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2-Aminoethoxydiphenyl borate

Diphenylborinic acid 2-aminoethyl ester 2-Aminoethyl diphenylborinate

2-Aminoethoxydiphenyl borate (2-APB) is a chemical that acts to inhibit both IP3 receptors and TRP channels (although it activates TRPV1, TRPV2, & TRPV3 at higher concentrations). In research it is used to manipulate intracellular release of calcium ions (Ca2+) and modify TRP channel activity, although the 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 made of connexin. Increasing evidence showed that 2-APB is a powerful modifier of store-operated calcium channels (SOC) function, low concentration of 2-APB can enhance SOC while high concentration induces a transient increase followed by complete inhibition.

References

References

  1. (2001-11-01). "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.
  2. (2005-06-01). "Block of TRPC5 channels by 2-aminoethoxydiphenyl borate: a differential, extracellular and voltage-dependent effect". British Journal of Pharmacology.
  3. (2002-08-01). "2-aminoethoxydiphenyl borate (2-APB) is a reliable blocker of store-operated Ca2+ entry but an inconsistent inhibitor of InsP3-induced Ca2+ release". FASEB Journal.
  4. (2006-12-01). "Block of specific gap junction channel subtypes by 2-aminoethoxydiphenyl borate (2-APB)". The Journal of Pharmacology and Experimental Therapeutics.
  5. Ma HT, et al. (2000) Requirement of the inositol trisphosphate receptor for activation of store-operated Ca2+ channels. Science 287:1647–1651.
  6. Prakriya M, Lewis RS (2001) Potentiation and inhibition of Ca2+ release-activated Ca2+ channels by 2-aminoethyldiphenyl borate (2-APB) occurs independently of IP 3 receptors. J Physiol 536:3–19.
  7. Ma HT, Venkatachalam K, Parys JB, Gill DL (2002) Modification of store-operated channel coupling and inositol trisphosphate receptor function by 2-aminoethoxydiphenyl borate in DT40 lymphocytes. J Biol Chem 277:6915–6922.
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organoboron-compounds phenyl-compounds aminoethyl-compounds
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