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Journal of Pharmacology And Experimental Therapeutics, Vol. 58, Issue 3, 337-360, 1936
Copyright © 1936 by American Society for Pharmacology and Experimental Therapeutics

A COMPARATIVE STUDY OF THE EFFECTS OF FIVE CHOLINE COMPOUNDS USED IN THERAPEUTICS: ACETYLCHOLINE CHLORIDE, ACETYL BETA-METHYLCHOLINE CHLORIDE, CARBAMINOYL CHOLINE, ETHYL ETHER BETA-METHYLCHOLINE CHLORIDE, CARBAMINOYL BETA-METHYLCHOLINE CHLORIDE

H. MOLITOR 1

1 Merck Institute of Therapeutic Research, Rahway, New Jersey

1. The pharmacologic and toxicologic properties of acetylcholine chloride(A), acetyl beta-methylcholine chloride (M), carbaminoyl choline chloride (L), ethyl ether beta-methylcholine chloride (E), and carbaminoyl beta-methylcholine chloride (U) have been compared with the following methods of testing: toxicity in mice and rats after intravenous, subcutaneous and peroral administration; circulatory and intestinal action in rabbits and dogs; miotic action in rabbits and cats; action on isolated intestines and isolated frog heart.

2. A, M and L were found to possess the same pharmacological activity when given intravenously. The potency of E and U was found to be between 100 and 150 times less.

3. In subcutaneous and peroral administration the potency depends largely upon the stability of the choline derivatives in body fluids. Stable compounds like L are, under these circumstances, much more effective than the otherwise equally potent A and M.

4. The procedure followed in testing the miotic action of drugs greatly influences the results. Slight massage of the eyelids may increase the effect up to 100 times.

5. Within the scope of these experiments no selective affinity of the various choline derivatives for certain parts of the parasympathetic nervous system was found.

6. The presence or absence of nicotinic action in a choline derivative does not influence the results under normal experimental conditions, i.e., without previous atropinization.

Submitted on July 29, 1936




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Copyright © 1936 by the American Society for Pharmacology and Experimental Therapeutics.