Drug Information
| Drug General Information | Top | |||
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| Drug ID |
D00HCI
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| Former ID |
DIB018541
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| Drug Name |
2-APB
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| Synonyms |
2-aminoethoxydiphenyl borate; 2-aminoethoxydiphenylborane
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| Drug Type |
Small molecular drug
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| Indication | Discovery agent [ICD-11: N.A.] | Investigative | [1] | |
| Structure |
 |
Download2D MOL
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| Formula |
C14H16BNO
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| Canonical SMILES |
B(C1=CC=CC=C1)(C2=CC=CC=C2)OCCN
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| InChI |
1S/C14H16BNO/c16-11-12-17-15(13-7-3-1-4-8-13)14-9-5-2-6-10-14/h1-10H,11-12,16H2
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| InChIKey |
BLZVCIGGICSWIG-UHFFFAOYSA-N
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| CAS Number |
CAS 524-95-8
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| PubChem Compound ID | ||||
| PubChem Substance ID |
80520, 640123, 3135688, 7359192, 8151194, 11113973, 15121526, 24439922, 24714959, 24866796, 24894325, 26612756, 26612795, 26747159, 26747160, 26758115, 47736594, 48334609, 49894996, 50104769, 52810066, 53790042, 56310701, 56367707, 57320949, 57654145, 87566979, 88835197, 103424618, 104298176, 107952133, 117531776, 118508205, 125538800, 126539182, 127535009, 135025689, 135366660, 135649695, 135727592, 135727788, 137132621, 139663054, 144024979, 160798980, 162022827, 162093686, 162293458, 162757883, 163688713
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| ChEBI ID |
CHEBI:131184
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| Target and Pathway | Top | |||
|---|---|---|---|---|
| Target(s) | Long transient receptor potential channel 2 (TRPM2) | Target Info | Blocker (channel blocker) | [2] |
| Long transient receptor potential channel 3 (TRPM3) | Target Info | Inhibitor (gating inhibitor) | [3] | |
| Long transient receptor potential channel 6 (TRPM6) | Target Info | Activator | [4] | |
| Long transient receptor potential channel 7 (TRPM7) | Target Info | Activator | [5] | |
| Long transient receptor potential channel 8 (TRPM8) | Target Info | Blocker (channel blocker) | [6] | |
| Short transient receptor potential channel 1 (TRPC1) | Target Info | Blocker (channel blocker) | [7] | |
| Short transient receptor potential channel 2 (TRPC2) | Target Info | Blocker (channel blocker) | [8] | |
| Short transient receptor potential channel 3 (TRPC3) | Target Info | Blocker (channel blocker) | [9] | |
| Short transient receptor potential channel 4 (TRPC4) | Target Info | Blocker (channel blocker) | [10] | |
| Short transient receptor potential channel 5 (TRPC5) | Target Info | Blocker (channel blocker) | [3] | |
| Short transient receptor potential channel 6 (TRPC6) | Target Info | Blocker (channel blocker) | [11] | |
| Short transient receptor potential channel 7 (TRPC7) | Target Info | Blocker (channel blocker) | [12] | |
| Transient receptor potential cation channel V1 (TRPV1) | Target Info | Activator | [13] | |
| Transient receptor potential cation channel V2 (TRPV2) | Target Info | Activator | [14] | |
| Transient receptor potential cation channel V3 (TRPV3) | Target Info | Activator | [15] | |
| Transient receptor potential cation channel V6 (TRPV6) | Target Info | Activator | [16] | |
| BioCyc | Eumelanin biosynthesis | |||
| KEGG Pathway | Neuroactive ligand-receptor interaction | |||
| Inflammatory mediator regulation of TRP channels | ||||
| Salivary secretion | ||||
| Mineral absorption | ||||
| NetPath Pathway | IL2 Signaling Pathway | |||
| Panther Pathway | Alzheimer disease-presenilin pathway | |||
| Pathway Interaction Database | Trk receptor signaling mediated by the MAPK pathway | |||
| Trk receptor signaling mediated by PI3K and PLC-gamma | ||||
| Endothelins | ||||
| Nephrin/Neph1 signaling in the kidney podocyte | ||||
| EPO signaling pathway | ||||
| PAR1-mediated thrombin signaling events | ||||
| TCR signaling in naï | ||||
| Signaling events mediated by PTP1B | ||||
| TCR signaling in naï | ||||
| Reactome | TRP channels | |||
| Role of second messengers in netrin-1 signaling | ||||
| Antigen activates B Cell Receptor (BCR) leading to generation of second messengers | ||||
| Effects of PIP2 hydrolysis | ||||
| WikiPathways | Signaling by the B Cell Receptor (BCR) | |||
| Netrin-1 signaling | ||||
| Primary Focal Segmental Glomerulosclerosis FSGS | ||||
| Platelet homeostasis | ||||
| GPCR downstream signaling | ||||
| Effects of PIP2 hydrolysis | ||||
| Vitamin D Receptor Pathway | ||||
| miR-targeted genes in lymphocytes - TarBase | ||||
| References | Top | |||
|---|---|---|---|---|
| REF 1 | URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 2433). | |||
| REF 2 | Inhibition of the transient receptor potential cation channel TRPM2 by 2-aminoethoxydiphenyl borate (2-APB). Br J Pharmacol. 2008 Mar;153(6):1324-30. | |||
| REF 3 | Block of TRPC5 channels by 2-aminoethoxydiphenyl borate: a differential, extracellular and voltage-dependent effect. Br J Pharmacol. 2005 Jun;145(4):405-14. | |||
| REF 4 | Functional characterization of homo- and heteromeric channel kinases TRPM6 and TRPM7. J Gen Physiol. 2006 May;127(5):525-37. | |||
| REF 5 | LTRPC7 is a Mg.ATP-regulated divalent cation channel required for cell viability. Nature. 2001 May 31;411(6837):590-5. | |||
| REF 6 | Effects of antagonists and heat on TRPM8 channel currents in dorsal root ganglion neuron activated by nociceptive cold stress and menthol. Neurochem Res. 2012 Feb;37(2):314-20. | |||
| REF 7 | TRPC1 and TRPC5 form a novel cation channel in mammalian brain. Neuron. 2001 Mar;29(3):645-55. | |||
| REF 8 | A diacylglycerol-gated cation channel in vomeronasal neuron dendrites is impaired in TRPC2 mutant mice: mechanism of pheromone transduction. Neuron. 2003 Oct 30;40(3):551-61. | |||
| REF 9 | Mechanism of inhibition of TRPC cation channels by 2-aminoethoxydiphenylborane. Mol Pharmacol. 2005 Sep;68(3):758-62. | |||
| REF 10 | URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Target id: 489). | |||
| REF 11 | URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Target id: 491). | |||
| REF 12 | URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Target id: 492). | |||
| REF 13 | 2-aminoethoxydiphenyl borate is a common activator of TRPV1, TRPV2, and TRPV3. J Biol Chem. 2004 Aug 20;279(34):35741-8. | |||
| REF 14 | Pharmacological characterization and molecular determinants of the activation of transient receptor potential V2 channel orthologs by 2-aminoethoxy... Mol Pharmacol. 2007 Nov;72(5):1258-68. | |||
| REF 15 | 2-aminoethoxydiphenyl borate activates and sensitizes the heat-gated ion channel TRPV3. J Neurosci. 2004 Jun 2;24(22):5177-82. | |||
| REF 16 | URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Target id: 512). | |||
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