Table 3

Percent inhibition at 10 μM inhibitor for fluorometric and traditional substrates

CompoundBzResBQDBFBFCNFTSMDZ
Astemizole21707178937492
CarbamazepineActivation060100212
Cisapride53968493989193
Clotrimazole90100989810097100
Cyclosporin83396877533588
Digitoxin00000 40
Erythromycin75102672141427
Ethynylestradiol50717685707740
HaloperidolActivation121925961727
Itraconazole75739287939392
Ketoconazole8093989610096100
Miconazole788795931009699
Midazolam15688182657150 3-a
NaphthoflavoneActivationActivation15Activation203312
Nicardipine808878989998100
Nifedipine037715750 3-a 6126
Nimodipine75778091899194
Posicor8397939510097100
ProgesteroneActivation050Activation61817
Propofol2386178 016
Quercetin076193270
Quinidine208521303010
TamoxifenActivation157290 06
TerfenadineActivation537472817094
TestosteroneActivation020Activation550 3-a 14
Troleandomycin84638097835597
Verapamil66517392255946

Assays were conducted as described under Experimental Procedures. For linear regression analysis, activation was treated as 0% inhibition.

  • 3-a  Assigned 50% inhibition based on the use of a concentration that gives a half maximal rate of metabolism.