Fig. 3.

Accumulation of currently marketed statins in whole brain tissue is determined by OATP-mediated transport at the BBB. Effect of an established Oatp transport inhibitor (i.e., FEX) on the uptake of [³H]atorvastatin (A), [³H]pravastatin (B), and [³H]rosuvastatin (C) was assessed by in situ brain perfusion studies. Accumulation of statin drugs was measured in animals injected with BMP-9 (1 μg/kg, i.p.; 6-hour treatment) in the presence and absence of LDN193189 (10 mg/kg, i.p.; 1-hour pretreatment) where animals were perfused with FEX (100 μM) prior to perfusion with radiolabeled atorvastatin, pravastatin, or rosuvastatin. Results are expressed as mean ± S.D. of six animals per time point. Asterisks represent data points that were significantly different from control animals (*p < 0.05; **p < 0.01).