AI Article Synopsis
- The study examined how different forms of propranolol (R-(+) and S-(-)) are metabolized through glucuronidation in rats' liver microsomes.
- A special analytical method was created to quantify the amounts of each form of propranolol’s glucuronide produced during metabolism.
- Results indicated that R-(+) propranolol is metabolized more than S-(-), showing a clear preference in the metabolic process, which also suggested a concentration-dependent interaction between the two forms.
Article Abstract
Objective: To study the stereoselectivity of R-(+) and S-(-)-propranolol glucuronidation and metabolic interaction between R(+)- and S-(-)-propranolol.
Methods: A RP-HPLC analytical method was developed for determination of R-(+)-and S-(-)-propranolol glucuronide (PG) incubated with rat hepatic microsome induced with phenobarbital (PB). The method was applied to investigate the stereoselectivity metabolism of racemic propranolol glucuronidation in vitro.
Result: In control and PB group, the concentration of R-(+)-PG produced at different substrates was higher than that of S-(-)-PG. Compared with the control, the V(max) and Cl(int) for R(+)-and S-(-)-propranolol increased significantly the K(m) for R(+)-propranolol was elevated, while that for S-(-) propranolol was decreased.
Conclusion: There is a stereoselectivity in glucuronidation of propranolol in rat hepatic microsome induced with PB and R-(+)-propranolol is preferred. Metabolic interaction between R-(+)-and S-(-)-propranolol exists with a concentration-dependent mode.
Download full-text PDF |
Source |
|---|---|
| http://dx.doi.org/10.3785/j.issn.1008-9292.2004.01.002 | DOI Listing |
Publication Analysis
Top Keywords
Similar Publications
Want AI Summaries of new PubMed Abstracts delivered to your In-box?
Enter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!