Evaluation of the endothelin receptor antagonists ambrisentan, bosentan, macitentan, and sitaxsentan as hepatobiliary transporter inhibitors and substrates in sandwich-cultured human hepatocytes.

Evaluation of the endothelin receptor antagonists ambrisentan, bosentan, macitentan, and sitaxsentan as hepatobiliary transporter inhibitors and substrates in sandwich-cultured human hepatocytes.

Inhibition of the transporter-mediated hepatobiliary elimination of bile salts is a putative mechanism for liver toxicity observed with some endothelin receptor antagonists (ERAs).Sandwich-cultured human hepatocytes were used to study the hepatobiliary distribution and accumulation of exogenous taur...

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Bibliographic Details
Main Authors: Eve-Irene Lepist, Hunter Gillies, William Smith, Jia Hao, Cassandra Hubert, Robert L St Claire, Kenneth R Brouwer, Adrian S Ray
Format: Article
Language:English
Published: Public Library of Science (PLoS) 2014-01-01
Series:PLoS ONE
Online Access:http://europepmc.org/articles/PMC3907537?pdf=render

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http://europepmc.org/articles/PMC3907537?pdf=render

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