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Substrates have been more difficult to determine for OATs because of the demand for radiolabeled substrates or mass spectrometry‐based analysis methods. A popular alternative to these types of studies is to perform inhibition assays, where potential interacting molecules are screened for inhibition of classic OAT function, often with probe substrates or fluorescent substrates. Due to the multi‐specific nature of the OATs, several inhibitors of OAT function have been reported, yet specific inhibitors of the individual transporters have yet to be identified. Nevertheless probenecid, which is nonspecific, has historically been used as an inhibitor of OAT‐mediated anionic drug uptake and handling [23]. Probenecid does not appear to be transported by the OATs and is believed to block transport of other organic anions through its binding to the transporter which (in the case of the kidney) decreases renal excretion and enhances plasma retention of drugs, an example being the common practice of co‐administering probenecid to prolong the action of beta‐lactam antibiotics [23].