Abstract

Rat liver UDP glucuronosyltransferase activities may be divided into at least two groups with differential responses towards substrates. This paper deals with an attempt to describe on what chemical basis the two groups may be distinguished. We studied the glucuronidation of 24 substrates in liver-microsomes of Sprague-Dawley rats pretreated with 3-methylcholanthrene or phenobarbital. The conjugation of 11 substrates was stimulated most strongly by 3-methylcholanthrene and that of the others, by phenobarbital. The estimated thickness of the molecules in their most likely conformation was below 4 Å for molecules of the first group and more than 4 Å for the second. The thickness or the bulkiness of the molecules seems to play an important role. However, for phenol substituted in the position 2, a steric effect or intramolecular interactions may change the substrate's classification within these two groups. It was also noticed that phenobarbital stimulated more than 3-methylcholanthrene the glucuronidation of the corresponding hydroxylated metabolite.

Full Text
Paper version not known

Talk to us

Join us for a 30 min session where you can share your feedback and ask us any queries you have

Schedule a call

Disclaimer: All third-party content on this website/platform is and will remain the property of their respective owners and is provided on "as is" basis without any warranties, express or implied. Use of third-party content does not indicate any affiliation, sponsorship with or endorsement by them. Any references to third-party content is to identify the corresponding services and shall be considered fair use under The CopyrightLaw.