Specific Activity3-b | NVP Metabolite3-a | |||||||
---|---|---|---|---|---|---|---|---|
2-HydroxyNVP | 3-HydroxyNVP | 8-HydroxyNVP | 12-HydroxyNVP | |||||
25 μM | 100 μM | 25 μM | 100 μM | 25 μM | 100 μM | 25 μM | 100 μM | |
EROD | 0.032 | 0.007 | 0.253 | 0.283 | 0.047 | 0.141 | 0.064 | 0.020 |
CNDM | 0.079 | 0.034 | 0.381 | 0.407 | 0.107 | 0.239 | 0.132 | 0.061 |
CH | 0.073 | 0.110 | 0.214 | 0.268 | 0.873 | 0.206 | 0.182 | 0.151 |
EFCOD | 0.592 | 0.456 | 0.944 | 0.980 | 0.742 | 0.848 | 0.679 | 0.531 |
MND | 0.643 | 0.546 | 0.947 | 0.988 | 0.877 | 0.895 | 0.752 | 0.623 |
TMH | 0.418 | 0.566 | 0.001 | 0.033 | 0.078 | 0.240 | 0.410 | 0.527 |
MPH | 0.002 | 0.006 | 0.045 | 0.000 | 0.326 | 0.000 | 0.010 | 0.012 |
DODM | 0.046 | 0.104 | 0.007 | 0.000 | 0.025 | 0.017 | 0.064 | 0.100 |
CZH | 0.149 | 0.236 | 0.005 | 0.004 | 0.351 | 0.078 | 0.106 | 0.182 |
TSTH | 0.933 | 0.994 | 0.322 | 0.500 | 0.126 | 0.821 | 0.919 | 0.978 |
LAH | 0.196 | 0.379 | 0.002 | 0.048 | 0.000 | 0.163 | 0.273 | 0.346 |
↵3-a Bold numbers indicate the best correlations.
↵3-b EROD = 7-Ethoxyresorufin-O-deethylase (CYP1A)
CNDM = Caffeine N-demethylase (CYP1A2)
CH = Coumarin 7-hydroxylase (CYP2A6)
EFCOD = furafylline-inhibited 7-ethoxy-4-trifluoromethyl coumarin-O-deethylase (CYP2B6)
MND = S-Mephenytoin N-demethylase (CYP2B6)
TMH = Tolbutamide methyl-hydroxylase (CYP 2C9)
MPH = S-Mephenytoin 4-hydroxylase (CYP2C19)
DODM = Dextromethorphan O-demethylase (CYP2D6)
CZH = Chlorzoxazone 6-hydroxylase (CYP2E1)
TSTH = Testosterone 6β-hydroxylase (CYP3A4)
LAH = Lauric acid 12-hydroxylase (CYP4A)
n = 10, except for 3-hydroxynevirapine (25 μM), wheren = 9, and 8-hydroxynevirapine (25 μM), wheren = 5