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Journal of Pharmacology And Experimental Therapeutics, Vol. 97, Issue 1, 48-57, 1949
Copyright © 1949 by American Society for Pharmacology and Experimental Therapeutics

THE GANGLIONIC BLOCKING ACTION OF THIOPHANIUM DERIVATIVES

Lowell O. Randall 1, William G. Peterson 1, and G. Lehmann 1

1 Pharmacology Department, Hoffmann-La Roche Inc., Nutley 10, N. J.

Nu-2222 is a thiophanium derivative which has the characteristic ganglionic blocking and hypotensive effects of tetraethylammonium bromide. It has about 30 times the potency and twice the duration of TEA in the dog, cat and monkey. It blocks transmission through the superior cervical ganglion, vagus action on the heart and the carotid sinus pressor reflex. The hypotensive effects are counteracted by ephedrine and large doses of neostigmine. It has no curariform action. It has only a slight effect on intestinal tone but inhibits gastric motility in large doses. It is two to four times as toxic as TEA intravenously in mice, rats and rabbits but 75 times as toxic in dogs. The lethal and hemorrhagic effects in dogs can be modified to a large extent by antihistamine and antiheparin agents.

Submitted on May 26, 1949




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Copyright © 1949 by the American Society for Pharmacology and Experimental Therapeutics.