Probenecid (Benemid) is a benzoic acid derivative with antihyperuricemic property.

Probenecid是肾脏,肝脏和眼睛中单胺转运的竞争性抑制剂.Probenecid能够降低肾脏对抗生素的清除,这能够增强了血清中抗生素的水平.Probenecid作为OTA竞争性抑制剂,这阻止了OAT介导的尿酸从尿液中再摄取进入血清,增强肾脏中尿酸的排泄.

在1321N1星形细胞瘤中,Probenecid（2.5 mM） 能够阻断Fura-2从流出,并且不改变基底钙离子浓度或毒蕈碱钙响应。

Probenecid is dissolved at 500 mM in 1 N NaOH and titrated to pH 7.0[1]. HEK-293T cells are transfected with hTAS2R expression constructs using Lipofectamine 2000 in poly-lysine coated, black 384-well plates with clear bottoms and incubated for 22 hours at 37°C. Growth media is removed and cells are washed twice with HBSS containing 20 mM HEPES, then loaded with a calcium indicator dye in HBSS containing 20 mM HEPES (Calcium 4 Assay kit) with or without 1 mM Probenecid. Cells are incubated at 37°C for 1 hour in the presence of both dye and Probenecid, then moved to a Flexstation II-384 set for 32°C. After a 15-minute temperature equilibration (without washout), indicated compounds are injected (at t=~25 seconds) and fluorescence is measured for 100 to 180 seconds, reading every 3 seconds. Data sets are analyzed and represented as % over baseline signal using Prism 5.0 software. For Schild plots, replicates of raw calcium flux values are expressed as % over baseline signal. The mean value at 36 seconds (corresponding to the maximum flux signal) for each concentration of TAS2R ligand in the presence of the indicated concentration of Probenecid is plotted against the log of ligand concentration. Data points are fit using non-linear regression in GraphPad Prism[1].