Cayman Probenecid

Probenecid is a benzoic acid derivative that inhibits organic anion transporters (OATs) and the ATP-binding cassette transporter (ABCC1) multidrug resistance protein 1 (MRP1) and activates the transient receptor potential (TRP) channel TRPV2.^,,,,, It inhibits OAT1, OAT3, and OAT6 (K_is = 6.3, 9.0, and 8.4 µM, respectively), as well as OAT2 (IC₅₀ = 0.67 µM), and is selective for OATs over organic cation transporter 1 (OCT1) and OCT2 (IC₅₀s = 1,600 and 1,700 µM, respectively).^,,, Probenecid (7 mm) decreases Fas antibody-induced glutathione (GSH) efflux and staurosporine-induced efflux of the MRP1 substrate calcein in Jurkat cells and decreases apoptotic progression. It is an agonist of TRPV2 (EC₅₀ = 31.9 µM). It induces nociceptive behavior in mouse models of carrageenan- or complete Freund’s adjuvant-induced inflammatory pain when administered at a dose of 20 mm in drinking water in combination with doses of carrageenan or CFA that do not provoke pain responses alone. Formulations containing probenecid have been used in the treatment of gouty arthritis.

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