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Phenobarbital Confers its Diverse Effects by Activating the Orphan Nuclear Receptor Car

Year: 2006

Type: review

Abstract: In the early 1960s, phenobarbital (PB) was shown to induce hepatic drug metabolism and the induction was implicated in the molecular mechanism of drug tolerance development. Since then, it has become evident that PB not only induces drug metabolism, but also triggers pleiotropic effects on liver function, such as cell growth and communication, proliferation of the endoplasmic reticulum, tumor promotion, glucose metabolism, steroid/thyroid hormone metabolism, and bile acid synthesis. Upon activation by PB and numerous PB-type inducers, the nuclear receptor CAR mediates those pleiotropic actions by regulating various hepatic genes, utilizing multiple regulatory mechanisms.

Source: Drug Metabolism Reviews

DOI: 10.1080/03602530600569851

Authors: Susumu Kodama, Masahiko Negishi

Institutions: National Institutes of Health, National Institute of Environmental Health Sciences

Language: English

Topic: Pharmacogenetics and Drug Metabolism

Subfield: Pharmacology

Field: Pharmacology, Toxicology and Pharmaceutics

Domain: Life Sciences

SDG: Good health and well-being

Open Access status: green

OpenAlex ID: W2154022599

FWCI: 0.997

Cites: 62

Cited by: 77

Related to: 10