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Probenecid, a gout remedy, inhibits pannexin 1 channels
Open accessAbstract
Probenecid is a well-established drug for the treatment of gout and is thought to act on an organic anion transporter, thereby affecting uric acid excretion in the kidney by blocking urate reuptake. Probenecid also has been shown to affect ATP release, leading to the suggestion that ATP release involves an organic anion transporter. Other pharmacological evidence and the observation of dye uptake, however, suggest that the nonvesicular release of ATP is mediated by large membrane channels, with pannexin 1 being a prominent candidate. In the present study we show that probenecid inhibited currents mediated by pannexin 1 channels in the same concentration range as observed for inhibition of transport processes. Probenecid did not affect channels formed by connexins. Thus probenecid allows for discrimination between channels formed by connexins and pannexins.
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Cited by
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Chekeni, F. B., Elliott, M. R., Sandilos, J. K., Walk, S. F., Kinchen, J. M., Lazarowski, E. R., Armstrong, A. J., Penuela, S., Laird, D. W., Salvesen, G. S., et al. (2010) · Nature · doi:10.1038/nature09413 · Cited by 1,120
Fontainhas, A. M., Wang, M., Liang, K. J., Chen, S., Mettu, P., Damani, M., Fariss, R. N., Li, W., & Wong, W. T. (2011) · PLoS ONE · doi:10.1371/journal.pone.0015973 · Cited by 334
Intercellular Ca2+Waves: Mechanisms and Function
Leybaert, L., & Sanderson, M. J. (2012) · Physiological Reviews · doi:10.1152/physrev.00029.2011 · Cited by 331
Activation of Neuronal NMDA Receptors Triggers Transient ATP-Mediated Microglial Process Outgrowth
Dissing-Olesen, L., LeDue, J. M., Rungta, R. L., Hefendehl, J. K., Choi, H. B., & MacVicar, B. A. (2014) · Journal of Neuroscience · doi:10.1523/jneurosci.0405-14.2014 · Cited by 286
Glial Connexins and Pannexins in the Healthy and Diseased Brain
Giaume, C., Naus, C. C., Sáez, J. C., & Leybaert, L. (2021) · Physiological Reviews · doi:10.1152/physrev.00043.2018 · Cited by 154
Metadata
- Authors
- Silverman, W., Locovei, S., & Dahl, G.
- Venue
- American Journal of Physiology-Cell Physiology
- Publisher
- American Physiological Society
- Published
- 2008-09
- Volume
- 295
- Issue
- 3
- Pages
- C761-C767
- ISSN
- 0363-6143 (ISSN-L)
- 1522-1563
- OpenAlex
- W2157577807
- Cited by
- 426
- References
- 0
- FWCI
- 10.94
- Type
- journal article
- Language
- en
- Open access
- green
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- Silverman, W., Locovei, S., & Dahl, G. (2008). Probenecid, a gout remedy, inhibits pannexin 1 channels. American Journal of Physiology-Cell Physiology. https://doi.org/10.1152/ajpcell.00227.2008
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