Evaluation of 5-hydroxytryptophol and other endogenous serotonin (5-hydroxytryptamine) analogs as substrates for udp-glucuronosyltransferase 1a6.
AuthorsKrishnaswamy S, Hao Q, Von Moltke LL, Greenblatt DJ, Court MH,
JournalDrug Metab Dispos
PubMed ID15258112
'Serotonin is a specific in vitro substrate for human UDP-glucuronosyltransferase (UGT) 1A6. In this study, the contribution of UGT1A6 to the glucuronidation of endogenous structural analogs of serotonin, including 5-hydroxytryptophol, N-acetylserotonin, and 6-hydroxymelatonin, was evaluated using available recombinant human UGT isoforms, human liver microsomes, and liver microsomes from animals that ... More
The main role of UGT1A9 in the hepatic metabolism of mycophenolic acid and the effects of naturally occurring variants.
AuthorsBernard O, Guillemette C,
JournalDrug Metab Dispos
PubMed ID15258099
Mycophenolic acid (MPA), a standard immunosuppressive drug, is characterized by unexplained highly variable pharmacokinetics in transplant recipients. The primary metabolic pathway of MPA is glucuronidation; however, literature reports are inconsistent and the contribution of all human UDP-glucuronosyltransferases (UGTs) has never been systematically assessed. Sixteen heterologously expressed UGTs were studied for ... More