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- W2001524017 abstract "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 (Kt = 15.4 ± 4.1 μM, Jmax = 0.476 ± 0.028 pmol/s/cm2). hOCT3 transported pramipexole in a low affinity manner (Kt = 138 ± 31 μM, Jmax = 1.10 ± 0.08 pmol/s/cm2). 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." @default.
- W2001524017 created "2016-06-24" @default.
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- W2001524017 date "2010-06-03" @default.
- W2001524017 modified "2023-10-10" @default.
- W2001524017 title "Uptake of Pramipexole by Human Organic Cation Transporters" @default.
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- W2001524017 doi "https://doi.org/10.1021/mp100036b" @default.
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