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

Add time:09/01/2019    Source:sciencedirect.com

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-β-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∼50 μM) 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 α-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 suggest that Z-GGR-N is a novel tripeptide possessing curare-like actions at both presynaptic and postsynaptic sites and that these actions are independent of its protease substrate property.

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