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Tissue distribution and metabolism of O ‐(4‐methoxyphenylcarbamoyl)‐3‐diethylaminopropiophenone oxime hydrochloride (USVP‐E142) in the rat
Author(s) -
Gollamudi Ramachander,
Glassman Jerome M.
Publication year - 1982
Publication title -
journal of applied toxicology
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.784
H-Index - 87
eISSN - 1099-1263
pISSN - 0260-437X
DOI - 10.1002/jat.2550020106
Subject(s) - hydrochloride , chemistry , oxime , in vivo , metabolism , urea , oral administration , hydrolysis , pharmacology , endocrinology , biochemistry , biology , microbiology and biotechnology
The disposition of 0‐(4‐methoxyphenylcarbamoyl)‐3‐diethylaminopropiophenone oxime‐(carbonyl)‐ 14 C hydrochloride in the rat was studied in vivo and in vitro. Upon oral administration, radioactivity was detected within 15 min in many tissues, including the brain. The lung and the liver had the highest levels. The first‐order rate constant for the disappearance of 14 C from the stomach was 8.2 × 10 −3 min −1 for fasted and 5.7 × 10 −3 min −1 for non‐fasted rats. Most of the radioactivity was eliminated in the form of 14 CO 2 . The major metabolic pathway appears to be the hydrolysis of the carbamoyl bond followed by decarboxylation of the resultant carbamic acid, leading to the liberation of CO 2 . Bis( p ‐methoxyphenyl)urea and 3‐diethylamino‐4′‐hydroxypropiophenone were identified as urinary metabolites.