The in vitro metabolism of 3-(1-hydroxy-2-piperidinoethyl)-5-phenylisoxazole citrate (31252-S) with rabbit liver homogenate.
- 1 January 1976
- journal article
- research article
- Published by Pharmaceutical Society of Japan in CHEMICAL & PHARMACEUTICAL BULLETIN
- Vol. 24 (8) , 1757-1764
- https://doi.org/10.1248/cpb.24.1757
Abstract
The in vitro metabolism of generally labeled 3H-3-(1-hydroxy-2-piperidinoethyl)-5-phenylisoxazole (3H-31252-S) using the 9000 .times. g supernatant fraction of rabbit liver homogenate was studied. The metabolites were identified and determined quantitatively by reverse isotope dilution analysis. The drug is extensively metabolized, the main metabolic pathways being N-oxidation of piperidine and p-hydroxylation of the phenyl ring. 3-{1-Hydroxy-2-(4-hydroxypiperidino) ethyl}-5-phenylisoxazole showed slightly stronger analgesic activity than the parent compound 31252-S. All metabolites were less toxic than the parent 31252-S.This publication has 0 references indexed in Scilit: