The DOI matches its Crossref record; 26 of the 26 references it cites were found in a registry or an index.
2-Aminoethoxydiphenyl borate (2-APB) antagonises inositol 1,4,5-trisphosphate-induced calcium release, inhibits calcium pumps and has a use-dependent and slowly reversible action on store-operated calcium entry channels
Open accessAbstract
The action of 2-aminoethoxydiphenyl borate (2-APB) on Ca(2+) signalling in HeLa cells and cardiac myocytes was investigated. Consistent with other studies, we found that superfusion of cells with 2-APB rapidly inhibited inositol 1,4,5-trisphosphate (InsP(3))-mediated Ca(2+) release and store-operated Ca(2+) entry (SOC). In addition to abrogating hormone-evoked Ca(2+) responses, 2-APB could antagonise Ca(2+) signals evoked by a membrane permeant InsP(3) ester. 2-APB also slowed the recovery of intracellular Ca(2+) signals consistent with an effect on Ca(2+) ATPases. The inhibitory action of 2-APB on InsP(3) receptors (InsP(3)Rs), SOC channels and Ca(2+) pumps persisted for several minutes after washout of the compound. Application of 2-APB to unstimulated cells had no effect on subsequent Ca(2+) responses suggesting that it has a use-dependent action. Mitochondria in cells treated with 2-APB showed a rapid and slowly reversible swelling. 2-APB did not cause the mitochondria to depolarise, but it reduced the extent of mitochondrial calcium uptake. Although 2-APB has been demonstrated not to affect voltage-operated Ca(2+) channels or ryanodine receptors, we found that it gave a concentration-dependent long-lasting inhibition of Ca(2+) signalling in electrically-stimulated cardiac myocytes, where InsP(3)Rs and SOC channels do not play a significant role. Our data suggest that 2-APB has multiple cellular targets, a use-dependent action, is difficult to reverse and may affect Ca(2+) signalling in cell types where InsP(3) and SOC are not active.
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Cites
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Self-citationXestospongins: Potent Membrane Permeable Blockers of the Inositol 1,4,5-Trisphosphate Receptor
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Requirement of the Inositol Trisphosphate Receptor for Activation of Store-Operated Ca 2+ Channels
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Cited by
Physiology and Pathophysiology of the Calcium Store in the Endoplasmic Reticulum of Neurons
Verkhratsky, A. (2005) · Physiological Reviews · doi:10.1152/physrev.00004.2004 · Cited by 709
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Capel, R. A., Bose, S. J., Collins, T. P., Rajasundaram, S., Ayagama, T., Zaccolo, M., Burton, R.-A. B., & Terrar, D. A. (2021) · American Journal of Physiology-Heart and Circulatory Physiology · doi:10.1152/ajpheart.00380.2020 · Cited by 40
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Metadata
- Authors
- Peppiatt, C. M., Collins, T. J., Mackenzie, L., Conway, S. J., Holmes, A. B., Bootman, M. D., Berridge, M. J., Seo, J. T., & Roderick, H. L.
- Venue
- Cell Calcium
- Publisher
- Elsevier BV
- Published
- 2003-07
- Volume
- 34
- Issue
- 1
- Pages
- 97-108
- ISSN
- 0143-4160 (ISSN-L)
- OpenAlex
- W2062061647
- Cited by
- 295
- References
- 26
- FWCI
- 8.97
- Type
- journal article
- Language
- en
- Open access
- green
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- Peppiatt, C. M., Collins, T. J., Mackenzie, L., Conway, S. J., Holmes, A. B., Bootman, M. D., Berridge, M. J., Seo, J. T., & Roderick, H. L. (2003). 2-Aminoethoxydiphenyl borate (2-APB) antagonises inositol 1,4,5-trisphosphate-induced calcium release, inhibits calcium pumps and has a use-dependent and slowly reversible action on store-operated calcium entry channels. Cell Calcium. https://doi.org/10.1016/s0143-4160(03)00026-5
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