q000378:metabolism*; D026902:Potassium Channel Blockers / Q000494:pharmacology*; D015221:Potassium Channels / Q000187:drug effects / Q000502:physiology*
chemical_list: D026902:Potassium Channel Blockers; D015221:Potassium Channels; D011188:Potassium