Premium
Evaluation of the metabolism of propranolol by linear ion trap technology in mouse, rat, dog, monkey, and human cryopreserved hepatocytes
Author(s) -
Baughman Todd M.,
Talarico Christine L.,
Soglia John R.
Publication year - 2009
Publication title -
rapid communications in mass spectrometry
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.528
H-Index - 136
eISSN - 1097-0231
pISSN - 0951-4198
DOI - 10.1002/rcm.4130
Subject(s) - hepatocyte , drug metabolism , chemistry , propranolol , metabolism , metabolite , microsome , biochemistry , pharmacology , biology , enzyme , in vitro , endocrinology
Propranolol is a widely used quality control and validation compound for liver microsome and hepatocyte metabolism studies. A multitude of literature reports describing the identification of propranolol metabolites exists today. However, no literature reports currently exist showing hepatocyte metabolism across the five species commonly used during pre‐clinical drug discovery, namely mouse, rat, dog, monkey, and human. Herein, we present full metabolic profiles of propranolol in mouse, rat, dog, monkey and human hepatocytes. As expected, extensive phase I and phase II metabolism was observed across all five species and species‐specific metabolites were detected in monkey and dog hepatocytes. Of particular interest was the detection of an N ‐hydroxylamine glucuronide metabolite in monkey and dog hepatocytes. Copyright © 2009 John Wiley & Sons, Ltd.