The human organic anion transporter 1 (OAT1; SLC22A6) is highly expressed at the basolateral membrane of proximal tubule cells in human kidneys. There OAT1 mediates the transport of numerous endogenous and exogenous compounds like antibiotics, diuretics, NSAID (non-steroidal anti-inflammatory drugs), antivirals, cytostatics and toxins. OAT1 facilitate the first step uptake at basolateral membrane of proximal tubule cells for renal secretion of a huge number of substrates. Therefore, the regulatory agencies decided that drugs eliminated significantly via the kidney have to be tested as potential inhibitors (substrates) for hOAT1.
Inhibition of hOAT1 mediated PAH uptake by different drugs (100 µM)