Ephedrine blocks wild-type and long-lived mutant acetylcholine receptor channels.
A combination of transient expression of wild-type and a mutant muscle nicotinic receptor (AChR) found in a patient suffering from a congenital myasthenic syndrome and single-channel recordings was used to characterize the action of ephedrine on the AChR. In the presence of ephedrine, both types of AChR channel showed a flickering behaviour and a dose-dependent reduction in the mean open time. The duration of the blocking events was dependent on the membrane potential. The forward rate constant for the blocking process was of the order of 10(7) M-1 s-1 in both types of AChR. The results are consistent with ephedrine acting as a channel blocker in wild-type AChR as well as in long-lived AChR channels present in patients with the slow-channel syndrome.
Bouzat
C
C
Instituto de Investigaciones Bioquímicas de Bahía Blanca, Argentina.
D000818:Animals; D018680:Cholinergic Antagonists / Q000494:pharmacology*; D018076:DNA, Complementary; D004809:Ephedrine / Q000494:pharmacology*; D006801:Humans; D007473:Ion Channels / Q000378:metabolism / Q000502:physiology; D015624:Lambert-Eaton Myasthenic Syndrome; D008564:Membrane Potentials / Q000187:drug effects / Q000502:physiology; D051379:Mice; D009154:Mutation / Q000502:physiology*; D018408:Patch-Clamp Techniques; D011950:Receptors, Cholinergic / Q000235:genetics*
D018680:Cholinergic Antagonists; D018076:DNA, Complementary; D007473:Ion Channels; D011950:Receptors, Cholinergic; D004809:Ephedrine