title: The history and future of probenecid.
abstract: Probenecid was initially developed with the goal of reducing the renal excretion of antibiotics, specifically penicillin. It is still used for its uricosuric properties in the treatment in gout, but its clinical relevance has sharply fallen and is rarely used today for either. Interestingly, throughout the last 60 years, there have been a host of apparently unrelated studies using probenecid in the clinical and basic research arena, including its potential use in the diagnosis and treatment of depression and its use to prevent fura-2 leakage in calcium transient studies. Recently, it has been shown that it is also an agonist of the Transient Receptor Potential Vanilloid 2 channel. Due to its unique action and new findings implicating TRPV channels in physiology and in disease, probenecid may have a new future as a research tool, and perhaps as a clinical agent in the neurology and cardiology fields. We review the history of probenecid in this paper and its potential future uses.
authors.affiliation: Department of Internal Medicine, Division of Cardiovascular Diseases, College of Medicine, University of Cincinnati, Cincinnati, OH 45267, USA.
authors.forename: Nathan
authors.initials: N
authors.lastname: Robbins
authors.forename: Sheryl E
authors.initials: SE
authors.lastname: Koch
authors.forename: Michael
authors.initials: M
authors.lastname: Tranter
authors.forename: Jack
authors.initials: J
authors.lastname: Rubinstein
mesh_terms: D000818:Animals; D000900:Anti-Bacterial Agents / Q000037:antagonists & inhibitors / Q000493:pharmacokinetics; D003863:Depression / Q000188:drug therapy / Q000378:metabolism; D016257:Fura-2 / Q000378:metabolism; D006073:Gout / Q000188:drug therapy / Q000378:metabolism; D006801:Humans; D011339:Probenecid / Q000737:chemistry / Q000493:pharmacokinetics* / Q000627:therapeutic use*; D050916:TRPV Cation Channels / Q000502:physiology; D014528:Uricosuric Agents / Q000737:chemistry / Q000493:pharmacokinetics* / Q000627:therapeutic use*
chemical_list: D000900:Anti-Bacterial Agents; D050916:TRPV Cation Channels; C400769:TRPV2 protein, human; D014528:Uricosuric Agents; D011339:Probenecid; D016257:Fura-2