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2-Aminoethyl Diphenyl Borinate (2-APB) Inhibits TRPM7 Channels Through an Intracellular Acidification Mechanism
Channels
  • Rikki Chokshi
  • Petronilla Fruasaha
  • J. Ashot Kozak, Wright State University - Main Campus
Document Type
Article
Publication Date
8-24-2012
Abstract

2-APB is a widely used compound in ion channel research. It affects numerous channels including inositol 1,4,5-trisphosphate receptors, store-operated calcium channels and TRP channels, TRPV3 and TRPM7 among them. A characteristic property of TRPM7 channels is their sensitivity to intracellular Mg2+ and pH. Using patch clamp electrophysiology we find that in Jurkat T lymphocytes, 100–300 µM extracellular 2-APB reversibly inhibits TRPM7 channels when internal HEPES concentration is low (1 mM). Increasing the concentration to 140 mM abolishes the 2-APB effect. Using single-cell fluorescence pH video imaging, we show that at concentrations of 100 µM and higher, 2-APB potently acidifies the cytoplasm. We conclude that TRPM7 sensitivity to 2-APB is not direct but rather, can be explained by cytoplasmic acidification and a resulting channel inhibition.

DOI
10.4161/chan.21628
Citation Information
Rikki Chokshi, Petronilla Fruasaha and J. Ashot Kozak. "2-Aminoethyl Diphenyl Borinate (2-APB) Inhibits TRPM7 Channels Through an Intracellular Acidification Mechanism" Channels Vol. 6 Iss. 5 (2012) p. 1 - 8 ISSN: 1933-6969
Available at: http://works.bepress.com/j_kozak/30/