In Vitro Inhibition of Renal OCT2 and MATE1 Secretion by Antiemetic Drugs.

ABSTRACT: The organic cation transporter 2 (OCT2) and multidrug and toxin extrusion protein 1 (MATE1) mediate the renal secretion of drugs. Recent studies suggest that ondansetron, a 5-HT₃ antagonist drug used to prevent nausea and vomiting, can inhibit OCT2- and MATE1-mediated transport. The purpose of this study was to test the ability of five 5-HT₃ antagonist drugs to inhibit the OCT2 and MATE1 transporters. The transport of the OCT2/MATE1 probe substrate ASP⁺ was assessed using two models: (1) HEK293 kidney cells overexpressing human OCT2 or MATE1, and (2) MDCK cells transfected with human OCT2 and MATE1. In HEK293 cells, the inhibition of ASP⁺ uptake by OCT2 listed in order of potency was palonosetron (IC₅₀: 2.6 μM) > ondansetron > graniset

SUBMITTER: George B 

PROVIDER: S-EPMC8234231 | biostudies-literature | 2021 Jun

REPOSITORIES: biostudies-literature