NDLI: Pharmacokinetic Study and Metabolite Identification of 1-(3'-bromophenyl)-heliamine in Rats.

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Pharmacokinetic Study and Metabolite Identification of 1-(3'-bromophenyl)-heliamine in Rats.

Content Provider	Europe PMC
Author	Xi, Ruqi Abdulla, Rahima Zhang, Miaomiao Sherzod, Zhurakulov Ivanovna, Vinogradova Valentina Habasi, Maidina Liu, Yongqiang
Editor	Durazzo, Alessandra
Copyright 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.
Volume Number	15
PubMed Central reference number	PMC9781129
Issue Number	12
PubMed reference number	36558934
Journal	Pharmaceuticals (Basel)
e-ISSN	14248247
DOI	10.3390/ph15121483
Language	English
Publisher	MDPI
Publisher Date	2022-11-29
Access Restriction	Open
Rights License	Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license (https://creativecommons.org/licenses/by/4.0/). © 2022 by the authors.
Subject Keyword	pharmacokinetic metabolites LC−MS/MS in silico metabolite prediction rats
Content Type	Text
Resource Type	Article
Subject	Drug Discovery Pharmaceutical Science Molecular Medicine

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