RT Journal Article
SR Electronic
T1 PHARMACOLOGIC ACTION OF BASIC ESTERS OF p-XENYLACETIC AND p-XENYLGLYCOLIC ACID—NEW ANTISPASMODIC DRUGS
JF Journal of Pharmacology and Experimental Therapeutics
JO J Pharmacol Exp Ther
FD American Society for Pharmacology and Experimental Therapeutics
SP 19
OP 26
VO 100
IS 1
A1 Lands, A. M.
A1 Hoppe, James O.
A1 Lewis, John R.
A1 Ananenko, Estelle
YR 1950
UL http://jpet.aspetjournals.org/content/100/1/19.abstract
AB 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 β-diethylaminoethyl diphenylacetate. 2. The methyl-, ethyl- and propyl-p-xenylacetate esters of β-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.