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Vol. 60, Issue 3, 541-552, September 2001
Department of Physiological Sciences, Eastern Virginia Medical
School, Norfolk, Virginia
In this study, we examined 2-aminoethoxydiphenyl borate (2APB) as an
inhibitor of Ca2+ influx in human platelets. 2APB was found
to inhibit thrombin-mediated intracellular Ca2+
mobilization rapidly in platelets incubated in the absence of extracellular Ca2+. This result supports an intracellular
action of 2APB on inositol 1,4,5-trisphosphate
(IP3)-receptor Ca2+ channels. 2APB was without
effect on the ability of thapsigargin to mobilize intracellular
Ca2+. This result suggests that the efflux of
Ca2+ from the endoplasmic reticulum mediated by
thapsigargin is not via IP3 Ca2+ channels.
However, 2APB was able to prevent the entry of Ca2+ and
Sr2+ through thapsigargin-activated, store-operated
Ca2+ channels (SOCC). This result supports a direct
inhibitory effect of 2APB on SOCC. 2APB was also able to block the
entry of Sr2+, Ba2+, and Mn2+ entry
into unstimulated platelets, which suggests that 2APB was inhibiting
the Ca2+ influx channels directly. The capacity of 2APB to
prevent Ca2+ influx and Sr2+ influx was rapid
because it occurred immediately upon addition to the platelets. The
inhibition of Ca2+ and Sr2+ influx by 2APB was
similar to that seen with the cell-impermeable nonselective
Ca2+-channel blocker La3+ or the
Ca2+ chelator EGTA. Diphenylboronic anhydride and
2,2-diphenyltetrahydrofuran, two compounds that are structurally
similar to 2APB, also inhibited Ca2+ influx. It was
concluded that 2APB was a rapid and effective direct inhibitor of SOCC
in human platelets; as such, it cannot be used to support the
involvement of IP3 receptors in the activation of SOCC.
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