Research paperDistinction of CYP1A1 and CYP1A2 activity by selective inhibition using fluvoxamine and ISOSAFROLE (cas 120-58-1)

Add time:08/31/2019    Source:sciencedirect.com

Ethoxyresorufin O-deethylation (EROD) has been used as a specific probe for CYP1A1 and CYP1A2. Selective inhibition of one of these cytochromes P450 may differentiate their activity in human liver. Four inhibitors were chosen to examine the selective inhibition of EROD activity, using cDNA of CYP1A1 and CYP1A2. The two flavones, α-naphthoflavone and apigenin, while differing in potency, inhibited expressed human CYP1A1, CYP1A2, and human liver microsomes to a similar extent. Isosafrole and fluvoxamine were found to inhibit CYP1A2 selectively, with Ki, values of 14 and 800 times, respectively, lower than those for CYP1A1. A set of equations was developed to estimate both CYP1A1 and CYP1A2 activity. Levels of CYP1A2 in four human liver specimens ranged from 44.4 to 76.7 pmol/mg protein, which significantly correlated with phenacetin O-deethylase activity (gt = 0.99; P < 0.001). Low levels of CYP1A1 activity were present in all four investigated livers, ranging from 0.4 to 2.7 pmol/mg protein. BIOCHEM PHARMACOL 53;4:531–538, 1997. /sC 1997 Elsevier Science Inc.

We also recommend Trading Suppliers and Manufacturers of ISOSAFROLE (cas 120-58-1). Pls Click Website Link as below: cas 120-58-1 suppliers

Prev:Solvent and support electrolyte effects on the catalytic activity of Ti/RuO2 and Ti/IrO2 electrodes: oxidation of ISOSAFROLE (cas 120-58-1) as a probe model
Next:Catalytic and immunochemical properties of hepatic cytochrome P450 1A in three avian species treated with β-naphthoflavone or ISOSAFROLE (cas 120-58-1))