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Journal of Pharmacology And Experimental Therapeutics, Vol. 104, Issue 3, 284-290, 1952
Copyright © 1952 by American Society for Pharmacology and Experimental Therapeutics

SPASMOLYTIC ACTION OF BICYCLIC BASIC ALCOHOL ESTERS

Lowell O. Randall 1, Wilbur M. Benson 1, and Paul L. Stefko 1

1 Pharmacology Department, Hoffmann-La Roche Inc., Nutley 10, New Jersey

A series of eighteen esters of bicyclic amino alcohols have been assayed for spasmolytic activity. The quinuclidinol esters and azabicyclo-octanol esters have anticholinergic activity of the order of atrophic while the azabicyclononanol esters are considerably weaker.

The quaternary salt, Ro 2-3773 (1-methyl-3-benziloyloxy-quinuclidinium bromide), has an anticholinergic activity similar to atropine. Ro 2-3773 is equal to atropine in antiacetylcholine activity on isolated intestine and in antiacetylcholine and antivagal activity as measured on arterial pressure; it is slightly stronger in antisalivary and antilacrimating properties; and it is less active in protecting against methacholine-induced bronchospasm. Ganglionic blocking action is about equal to that of TEA and occurs at doses thirty times higher than the vagal blocking dose.

Submitted on November 8, 1951






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Copyright © 1952 by the American Society for Pharmacology and Experimental Therapeutics.