TABLE 4

Rank order comparison of inhibitors on the Pgp-mediated transport of selected probe substrates across MDR1-MDCKII cells


Probe

IC50 Value
<5
5-15
15-50
>50
μM
Calcein-AM 918, CsA K V, Q, VB, P, A
Colchicine 918, CsA K V, VB Q, P, A, Dau
Digoxin 918, CsA, K V, Q VB
Prazosin 918, CsA, K, V Q VB Prop, A, I
Vinblastine
918
CsA, K
V, Q
VB, A, Dau
  • 918, GF120918; A, amprenavir; CsA, cyclosporine A; Dau, daunorubicin; I, indinavir; K, ketoconazole; P, prazosin; Prop, propranolol; Q, quinidine; VB, vinblastine; V, verapamil.