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Pharmacokinetic Study and Metabolite Identification of 1-(3′-bromophenyl)-heliamine in Rats.
- Source :
-
Pharmaceuticals (14248247) . Dec2022, Vol. 15 Issue 12, p1483. 13p. - Publication Year :
- 2022
-
Abstract
- Tetrahydroisoquinolines have been widely investigated for the treatment of arrhythmias. 1−(3′−bromophenyl)−heliamine (BH), an anti−arrhythmias agent, is a synthetic tetrahydroisoquinoline. This study focuses on the pharmacokinetic characterization of BH, as well as the identification of its metabolites, both in vitro and in vivo. A UHPLC−MS/MS method was developed and validated to quantify BH in rat plasma with a linear range of 1–1000 ng/mL. The validated method was applied to a pharmacokinetic study in rats. The maximum concentration Cmax (568.65 ± 122.14 ng/mL) reached 1.00 ± 0.45 h after oral administration. The main metabolic pathways appeared to be phase-I of demethylation, dehydrogenation, and epoxidation, and phase II of glucuronide and sulfate metabolites. Finally, a total of 18 metabolites were characterized, including 10 phase I metabolites and 8 phase II metabolites. Through the above studies, we have gained a better understanding of the absorption and metabolism of BH in vitro and in vivo, which will provide us with guidance for future in-depth studies on this compound. [ABSTRACT FROM AUTHOR]
Details
- Language :
- English
- ISSN :
- 14248247
- Volume :
- 15
- Issue :
- 12
- Database :
- Academic Search Index
- Journal :
- Pharmaceuticals (14248247)
- Publication Type :
- Academic Journal
- Accession number :
- 161038413
- Full Text :
- https://doi.org/10.3390/ph15121483