Abstract
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.
Footnotes
- Received April 13, 1950.
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