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Journal of Pharmacology And Experimental Therapeutics, Vol. 87, Issue 2, 73-80, 1946
Copyright © 1946 by American Society for Pharmacology and Experimental Therapeutics

PHARMACOLOGY OF LOBELAN AND RELATED COMPOUNDS

R. H. K. FOSTER 1, LUCILLE J. MOENCH 1, and H. C. CLARK 1

1 From the Department of Pharmacology, Hoffmann-La Roche, Inc., Nutley, N. J.

1. Piperidine compounds of the lobelan type have been studied for spasmolytic action, respiratory and analeptic action, blood pressure, and toxicity and were shown to possess both peripheral spasmolytic action and central stimulating action. The spasmolytic tests were conducted on isolated tissues.

2. The neurotropic action as studied on acetylcholine-stimulated guinea pig intestine was greater than that of papaverine for most of the compounds. The most efficient compound, 1-methyl-2,6-di-(p-methoxyphenethyl)-piperidine (compound Ih), was 10 to 14 times as effective as papaverine.

3. The myotropic action as studied on barium-stimulated guinea pig intestine was about the same order as that of papaverine. However, against histamine contractions, compound Ih was 7 to 10 times more powerful than papaverine.

4. Analeptic action was noted for the compounds. As a respiratory stimulant in morphinized rabbits, compound Ih was much more effective than as an antagonist against allylisopropyl barbituric acid.

5. The circulatory effects were relatively slight.

Submitted on August 30, 1945






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Copyright © 1946 by the American Society for Pharmacology and Experimental Therapeutics.