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PMID: 12153982 Published · ppublish English Journal Article Review

2-aminoethoxydiphenyl borate (2-APB) is a reliable blocker of store-operated Ca2+ entry but an inconsistent inhibitor of InsP3-induced Ca2+ release.

Bootman MD, Collins TJ, Mackenzie L, Roderick HL, Berridge MJ, Peppiatt CM

Abstract

Since its introduction to Ca2+ signaling in 1997, 2-aminoethoxydiphenyl borate (2-APB) has been used in many studies to probe for the involvement of inositol 1,4,5-trisphosphate receptors in the generation of Ca2+ signals. Due to reports of some nonspecific actions of 2-APB, and the fact that its principal antagonistic effect is on Ca2+ entry rather than Ca2+ release, this compound may not have the utility first suggested. However, 2-APB has thrown up some interesting results, particularly with respect to store-operated Ca2+ entry in nonexcitable cells. These data indicate that although it must be used with caution, 2-APB can be useful in probing certain aspects of Ca2+ signaling.

MeSH Terms
Animals Boron Compounds/pharmacology Calcium/metabolism Calcium Channel Blockers/pharmacology Calcium Channels/metabolism Calcium Signaling/drug effects Inositol 1,4,5-Trisphosphate/antagonists & inhibitors Inositol 1,4,5-Trisphosphate Receptors Ion Transport/drug effects Macrocyclic Compounds Mice Oxazoles/pharmacology Receptors, Cytoplasmic and Nuclear/metabolism
Chemicals
Boron Compounds Calcium Channel Blockers Calcium Channels Inositol 1,4,5-Trisphosphate Receptors Macrocyclic Compounds Oxazoles Receptors, Cytoplasmic and Nuclear xestospongin A Inositol 1,4,5-Trisphosphate 2-aminoethoxydiphenyl borate Calcium
Authors & Affiliations
6 authors, click to expand affiliations / ORCID
Bootman Martin D
Laboratory of Molecular Signalling, The Babraham Institute, Babraham, Cambridge CB2 4AT, UK. martin.bootman@bbsrc.ac.uk
Collins Tony J
Mackenzie Lauren
Roderick H Llewelyn
Berridge Michael J
Peppiatt Claire M
Article Info
Journal
FASEB journal : official publication of the Federation of American Societies for Experimental Biology
Abbr.
FASEB J
ISSN
1530-6860
Published
2002-08-00
Pages
1145-50
Language
English
Region
United States
NLM ID
8804484
Subset
IM
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