Studies on curare-like action of the tripeptide carbobenzoxy-Gly-Gly-Arg-beta-naphthylamide in mouse diaphragm

European Journal of Pharmacology
S Y Lin-Shiau, M J Lin

Abstract

The effects of several protease substrates or protease inhibitors on neuromuscular transmission in the isolated mouse phrenic nerve-diaphragm were studied. N-Carbobenzoxy-Gly-Gly-Arg-beta-naphthylamide (Z-GGR-N) but none of the other agents inhibited the nerve-evoked muscle contractions. By means of electrophysiological studies, Z-GGR-N was found to inhibit the amplitudes of both end-plate potentials (epps) (IC50 approximately 50 microM) and miniature end-plate potentials (mepps) but to increase the frequencies of mepps. This tripeptide could protect the nicotinic acetylcholine receptor from the irreversible inhibitory action of alpha-bungarotoxin on the mouse diaphragm. Similar to D-tubocurarine, Z-GGR-N induced tetanic fading both of nerve-evoked muscle contractions and of the amplitude of epps. Furthermore, Z-GGR-N exhibited a greater depression of the amplitudes of train-epps than those of mepps, similar to that of hexamethonium and D-tubocurarine, indicating an effect on presynaptic autoreceptors. Suramin, which could competitively reverse the inhibitory effects of non-depolarizing relaxants, acted in this study as an antagonist of all the effects of Z-GGR-N, especially those at the presynaptic site. All of these findings ...Continue Reading

References

May 27, 1992·European Journal of Pharmacology·R H HenningA Den Hertog
May 1, 1992·British Journal of Pharmacology·S Y Lin-ShiauW M Fu
Apr 1, 1989·Trends in Pharmacological Sciences·W C Bowman
Apr 1, 1969·Biochemical Pharmacology·R J KitzS Ginsburg
Nov 1, 1980·The Journal of Pharmacy and Pharmacology·D A Kharkevich, A P Skoldinov
Jul 1, 1983·Proceedings of the National Academy of Sciences of the United States of America·D A BaxterW J Strittmatter

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Citations

Oct 21, 1999·European Journal of Pharmacology·S Y Lin-Shiau, M J Lin
Jan 4, 2001·Neurochemistry International·C F Chan, S Y Lin-Shiau

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