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Drug Metabolism Letters

Editor-in-Chief

ISSN (Print): 1872-3128
ISSN (Online): 1874-0758

The Utility of Stable Cell Lines to Assess Species Differences in PXR Transactivation

Author(s): Michael W. Sinz, Devin Pray and Judy Raucy

Volume 1, Issue 2, 2007

Page: [147 - 152] Pages: 6

DOI: 10.2174/187231207780363561

Price: $65

Abstract

A stable cell line was developed to assess activation of rat pregnane X receptor (rPXR) by xenobiotics. Characterization revealed that the greatest response occurred with dexamethasone (6-10 fold increase) while rifampicin failed to transactivate rPXR. Rodent PXR transactivation assays can be used to understand species differences in enzyme induction.

Keywords: Rat PXR, stable cells, CYP3A induction, toxicity, high volume screening


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