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4.4 OAT SUBSTRATES AND DRUG–DRUG (DRUG–METABOLITE) INTERACTION 4.4.1 Substrates

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Multiple reviews describe the OAT substrates in great detail [23, 24, 114]. Here, we provide some general information. OATs handle a remarkably chemically diverse set of small molecule organic anions, including important and commonly prescribed pharmaceuticals (e.g., penicillins, cephalosporins, antiretrovirals, antihypertensives, antineoplastics, and diuretics), endogenous metabolites (e.g., cortisol and estrone‐3‐sulfate), and hormones, as well as environmental contaminants and toxicants (e.g., conjugates of organic mercury, perfluoroctanoic acid, ochratoxin A, and aristocholic acid), among others [24]. Because of the broad spectrum nature of the substrates, there are several substrates that are commonly used as tracers in published studies mostly performed in vitro assays. Some of the tracer/substrates include glutarate, PAH (para‐aminohippurate, a synthetic molecule), estrone sulfate, and more recently fluorescent compounds of fluorescein, 6‐carboxyfluorecein, and 5‐carboxyfluorecein.

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