Biosynthesis of imipramine glucuronide and characterization of imipramine glucuronidation catalyzed by recombinant UGT1A41
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چکیده
منابع مشابه
Imipramine N-glucuronidation in human liver microsomes: biphasic kinetics and characterization of UDP-glucuronosyltransferase isoforms.
A method for the direct determination of imipramine N-glucuronidation in human liver microsomes by high-performance liquid chromatography with UV detection was developed. Imipramine was incubated with human liver microsomes and UDP-glucuronic acid. The Eadie-Hofstee plots of imipramine N-glucuronidation in human liver microsomes were biphasic. For the high-affinity component, the K(m) was 97.2 ...
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Imipramine, a potent antidepressive drug has been shown to antagonize the actions of a number of autopharmacological substances like histamine, 5-hydroxytryptamine, bradykinin, catecholamines and acetylcholine (1). Sigg and his coworkers (2, 3) observed a dual effect of imipramine on the various manifestations of the autonomic nervous system; a blocking action at higher dosage and a stimulant e...
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The role of human UDP glucuronosyltransferase (UGT) 2B10 in the N-glucuronidation of a number of tricyclic antidepressants was investigated and compared with that of UGT1A4 in both the Sf9 expressed system and human liver microsomes. The apparent K(m) (S(50)) values for the formation of quaternary N-glucuronides of amitriptyline, imipramine, clomipramine, and trimipramine were 2.60, 16.8, 14.4,...
متن کاملTrans-3'-hydroxycotinine O- and N-glucuronidations in human liver microsomes.
Trans-3'-hydroxycotinine is a major metabolite of nicotine in humans and is mainly excreted as O-glucuronide in smoker's urine. Incubation of human liver microsomes with UDP-glucuronic acid produces not only trans-3'-hydroxycotinine O-glucuronide but also N-glucuronide. The formation of N-glucuronide exceeds the formation of O-glucuronide in most human liver microsomes, although N-glucuronide h...
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ژورنال
عنوان ژورنال: Acta Pharmacologica Sinica
سال: 2006
ISSN: 1671-4083,1745-7254
DOI: 10.1111/j.1745-7254.2006.00314.x