2-APB

Ligand id: 2433

Name: 2-APB

Structure and Physico-chemical Properties

2D Structure
Calculated Physico-chemical Properties
Hydrogen bond acceptors 2
Hydrogen bond donors 1
Rotatable bonds 5
Topological polar surface area 35.25
Molecular weight 225.13
XLogP 4.46
No. Lipinski's rules broken 0

Molecular properties generated using the CDK

References
1. Chung MK, Lee H, Mizuno A, Suzuki M, Caterina MJ. (2004)
2-aminoethoxydiphenyl borate activates and sensitizes the heat-gated ion channel TRPV3.
J. Neurosci.24 (22): 5177-82. [PMID:15175387]
2. Hu HZ, Gu Q, Wang C, Colton CK, Tang J, Kinoshita-Kawada M, Lee LY, Wood JD, Zhu MX. (2004)
2-aminoethoxydiphenyl borate is a common activator of TRPV1, TRPV2, and TRPV3.
J. Biol. Chem.279 (34): 35741-8. [PMID:15194687]
3. Juvin V, Penna A, Chemin J, Lin YL, Rassendren FA. (2007)
Pharmacological characterization and molecular determinants of the activation of transient receptor potential V2 channel orthologs by 2-aminoethoxydiphenyl borate.
Mol. Pharmacol.72 (5): 1258-68. [PMID:17673572]
4. Li M, Jiang J, Yue L. (2006)
Functional characterization of homo- and heteromeric channel kinases TRPM6 and TRPM7.
J. Gen. Physiol.127 (5): 525-37. [PMID:16636202]
5. Lievremont JP, Bird GS, Putney JW. (2005)
Mechanism of inhibition of TRPC cation channels by 2-aminoethoxydiphenylborane.
Mol. Pharmacol.68 (3): 758-62. [PMID:15933213]
6. Lucas P, Ukhanov K, Leinders-Zufall T, Zufall F. (2003)
A diacylglycerol-gated cation channel in vomeronasal neuron dendrites is impaired in TRPC2 mutant mice: mechanism of pheromone transduction.
Neuron40 (3): 551-61. [PMID:14642279]
7. Nadler MJ, Hermosura MC, Inabe K, Perraud AL, Zhu Q, Stokes AJ, Kurosaki T, Kinet JP, Penner R, Scharenberg AM, Fleig A. (2001)
LTRPC7 is a Mg.ATP-regulated divalent cation channel required for cell viability.
Nature411 (6837): 590-5. [PMID:11385574]
8. Naziroğlu M, Ozgül C. (2012)
Effects of antagonists and heat on TRPM8 channel currents in dorsal root ganglion neuron activated by nociceptive cold stress and menthol.
Neurochem. Res.37 (2): 314-20. [PMID:21964764]
9. Neeper MP, Liu Y, Hutchinson TL, Wang Y, Flores CM, Qin N. (2007)
Activation properties of heterologously expressed mammalian TRPV2: evidence for species dependence.
J. Biol. Chem.282 (21): 15894-902. [PMID:17395593]
10. Qin N, Neeper MP, Liu Y, Hutchinson TL, Lubin ML, Flores CM. (2008)
TRPV2 is activated by cannabidiol and mediates CGRP release in cultured rat dorsal root ganglion neurons.
J. Neurosci.28 (24): 6231-8. [PMID:18550765]
11. Strübing C, Krapivinsky G, Krapivinsky L, Clapham DE. (2001)
TRPC1 and TRPC5 form a novel cation channel in mammalian brain.
Neuron29 (3): 645-55. [PMID:11301024]
12. Togashi K, Inada H, Tominaga M. (2008)
Inhibition of the transient receptor potential cation channel TRPM2 by 2-aminoethoxydiphenyl borate (2-APB).
Br. J. Pharmacol.153 (6): 1324-30. [PMID:18204483]
13. 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.
Br. J. Pharmacol.145 (4): 405-14. [PMID:15806115]