Chemical Name: 2-Aminoethoxydiphenylborane
Biological ActivityA functional and membrane permeable D-myo-inositol 1,4,5-trisphosphate (IP3) receptor antagonist (IC50 = 42 μM). Stimulates store-operated calcium (SOC) release at low concentrations (< 10 μM) and inhibits it at higher concentrations (up to 50 μM). Increases STIM-Orai channel conductance and limits ion selectivity. Modulator of TRP channels; blocks TRPC1, TRPC3, TRPC5, TRPC6, TRPV6, TRPM3, TRPM7, TRPM8 and TRPP2 and at higher concentrations stimulates TRPV1, TRPV2 and TRPV3. Also blocks specific gap channel subtypes.
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Tocris products are intended for laboratory research use only, unless stated otherwise.
STIM and Orai: the long-awaited constituents of store-operated calcium entry.
Varnai et al.
Block of specific gap junction channel subtypes by 2-aminoethoxydiphenyl borate (2-APB).
Bai et al.
2APB, 2-aminoethoxydiphenyl borate, a membrane-penetrable modulator of Ins(1,4,5)P3-induced Ca2+ release.
Maruyama et al.
Block of TRPC5 channels by 2-aminoethoxydiphenyl borate: a differential, extracellular and voltafe-dependent effect.
Xu et al.
Inhibition of the transient receptor potential cation channel TRPM2 by 2-aminoethoxydiphenyl borate (2-APB).
Togashi et al.
Citations for 2-APB
The citations listed below are publications that use Tocris products. Selected citations for 2-APB include:
44 Citations: Showing 1 - 10
TRPM4 Conductances in Thalamic Reticular Nucleus Neurons Generate Persistent Firing during Slow Oscillations
Authors: O'Malley Et al.
J Neurosci 2020;40:4813
Cell sensing and decision-making in confinement: The role of TRPM7 in a tug of war between hydraulic pressure and cross-sectional area.
Authors: Zhao Et al.
Sci Adv 2019;5:eaaw7243
Role of miRNA-181a-2-3p in cadmium-induced inflammatory responses of human bronchial epithelial cells.
Authors: Kim Et al.
J Thorac Dis 2019;11:3055
Neuronal Activity-Dependent Activation of Astroglial Calcineurin in Mouse Primary Hippocampal Cultures.
Authors: Lim Et al.
Int J Mol Sci 2018;19
Calcium-regulatory proteins as modulators of chemotherapy in human neuroblastoma.
Authors: Florea Et al.
Gpr158 mediates osteocalcin's regulation of cognition.
Authors: Khrimian Et al.
J Exp Med 2017;214:2859
Connexin 32-mediated cell-cell communication is essential for hepatic differentiation from humanembryonic stem cells
Authors: Qin Et al.
Scientific Reports 2016;6:37388
Layer-specific potentiation of network GABAergic inhibition in the CA1 area of the hippocampus.
Authors: Colavita Et al.
Sci Rep 2016;6:28454
Activation of the neurokinin 3 receptor promotes filopodia growth and sprouting in rat embryonic hypothalamic cells.
Authors: Flynn Et al.
The NLRP3 inflammasome is activated by nanoparticles through ATP, ADP and adenosine.
Authors: Baron Et al.
Dev Neurobiol 2015;6:e1629
Pathophysiological significance of the two-pore domain K(+) channel K2P5.1 in splenic CD4(+)CD25(-) T cell subset from a chemically-induced murine inflammatory bowel disease model.
Authors: Nakakura Et al.
Cell Death Dis 2015;6:299
Stimulation-evoked Ca2+ signals in astrocytic processes at hippocampal CA3-CA1 synapses of adult mice are modulated by glutamate and ATP.
Authors: Tang Et al.
J Neurosci 2015;35:3016
Caffeine Modulates Vesicle Release and Recovery at Cerebellar Parallel Fibre Terminals, Independently of Calcium and Cyclic AMP Signalling.
Authors: Dobson Et al.
Biomed Res Int 2015;10:e0125974
Dissecting out the complex Ca2+-mediated phenylephrine-induced contractions of mouse aortic segments.
Authors: Fransen Et al.
PLoS One 2015;10:e0121634
Both neurons and astrocytes exhibited tetrodotoxin-resistant metabotropic glutamate receptor-dependent spontaneous slow Ca2+ oscillations in striatum.
Authors: Tamura Et al.
PLoS One 2014;9:e85351
Capture of microtubule plus-ends at the actin cortex promotes axophilic neuronal migration by enhancing microtubule tension in the leading process.
Authors: Hutchins and Wray
J Biol Chem 2014;8:400
Potent functional uncoupling between STIM1 and Orai1 by dimeric 2-aminodiphenyl borinate analogs.
Authors: Hendron Et al.
Cell Calcium 2014;56:482
Cross-synaptic synchrony and transmission of signal and noise across the mouse retina.
Authors: Grimes Et al.
Activation of a TRP-like channel and intracellular Ca2+ dynamics during phospholipase-C-mediated cell death.
Authors: Gonçalves Et al.
J Cell Sci 2014;127:3817
Endoplasmic reticulum membrane reorganization is regulated by ionic homeostasis.
Authors: Varadarajan Et al.
PLoS One 2013;8:e56603
Antagonism of neuronal prostaglandin E(2) receptor subtype 1 mitigates amyloid β neurotoxicity in vitro.
Authors: Li Et al.
