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2012 ; 6
(5
): 362-9
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2-aminoethyl diphenyl borinate (2-APB) inhibits TRPM7 channels through an
intracellular acidification mechanism
#MMPMID22922232
Chokshi R
; Fruasaha P
; Kozak JA
Channels (Austin)
2012[Sep]; 6
(5
): 362-9
PMID22922232
show ga
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 Mg ( 2+) 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.