TABLE 3

Inhibition of efflux transporters by fluorescent bile acid derivatives

Transport experiments were performed as described in Material and Methods. The following substrates were used: BSEP 2 µM taurocholate and MRP2 10 µM estradiol 17β-d-glucuronide. Transport was measured for 5 minutes. Substrate uptake values in % were corrected for transport in the absence of ATP, and uptake in the absence of inhibitor was set to 100%. Results are the mean from two to four independent experiments with three technical replicates.

Compound[I]BSEPMRP2
µM
CenNBD0100100
187.594.5
1046.0124
10012.0140
CenDNS0100100
182.078.5
1050.5106
1006.0152
CenPB0100100
180.094.5
1058.094.5
10016.591.0
CDCenNBD0100100
167.5122
1040.5151
1006.5228
CDCenDNS0100100
185.5115
1043.0132
10025.5179
CDCenPB0100100
161.5107
1013.0151
1000.559.3
AcenNBD0100100
1103136
1097.5132
10094.5145
AcenDNS0100100
196.5139
1097.0136
10087.5151
AcenPB0100100
111699
1010895
10010293