Premium
Effects of pentobarbitone on acetylcholine‐activated channels in mammalian muscle
Author(s) -
Gage Peter W.,
McKin David
Publication year - 1985
Publication title -
british journal of pharmacology
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 2.432
H-Index - 211
eISSN - 1476-5381
pISSN - 0007-1188
DOI - 10.1111/j.1476-5381.1985.tb08851.x
Subject(s) - acetylcholine , pentobarbital , chemistry , neuroscience , neuromuscular junction , pharmacology , medicine , biology
1 Acetylcholine‐activated single channel currents were recorded from the extrajunctional region of chronically denervated skeletal muscle of the rat by the patch clamp technique. 2 In control experiments, the cumulative open‐time, closed‐time and burst length distributions could be well described by the sum of two exponentials. 3 Pentobarbitone decreased the mean open time and increased the time constant of the fast component of the closed time distribution. These effects increased with drug concentration. 4 The mean burst length was relatively independent of pentobarbitone concentration over the range of concentrations used (10–500 μM). 5 These observations are inconsistent with a simple sequential blocking model and it is suggested that pentobarbitone has an allosteric site of action on receptor‐channel complexes that makes the open state less stable.