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. 2009 May 18;37(8):1690–1697. doi: 10.1124/dmd.109.027342

TABLE 3.

P450 inhibition of demethyl-IQ formation by liver microsomes from BNF-treated mice

Incubations were conducted for 30 min at 37°C with 0.06 mM IQ. Furafylline was preincubated for 10 min before addition of IQ. For those incubations, the control microsomal activity was 0.25 ± 0.01 nmol, which is not different from the control value above. Data are expressed as mean nanomole of demethyl-IQ ± S.E. with n = 3.

Test Agents Type of P450 Inhibitor Concentration Activity % of Total
μM nmol
Control 0.26 ± 0.04 100
Ellipticine 1A 10 0.03 ± 0.01* 12
20 N.D. 0
Furafylline 1A2 20 0.22 ± 0.01 85
α-Naphthoflavone 1A 20 0.20 ± 0.01 77
100 0.15 ± 0.02* 58
SKF-525A Nonspecific 20 0.19 ± 0.04 73
100 0.12 ± 0.02* 46
Ketoconazole 3A 20 0.17 ± 0.02* 65
100 0.07 ± 0.04* 27
Sulfaphenazole 2C 20 0.19 ± 0.05 73
100 0.20 ± 0.03 77

N.D., not detected.

*

p < 0.05 compared with control.