A theoretical experimental method to determine the locus of desensitization.
Consider a ligand-gated channel with n agonist binding sites which can undergo desensitization. We present a theoretical experimental procedure for pinpointing the principal receptor state from which there is a transition to the desensitized state. The method is based on the observation that the dependence of the slope of the time constant of desensitization vs agonist concentration, at low concentrations, represents the state from which desensitization occurs. In those receptors where desensitization occurs from the open state (or the one immediately preceding it), the method also enables us to determine the number of binding sites.
Buchman
E
E
Department of Neurobiology and Otto Loewi Minerva Center for Cellular and Molecular Neurobiology, The Hebrew University of Jerusalem, Jerusalem 91904, Israel.
Parnas
H
H
D001665:Binding Sites; D003198:Computer Simulation; D015640:Ion Channel Gating; D007473:Ion Channels / Q000819:agonists / Q000378:metabolism; D007700:Kinetics; D008024:Ligands; D008954:Models, Biological
D007473:Ion Channels; D008024:Ligands