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Journal of Pharmacology And Experimental Therapeutics, Vol. 100, Issue 1, 19-26, 1950
Copyright © 1950 by American Society for Pharmacology and Experimental Therapeutics

PHARMACOLOGIC ACTION OF BASIC ESTERS OF p-XENYLACETIC AND p-XENYLGLYCOLIC ACID—NEW ANTISPASMODIC DRUGS

A. M. Lands 1, James O. Hoppe 1, John R. Lewis 1, and Estelle Ananenko 1

1 Pharmacology Section, Sterling-Winthrop Research Institute, Rensselaer, New York

1. The spasmolytic potency of various p-xenylacetic and p-xenylglycolic acid esters of basic amino alcohols has been determined on isolated segments of rabbit ileum. In general, they are less effective than beta-diethylaminoethyl diphenylacetate.

2. The methyl-, ethyl- and propyl-p-xenylacetate esters of beta-piperidinoethanol are effective intestinal spasmolytic agents when administered intravenously to rabbits and dogs. The pharmacologic actions of the methyl analog (WIN 5786) are described in some detail.

3. Scopolamine-like effects on the central nervous system were not observed in cats after intraperitoneal injections of WIN 5786 in doses as large as 40 mgm./ kgm.

4. The analgesic action of WIN 5786 in rats is comparable to that of aminopyrine.

5. Hypnotic action (Evipal potentiation technique) of WIN 5786 is about one-fifth that of diphenhydramine.

6. Acute and subacute toxicity experiments indicate that WIN 5786 has a low toxicity.

7. The results reported in this communication suggest that WIN 5786 may be an effective antispasmodic drug for the treatment of smooth muscle spasm.

Submitted on April 13, 1950






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