Abstract
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.
Footnotes
- Received November 8, 1951.
JPET articles become freely available 12 months after publication, and remain freely available for 5 years.Non-open access articles that fall outside this five year window are available only to institutional subscribers and current ASPET members, or through the article purchase feature at the bottom of the page.
|
