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]	BSEP	MRP2
	µM
CenNBD	0	100	100
	1	87.5	94.5
	10	46.0	124
	100	12.0	140
CenDNS	0	100	100
	1	82.0	78.5
	10	50.5	106
	100	6.0	152
CenPB	0	100	100
	1	80.0	94.5
	10	58.0	94.5
	100	16.5	91.0
CDCenNBD	0	100	100
	1	67.5	122
	10	40.5	151
	100	6.5	228
CDCenDNS	0	100	100
	1	85.5	115
	10	43.0	132
	100	25.5	179
CDCenPB	0	100	100
	1	61.5	107
	10	13.0	151
	100	0.5	59.3
AcenNBD	0	100	100
	1	103	136
	10	97.5	132
	100	94.5	145
AcenDNS	0	100	100
	1	96.5	139
	10	97.0	136
	100	87.5	151
AcenPB	0	100	100
	1	116	99
	10	108	95
	100	102	93