Effect of tetraalkylammonium derivative of 6-methyluracil on amplitude and temporal parameters of miniature endplate potentials in frog neuromuscular junction |
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| Authors: | Gorshkova O V Zobov V V Bukharaeva E A Nikol'skii E E Akamsin V D Galyametdinova I V Reznik V S |
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| Affiliation: | (1) Institute of Biochemistry and Biophysics, Russian Academy of Sciences, Russia;(2) A. E. Arbuzov Institute of Organic and Physical Chemistry, Kazan' |
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| Abstract: | The effect of C-547, a tetraalkylammonium derivative of 6-methyluracil, a novel highly selective acetylcholinesterase inhibitor, on frog neuromuscular junction was studied. In concentrations 10-9-10-7 M the preparation increased the amplitude and temporal parameters of miniature endplate potentials. In contrast to the effect of C-574 on purified acetylcholinesterase from mammals, the effect of this agent on frog neuromuscular junction was reversible. In a concentration of 10-6 M the preparation apart from anticholinesterase activity produced a parasympatholytic effect manifested in a decrease in amplitude and decay time constant of miniature endplate potentials accompanied by a decrease in spontaneous transmitter secretion. After washout, the parasympatholytic effect recovered more slowly, but disappeared more rapidly compared to anticholinesterase activity. These findings suggest that parasympatholytic effect of C-547 results from direct action on receptor-channel complexes in the endplate membrane. |
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| Keywords: | neuromuscular junction acetylcholinesterase inhibitors parasympatholytic activity pyrimidines |
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