2-Aminoethoxydiphenyl borate
2-Aminoethoxydiphenyl borate (2-APB) is a chemical that acts to inhibit both IP3 receptors[1] and TRP channels (although it activates TRPV1, TRPV2, & TRPV3 at higher concentrations).[2][3] In research it is used to manipulate intracellular release of calcium ions (Ca2+) and modify TRP channel activity, although there its lack of specific effects make it less than ideal under some circumstances. Additionally, there is evidence that 2-APB acts directly to inhibit gap junctions comprised of connexin26 or connexin32.[4]
Also note that many manufacturers provide descriptions of known pharmacologic activity for their products (i.e. Tocris or Sigma-Aldrich)
References
- ↑ Diver JM, Sage SO, Rosado JA (2001). The inositol trisphosphate receptor antagonist 2-aminoethoxydiphenylborate (2-APB) blocks Ca2+ entry channels in human platelets: cautions for its use in studying Ca2+ influx. Cell Calcium, 30(5), 323-329.
- ↑ Xu SZ, Zeng F, Boulay G, Grimm C, Harteneck C, Beech DJ (2005). Block of TRPC5 channels by 2-aminoethoxydiphenyl borate: a differential, extracellular and voltage-dependent effect. British Journal of Pharmacology, 145(4), 320-328.
- ↑ Bootman, MD, Collins, TJ, Makenzie, L, Roderick, HL, Berridge, MJ, & Peppiatt, CM (2002). 2-Aminoethoxydiphenyl borate (2-APB) is a reliable blocker of store-operated Ca2+ entry but an inconsistent inhibitor of InsP3-induced Ca2+ release. The FASEB Journal, 16(10), 1145-1150.
- ↑ Tao, L, & Harris, AL (2007). 2-aminoethoxydiphenyl borate directly inhibits channels composed of connexin26 and/or connexin32. Molecular Pharmacology, 71(2), 570-579.
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