TABLE 1

LogP/D values for the 39 drugs investigated and their respective fumic and fuhep values at microsomal and cell concentrations of 1 mg/ml and 106 cells/ml, respectively

Compound
logP/D
fumic
fuhep
a-Naphthoflavone1 Neutral 4.65 0.02 0.03
2-Ethoxybenzamide2,3 Neutral 1.34 0.98 0.90
Albendazole2,3 Neutral 3.29 0.56 0.66
Aldosterone1 Neutral 0.72 0.60 0.54
Androstenedione1 Neutral 2.89 0.49 0.54
Astemizole2,3 Base 4.14 0.01 0.04
Betaxolol2,3 Base 2.40 0.62 0.70
Bumetanide2,3 Acid 0.31 0.92 0.91
Caffeine1 Base –0.13 0.99 0.99
Cerivastatin2,3 Acid 1.44 0.65 0.67
Clozapine2,3 Base 3.60 0.26 0.50
Cortisol1 Neutral 1.42 0.21 0.21
Dextromethorphan1 Base 4.19 0.98 0.93
DHEA1 Neutral 3.42 0.39 0.28
Diazepam2,3 Neutral 2.25 0.69 0.77
Diclofenac1 Acid 1.26 0.76 0.82
Flavone1 Neutral 3.55 0.11 0.13
Fluconazole4 Base 0.50 0.98 0.99
Fluoxetine1 Base 4.05 0.09 0.26
Fluvoxamine1 Base 3.21 0.27 0.54
Gemfibrozil1 Acid 1.80 0.98 0.99
Glyburide2,3 Acid 2.19 0.82 0.60
Imipramine1 Base 4.80 0.45 0.46
Indapamide2,3 Neutral 1.76 0.96 0.82
Isradipine2,3 Neutral 3.75 0.34 0.28
Ketoconazole4 Base 3.54 0.13 0.26
Metyrapone2,3 Neutral 1.37 0.99 0.77
Miconazole4 Base 5.93 0.03 0.06
Naloxone1 Base 2.09 0.87 0.94
Oxaprozin2,3 Acid 1.61 0.87 0.83
Phenytoin1 Base 2.52 0.81 0.83
Progesterone1 Neutral 4.03 0.14 0.27
Propranolol1 Base 3.09 0.55 0.56
Quinidine1 Base 3.44 0.40 0.72
Quinine4 Base 3.44 0.36 0.85
Testosterone1 Base 3.47 0.49 0.62
Tolbutamide1 Acid 0.52 1.00 0.99
Verapamil2,3 Base 4.10 0.37 0.63
Warfarin1
Acid
0.28
1.00
0.93

  • ↵ 1 In-house data determined using dialysis (dead cells) or oil immersion (live cells)

  • ↵ 2 Austin et al. (2002)

  • ↵ 3 Austin et al. (2005)

  • ↵ 4 Brown et al. (2007a)