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. 2010 Mar 10;30(10):1742–1755. doi: 10.1038/jcbfm.2010.36

Figure 3.

Figure 3

The BCRP-specific BODIPY FL prazosin transport in isolated brain capillaries. (A) Accumulation of BODIPY FL prazosin (BP) fluorescence in capillary lumens is sensitive to unlabeled prazosin, to the BCRP inhibitors, FTC, Ko143, GF120918, and to the metabolic inhibitor, NaCN. In contrast, the P-glycoprotein-specific inhibitor, PSC833, and the Mrp substrates/inhibitors, LTC4, probenecid and MK571, had no effect on luminal BODIPY FL prazosin accumulation. These data indicate that BODIPY FL prazosin transport in brain capillaries is BCRP specific. (B–E) Nonlinear regression curves (Hill coefficient=1) for prazosin (B; EC50: 93.7 nmol/L), GF120918 (C; EC50: 94.1 nmol/L), FTC (D; EC50: 49.8 nmol/L), and Ko143 (E; EC50: 3.1 nmol/L). Each data point represents the mean±s.e.m. for 10 to 15 capillaries from a single preparation (pooled tissue from 3 to 10 rats). Units are arbitrary fluorescence units (scale 0 to 255). Statistical comparison: ***significantly lower than controls, P<0.001. BCRP, breast cancer resistance protein; FTC, fumitremorgin C.