MDI RE       MDI HLM   literature
  IC50 (µM) IC50 (µM) Fold   First IC50 Second IC50 Fold-  
Compound Y/N Y/N* results
(0-10 min) (25-30 min) change (µM) (µM) change
       
Amiodarone 8.75 1.01 8.62 Y 100 31.2 3.21 Y Y
Clozapine 18.90 1.50 12.60 Y 54 14.72 3.67 Y Y
Desipramine 54.23 16.74 3.24 Y 56.3 23.63 2.38 Y Y
Ketoconazole 0.10 0.10 1.00 N 0.1 0.1 1 N N
Miconazole 0.07 0.12 0.58 N 0.01 0.1 0.1 N N
Nifedipine 4.20 7.72 0.54 N 9.43 9.07 1.04 N N
Phenelzine 90.00 7.90 11.39 Y 100 42.3 2.36 Y Y
Terfenadine 0.18 0.66 0.27 N 96.5 46 2.1 Y Y
Troleandromycin 1.35 0.10 13.50 Y 9.75 0.89 10.98 Y Y
Verapamil 6.20 1.44 4.30 Y 24.83 2.37 10.49 Y Y
Compound 1 1.23 0.09 13.22 Y 40.6 2.4 16.92 Y NR**
Compound 2 100.00 100.00 1.00 N 25.5 0.79 32.28 Y NR
Compound 3 100.00 100.00 1.00 N 100 12 8.33 Y NR
Compound 4 10.07 1.40 7.19 Y 68.8 9.1 7.56 Y NR
Compound 5 0.66 0.07 9.47 Y 29.96 3.62 8.93 Y NR
Compound 6 41.66 25.00 1.67 N 13.9 4.7 2.96 Y NR
Compound 7 100.00 90.00 1.11 N 28.9 27.6 1.05 N NR
Compound 8 100.00 100.00 1.00 N 100 100 1 N NR
Compound 9 100.00 100.00 1.00 N 100 1.9 52.63 Y NR
Compound 10 25.12 2.00 12.56 Y 89.5 3.4 26.32 Y NR
Compound 11 100.00 4.00 25.00 Y 25 1.9 13.16 Y NR
Compound 12 100.00 3.00 33.33 Y 100 26.3 3.8 Y NR
Compound 13 63.10 0.30 210.32 Y 20.7 1.2 17.25 Y NR
Compound 14 100.00 100.00 1.00 N 54.7 0.75 72.93 Y NR
Compound 15 12.59 1.20 10.49 Y 1.2 0.38 3.16 Y NR
Compound 16 100.00 100.00 1.00 N 58.8 7 8.4 Y NR
Compound 17 100.00 5.90 16.95 Y 55.6 4.7 11.83 Y NR
*Y/N: Yes/No; NR**: Not reported
Table 1: Results obtained for potential for MDI using recombinant enzyme (RE) and human liver microsomes (HLM).