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At least 145 records · Page 8Linked to original sources
PubMed1991

Activation of ion channels in the frog endplate by several analogues of acetylcholine.

1. Single-ion-channel recording has been used to estimate the equilibrium concentration-response relationship for several acetylcholine analogues. The response, corrected for desensitization, was taken as the probability of a channel being open during clusters of openings that were separated by desensitized periods. 2. All agonists were able to block the channels which they themselves opened. Carbachol, suberyldicholine and the sulphonium analogue of acetylcholine were all found to be efficacious agonists in the sense that the results indicate that all of them, in sufficiently high concentration, would be able to open 90% or more of channels if it were not for channel block. 3. In the case of suberyldicholine the results are much as predicted by the interpretation of the fine structure of channel openings at low agonist concentrations. 4. The maximum probability of opening that could be obtained with decamethonium and with phenyltrimethylammonium was low (below 4%), and it was not possible to distinguish whether this was wholly a result of the powerful (relative to activation potency) channel-blocking action of these agonists, or whether it was to some extent attributable to their being genuine partial agonists. 5. The results suggest that, for a range of agonists, differences in equilibrium potency are usually more strongly influenced by affinity for binding to the resting state of the receptor than by ability to activate the receptor once bound, though in the case of suxamethonium (relative to acetylcholine) the contributions of each factor are similar.

Acetylcholine↗
PubMed1995

Determinants of antiarrhythmic drug action. Electrostatic and hydrophobic components of block of the human cardiac hKv1.5 channel.

The molecular basis of antiarrhythmic drug action is still poorly understood. We recently reported that block of the human cardiac hKv1.5 channel by quinidine displayed similarity with internal quaternary ammonium block of squid and Shaker potassium channels. To gain further insight into the molecular determinants of the affinity and the stereoselectivity of antiarrhythmic drug action, we studied the effects of quinine (a diastereomer of quinidine), clofilium (a quaternary ammonium class III agent), and tetrapentylammonium (TPeA, a biophysical reference probe for the internal quaternary ammonium binding site). For all compounds, block was voltage dependent, with a steep increase over the voltage range of channel opening and a superimposed weaker voltage dependence at more positive potentials. The latter electrostatic component was similar for all drugs, consistent with a binding reaction sensing approximately 20% of the transmembrane electrical field. Clofilium and TPeA displayed a higher apparent affinity (0.15 and 0.28 mumol/L, respectively), and quinine displayed a lower one (21 mumol/L) compared with quinidine (6.2 mumol/L). Block development upon depolarization was time dependent for clofilium and TPeA but slow compared with quinidine. A time-dependent component was difficult to resolve for quinine, but the time course of deactivating tail currents was slower than in the control condition. The resulting crossover phenomenon was also observed for the quaternary drugs. Compared with TPeA alone, the combined application of quinine and TPeA resulted in a reduced current that decayed slower, consistent with competition.(ABSTRACT TRUNCATED AT 250 WORDS)

Anti-Arrhythmia Agents↗