Title : Benzodiazepines medazepam and midazolam are activators of pregnane X receptor and weak inducers of CYP3A4: investigation in primary cultures of human hepatocytes and hepatocarcinoma cell lines.

Pub. Date : 2010 Mar 15

PMID : 20080160






3 Functional Relationships(s)
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1 Benzodiazepines medazepam and midazolam are activators of pregnane X receptor and weak inducers of CYP3A4: investigation in primary cultures of human hepatocytes and hepatocarcinoma cell lines. Midazolam nuclear receptor subfamily 1 group I member 2 Homo sapiens
2 Consistently, two-hybrid mammalian assay using hybrid fusion plasmids GAL4-PXR ligand-binding domain (LBD) and VP16-SRC-1-receptor-interacting domain (RID) confirmed PXR activation by Midazolam and Medazepam. Midazolam nuclear receptor subfamily 1 group I member 2 Homo sapiens
3 Medazepam and Midazolam slightly activated pregnane X receptor and displayed weak potency to induce CYP3A4 mRNA in human hepatocytes. Midazolam nuclear receptor subfamily 1 group I member 2 Homo sapiens