Pharmacology studies on bis-(1-carbo-beta-diethylaminoethoxy)-1-phenylcyclopentane)-ethane disulfonate.

Abstract

1. 6-Dimethylamino-4,4-diphenyl-3-heptanone hydrochloride, codeine and bis-(1-(carbo-β-diethylaminoethoxy)-1-phenyl-cyclopentane)-ethane disulfonate (SKF No. 769-J 2 ) were found to exhibit antitussive activity when tested by a modification of the Domenjoz method. 3,3-Diethyl-2,4-dioxopiperidine was ineffective in doses up to 100 mgm./kgm. 2. In effective antitussive doses, SKF No. 769-J 2 produced either an increase or slight decrease in respiratory volume in dogs, whereas codeine caused a marked decrease. 3. SKF No. 769-J 2 had 1/2 to 1/10 the antispasmodic activity of atropine on the isolated rabbit intestine, and 1/2 the local anesthetic activity of cocaine on the rabbit cornea. 4. In subacute and chronic toxicity studies, no evidence of changes due to administration of SKF No. 769-J 2 was observed by histological examination of tissues removed from rats and dogs which received massive daily doses of this compound for periods of 1 to 3 months. 5. The data obtained in the present experiments indicate that SKF No. 769-J 2 should be evaluated clinically as an antitussive agent.