The Peripheral Benzodiazepine Receptor Ligand PK11195 is a Novel Antagonist of Human Constitutive Androstane Receptor
نویسندگان
چکیده
Department of Pharmaceutical Sciences, School of Pharmacy, University of Maryland at Baltimore, 20 Penn Street, Baltimore Maryland 21201 (L. L., T. C., J. D. S., H. W.) and Pharmacogenetics Section, Laboratory of Reproductive and Developmental Toxicology, National Institute of Environmental and Health Sciences, National Institutes of Health, Research Triangle Park, North Carolina 27709 (T. S., M. N.). Molecular Pharmacology Fast Forward. Published on May 20, 2008 as doi:10.1124/mol.108.046656
منابع مشابه
The peripheral benzodiazepine receptor ligand 1-(2-chlorophenyl-methylpropyl)-3-isoquinoline-carboxamide is a novel antagonist of human constitutive androstane receptor.
As a promiscuous xenobiotic sensor, the constitutive androstane receptor (CAR; NR1I3) regulates the expression of multiple drug-metabolizing enzymes and transporters in liver. The constitutively activated nature of CAR in the cell-based transfection assays has hindered its use as a predictor of metabolism-based drug-drug interactions. Here, we have identified 1-(2-chlorophenylmethylpropyl)-3-is...
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The effects of PK11195, a high-affinity peripheral benzodiazepine receptor (PBR) ligand, on protein phosphorylation in isolated purified rat brain mitochondria were investigated. The isoquinoline carboxamide ligand of PBR, PK11195, but not the benzodiazepine ligand Ro5-4864, in the nanomolar concentration range strongly increased the phosphorylation of 3.5 and 17 kDa polypeptides. The effect of...
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