Figure 2.

Inhibition of OAT1-mediated fluorescein uptake by a panel of drugs commonly used in CKD management. (A) Schematic representation of the co-incubation of fluorescein with variable concentration of drugs. (B) Fluorescein uptake (1 µM) by ciPTEC-OAT1 in the presence of drugs (ACEIs: captopril, enalaprilate and lisinopril; ARBs: losartan and valsartan; statins: pravastatin and simvastatin; diuretics: furosemide) relative to the uptake of fluorescein without drugs (=100%). The histamine H2 receptor antagonist (H2RA): cimetidine) was used as a reference of no inhibitory effect on OAT1-mediated fluorescein. All data are expressed as mean ± SD of four independent experiments. Grey regions indicate the therapeutic window of the respective drug.