Publication Details

Bartlett, R., Stokes, L., Curtis, S. J., Curtis, B. L. & Sluyter, R. (2017). Probenecid directly impairs activation of the canine P2X7 receptor. Nucleosides, Nucleotides and Nucleic Acids: an international journal for rapid communication, 36 (12), 736-744.


The current study aimed to determine if probenecid could directly impair the canine P2X7 receptor, a ligand-gated cation channel activated by extracellular adenosine 5′-triphosphate (ATP). Patch clamp measurements demonstrated that probenecid impairs ATP-induced inward currents in HEK-293 cells expressing canine P2X7. Flow cytometric measurements of ethidium + uptake into HEK-293 cells expressing canine P2X7 showed that probenecid impairs ATP-induced pore formation in a concentration-dependent manner, with a half maximal inhibitory concentration of 158 µM. Finally, ELISA measurements revealed that probenecid impairs ATP-induced interleukin-1β release in dog blood. In conclusion, this study reveals that probenecid can directly impair canine P2X7 activation.



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