Pramipexole is a hydrophilic, weakly basic drug, but exhibits high oral bioavailability in humans (>90%). In rats, rOct1 and rOct2 contribute toward pramipexole excretion into urine. The objective of this study was to assess whether pramipexole is a substrate for human OCT1-3. In vitro uptake studies were performed using hOCT1-MDCK monolayers, hOCT2-HEK cells and hOCT3-HEK cells. hOCT2 transported pramipexole in a high affinity manner (K(t) = 15.4 +/- 4.1 microM, J(max) = 0.476 +/- 0.028 pmol/s/cm(2)). hOCT3 transported pramipexole in a low affinity manner (K(t) = 138 +/- 31 microM, J(max) = 1.10 +/- 0.08 pmol/s/cm(2)). Although previously reported to be translocated by rOct1, pramipexole was not a substrate for hOCT1. The human intestinal absorption of pramipexole may involve transport by OCT3 and possibly OCT2. OCT2- and OCT3-mediated transport of pramipexole have implications in the drug's elimination from the kidney and distribution in the brain, respectively.
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