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.^1,2,3,4,5,6 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).^1,2,3,4 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.⁶ It is an agonist of TRPV2 (EC₅₀ = 31.9 µM).⁵ 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.⁵ Formulations containing probenecid have been used in the treatment of gouty arthritis.

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