Compounds > 6-(4-chlorophenyl)imidazo(2-1-b)(1-3)thiazole-5-carbaldehyde-o-(3-4-dichlorobenzyl)oxime

6-(4-chlorophenyl)imidazo(2-1-b)(1-3)thiazole-5-carbaldehyde-o-(3-4-dichlorobenzyl)oxime and 1-aminobenzotriazole

6-(4-chlorophenyl)imidazo(2-1-b)(1-3)thiazole-5-carbaldehyde-o-(3-4-dichlorobenzyl)oxime has been researched along with 1-aminobenzotriazole* in 1 studies

Other Studies

1 other study(ies) available for 6-(4-chlorophenyl)imidazo(2-1-b)(1-3)thiazole-5-carbaldehyde-o-(3-4-dichlorobenzyl)oxime and 1-aminobenzotriazole

Article	Year
Induction of CYP2B6 and CYP3A4 expression by 1-aminobenzotriazole (ABT) in human hepatocytes. Drug metabolism letters, 2010, Volume: 4, Issue:3 1-Aminobenzotriazole (ABT) has been widely used in drug development process as an irreversible inhibitor of CYP enzymes. One potential use of ABT is to potentiate pharmacological effects of rapidly-metabolized drugs on CYP expression by inhibiting their metabolism; however, ABT's own effects on CYP expression have been unknown. In this study, we show that ABT up-regulates expression of CYP2B6 and CYP3A4 potentially by activating nuclear receptor CAR. In freshly isolated human hepatocytes, ABT increased mRNA expression of CYP2B6 and CYP3A4 in a concentration-dependent manner. ABT also modulated CYP-inducing actions of CITCO and rifampin, the known inducers of CYP2B6 and CYP3A4. Results from luciferase reporter assays confirmed that ABT increases CYP2B6 promoter activity in CAR-expressing HepG2 cells. These results suggest that the use of ABT as a potentiator of pharmacological effects of rapidly-metabolized drugs is limited due to its own pharmacological actions on CYP expression as a CAR activator. Topics: Aryl Hydrocarbon Hydroxylases; Constitutive Androstane Receptor; Cytochrome P-450 CYP2B6; Cytochrome P-450 CYP3A; Dose-Response Relationship, Drug; Enzyme Induction; Gene Expression Regulation, Enzymologic; Hep G2 Cells; Hepatocytes; Humans; Oxidoreductases, N-Demethylating; Oximes; Promoter Regions, Genetic; Receptors, Cytoplasmic and Nuclear; Rifampin; RNA, Messenger; Thiazoles; Transcriptional Activation; Transfection; Triazoles	2010

Article

Year

Induction of CYP2B6 and CYP3A4 expression by 1-aminobenzotriazole (ABT) in human hepatocytes.

Drug metabolism letters, 2010, Volume: 4, Issue:3

1-Aminobenzotriazole (ABT) has been widely used in drug development process as an irreversible inhibitor of CYP enzymes. One potential use of ABT is to potentiate pharmacological effects of rapidly-metabolized drugs on CYP expression by inhibiting their metabolism; however, ABT's own effects on CYP expression have been unknown. In this study, we show that ABT up-regulates expression of CYP2B6 and CYP3A4 potentially by activating nuclear receptor CAR. In freshly isolated human hepatocytes, ABT increased mRNA expression of CYP2B6 and CYP3A4 in a concentration-dependent manner. ABT also modulated CYP-inducing actions of CITCO and rifampin, the known inducers of CYP2B6 and CYP3A4. Results from luciferase reporter assays confirmed that ABT increases CYP2B6 promoter activity in CAR-expressing HepG2 cells. These results suggest that the use of ABT as a potentiator of pharmacological effects of rapidly-metabolized drugs is limited due to its own pharmacological actions on CYP expression as a CAR activator.

Topics: Aryl Hydrocarbon Hydroxylases; Constitutive Androstane Receptor; Cytochrome P-450 CYP2B6; Cytochrome P-450 CYP3A; Dose-Response Relationship, Drug; Enzyme Induction; Gene Expression Regulation, Enzymologic; Hep G2 Cells; Hepatocytes; Humans; Oxidoreductases, N-Demethylating; Oximes; Promoter Regions, Genetic; Receptors, Cytoplasmic and Nuclear; Rifampin; RNA, Messenger; Thiazoles; Transcriptional Activation; Transfection; Triazoles

2010