Enzymic synthesis of two glucuronides of the hydroxyisoxazole GABA-agonist, THIP, and thein vivoglucuronidation of THIP in rat

Abstract
1. A method for preparative enzymic synthesis of two glucuronides of THIP (3-hydroxy-4,5,6,7-tetrahydro-isoxazolo[5,4-c]pyridine) is described. 2. Using FAB mass spectrometry, u.v. and 1H- and 13C-n.m.r. spectroscopy, the two glucuronides were identified as N- and 13O-glucuronides respectively. 3. An h.p.l.c method for determination of THIP and the two intact glucuronides in urine has been developed. 4. The glucuronidation pattern of THIP in rats has been examined; THIP was excreted as a THIP-O-glucuronide but not as a THIP-N-glucuronide.