Biochem Pharmacol 2013;8:87
AMP-activated protein kinase as regulator of P2Y(6) receptor-induced Ins secretion in mouse pancreatic β-cells.
Authors: Balasubramanian Et al.
Areca nut-induced buccal mucosa fibroblast contraction and its signaling: a potential role in oral submucous fibrosis--a precancer condition.
Authors: Chang Et al.
Front Cell Neurosci 2013;34:1096
Calcium release-dependent actin flow in the leading process mediates axophilic migration.
Authors: Hutchins Et al.
J Pharmacol Exp Ther 2013;33:11361
In vivo epithelial wound repair requires mobilization of endogenous intracellular and extracellular calcium.
Authors: Aihara Et al.
PLoS One 2013;288:33585
SKF83959, an agonist of phosphatidylinositol-linked D(1)-like receptors, promotes ERK1/2 activation and cell migration in cultured rat astrocytes.
Authors: Huang Et al.
Korean J Physiol Pharmacol 2012;7:e49954
The calcium-sensing receptor regulates the NLRP3 inflammasome through Ca2+ and cAMP.
Authors: Lee Et al.
DHA inhibits ER Ca2+ release and ER stress in astrocytes following in vitro ischemia.
Authors: Begum Et al.
J Neurochem 2012;120:622
Regulation of Substantia Nigra Pars Reticulata GABAergic Neuron Activity by H?O? via Flufenamic Acid-Sensitive Channels and K(ATP) Channels.
Authors: Lee Et al.
Front Syst Neurosci 2011;5:14
Calcium-sensing receptor modulates extracellular Ca(2+) entry via TRPC-encoded receptor-operated channels in human aortic smooth muscle cells.
Authors: Chow Et al.
PLoS One 2011;301:C461
The amiloride-sensitive epithelial Na+ channel PPK28 is essential for drosophila gustatory water reception.
Authors: Chen Et al.
J Neurosci 2010;30:6247
Non-cardiomyocytes influence the electrophysiological maturation of human embryonic stem cell-derived cardiomyocytes during differentiation.
Authors: Kim Et al.
Front Physiol 2010;19:783
Caffeine and 2-Aminoethoxydiphenyl Borate (2-APB) Have Different Ability to Inhibit Intracellular Calcium Mobilization in Pancreatic Acinar Cell.
Authors: Choi Et al.
J Neuroimmune Pharmacol 2010;14:105
Mobilization of calcium from intracellular stores facilitates somatodendritic DA release.
Authors: Patel Et al.
J Neurosci 2009;29:6568
Adenosine-evoked hyperpolarization of retinal ganglion cells is mediated by G-protein-coupled inwardly rectifying K+ and small conductance Ca2+-activated K+ channel activation.
Authors: Clark Et al.
J Neurosci 2009;29:11237
P2Y receptors mediate Ca2+ signaling in duodenocytes and contribute to duodenal mucosal bicarbonate secretion.
Authors: Dong Et al.
Am J Physiol Gastrointest Liver Physiol 2009;296:G424
Estrogen attenuates glutamate-induced cell death by inhibiting Ca2+ influx through L-type voltage-gated Ca2+ channels.
Authors: Sribnick Et al.
Brain Res 2009;1276:159
Regulated release of BDNF by cortical oligodendrocytes is mediated through metabotropic glutamate receptors and the PLC pathway.
Authors: Bagayogo and Dreyfus
ASN Neuro 2009;1
Low concentrations of sphingosylphosphorylcholine enhance pulmonary artery vasoreactivity: the role of protein kinase C δ and Ca2+ entry.
Authors: Snetkov Et al.
Am J Physiol Cell Physiol 2008;51:239
Calcium release from presynaptic internal stores is required for ethanol to increase spontaneous γ-aminobutyric acid release onto cerebellum Purkinje neurons.
Authors: Kelm Et al.
Stem Cells Dev 2007;323:356
Contribution of both Ca2+ entry and Ca2+ sensitization to the alpha1-adrenergic vasoconstriction of rat penile small arteries.
Authors: Villalba Et al.
Am J Physiol Heart Circ Physiol 2007;292:H1157
Nimodipine selectively stimulates beta-amyloid 1-42 secretion by a mechanism independent of calcium influx blockage.
Authors: Facchinetti Et al.
Neurobiol Aging 2006;27:218
PI3K and PKC contribute to membrane depolarization mediated by alpha2-adrenoceptors in the canine isolated mesenteric vein.
BMC Physiol 2005;5:9
2-aminoethoxydiphenyl borate stimulates pulmonary C neurons via the activation of TRPV channels.
Authors: Gu Et al.
Am J Physiol Lung Cell Mol Physiol 2005;288:L932
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HEK293 cells were incubated with intracellular Ca2+ sensitive dye, Fura-2AM in normal tyrode solution for 40 min, washed and kept aside for 20 min. Fura2-loaded cells were excited alternately at 340 and 380 nm and fluorescence at 510 nm was expressed as 340/380 ratio. Intracellular Ca2+ stores were depleted with 30 μM BHQ which promotes store-operated Ca2+ entry into the cells upon addition of 1 mM extracellular Ca2+. Preincubation of cells with 50 μM 2-APB for 10 min reduces this Ca2+ entry.
We used 2-APB to determine whether IP3R involved in the related calcium signaling
2-APB (50uM) was applied to mouse brain slices while measuring evoked dopamine release.