Antitussive Activity of a Series of Dialkylaminodiphenylbutanol Esters

The effect of structural modifications upon the antitussive activity of a series of dialkylaminodiphenylbutanol esters was examined. In an attempt to investigate a possible correlation of pharmacological activities, the compounds were also evaluated for their spasmogenic effect upon the intestine an...

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Bibliographic Details
Published in:Journal of pharmaceutical sciences 1963-05, Vol.52 (5), p.446-451
Main Authors: Miller, Joseph A., Robbins, E.Brown, Meyers, Donald B.
Format: Article
Language:English
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Summary:The effect of structural modifications upon the antitussive activity of a series of dialkylaminodiphenylbutanol esters was examined. In an attempt to investigate a possible correlation of pharmacological activities, the compounds were also evaluated for their spasmogenic effect upon the intestine and their analgesic activity. Antitussive activity was determined in guinea pigs by means of SO2-induced cough. Spasmogenic activity was determined by inserting a balloon into the duodenum of anesthetized dogs. Analgesic activity was determined by the rat-tail heat method. The optimum antitussive structure tested within this series was α-dl-2-propionoxy-l,2-diphenyl-3-methyl-4-dimethylaminobutane hydrochloride. The optimum analgesic structure tested in this series was the 2-acetoxy analog of the same compound. Some degree of correlation was shown among the activities, although exceptions were noted.
ISSN:0022-3549
1520-6017
DOI:10.1002/jps.2600520509