Table 3.
Compd | ATPase activity (nmoles Pi/min/mg protein)[a] |
Fold stimulation |
---|---|---|
13 | 78 | 2.80 |
14 | 41.40 | 1.47 |
15 | 60.70 | 2.16 |
17 | 78.75 | 2.81 |
18 | 83.70 | 2.98 |
19 | 54.30 | 1.93 |
20 | 42.15 | 1.50 |
21 | 77.20 | 2.75 |
22 | 89.4 | 3.31 |
23 | 92.3 | 3.42 |
Crude membranes (100 μg protein/ml) from P-gp expressing High-Five cells were incubated at 37 °C with 2.5 μM of selected derivatives in the presence and absence of 0. 3 mM sodium orthovanadate in ATPase assay buffer for 5 min, and the vanadate-sensitive ATPase activity of P-gp was determined as described.[44] The vanadate-sensitive ATPase activity was calculated as nmoles Pi/min/mg protein and expressed as fold stimulation with respect to basal ATPase activity (in the presence of solvent DMSO) taken as 1.0. With the same membranes 50 μM verapamil stimulated the ATPase activity of P-gp by 2.5-fold (70 nmoles Pi/min/mg protein).The values are an average of two independent experiments.