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EFFECTS OF SOME GUANIDINE DERIVATIVES ON NEUROMUSCULAR AND GANGLIONIC TRANSMISSION
Author(s) -
BARZAGHI F.,
MANTEGAZZA P.,
RIVA M.
Publication year - 1962
Publication title -
british journal of pharmacology and chemotherapy
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 2.432
H-Index - 211
eISSN - 1476-5381
pISSN - 0366-0826
DOI - 10.1111/j.1476-5381.1962.tb01446.x
Subject(s) - neuromuscular transmission , guanidine , chemistry , neuromuscular junction , pharmacology , acetylcholine , neuroscience , biophysics , medicine , anesthesia , biochemistry , biology
The anticurare activity of some guanidine derivatives has been studied using the fowl sciatic nerve‐gastrocnemius muscle preparation and the cat sciatic nerve‐gastrocnemius and tibialis anterior muscle preparations. Among the compounds tested, and in decreasing order of potency, were NN ‐dimethylguanidine, N ‐methylguanidine, guanidine and N ‐aminoguanidine which antagonized or prevented tubocurarine or gallamine triethiodide‐induced paralysis. None of the derivatives antagonized the effects of suxamethonium or decamethonium. NN ‐Dimethylguanidine, N ‐methylguanidine and guanidine antagonized or prevented the curare‐like effects of magnesium without altering the activity of hemicholinium. At high doses NN ‐dimethylguanidine induced a decamethonium‐like spastic paralysis in the fowl sciatic nerve‐gastrocnemius muscle preparation. NN ‐Diethylguanidine, however, induced a tubocurarine‐like flaccid paralysis. The derivatives possessing anticurare activity were also studied using the cat superior cervical ganglion‐nictitating membrane preparation to check their possible effects against ganglionic blocking agents. Only guanidine antagonized or prevented the effects of hexamethonium, pentolinium and mecamylamine; it had no effect on the actions of pempidine and chlorisondamine. NN ‐Diethylguanidine was the only compound in the series to show a ganglionic blocking action.