Drug Information
| Drug General Information | |||||
|---|---|---|---|---|---|
| Drug ID |
D00HCI
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| Former ID |
DIB018541
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| Drug Name |
2-APB
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| Synonyms |
2-APB; 2-aminoethoxydiphenyl borate; 2-aminoethoxydiphenylborane
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| Drug Type |
Small molecular drug
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| Indication | Discovery agent | Investigative | [1] | ||
| Structure |
|
Download2D MOL |
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| Formula |
C14H16BNO
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| InChI |
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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| 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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| Target and Pathway | |||||
| Target(s) | Short transient receptor potential channel 1 | Target Info | Blocker (channel blocker) | [2] | |
| Vanilloid receptor 1 | Target Info | Activator | [3] | ||
| Short transient receptor potential channel 6 | Target Info | Blocker (channel blocker) | [4] | ||
| TRP cation channel C5 | Target Info | Blocker (channel blocker) | [5] | ||
| TRPV2 | Target Info | Activator | [6] | ||
| Short transient receptor potential channel 3 | Target Info | Blocker (channel blocker) | [7] | ||
| TRPM6 | Target Info | Activator | [8] | ||
| Long transient receptor potential channel 2 | Target Info | Blocker (channel blocker) | [9] | ||
| Transient receptor potential channel 6, subfamily V | Target Info | Activator | [10] | ||
| Transient receptor potential cation channel subfamily V member 3 | Target Info | Activator | [11] | ||
| TRPM3 | Target Info | Inhibitor (gating inhibitor) | [5] | ||
| TRPM8 protein | Target Info | Blocker (channel blocker) | [12] | ||
| TRPC2 | Target Info | Blocker (channel blocker) | [13] | ||
| TRPC7 | Target Info | Blocker (channel blocker) | [14] | ||
| TRPM7 | Target Info | Activator | [15] | ||
| TRPC4 | Target Info | Blocker (channel blocker) | [16] | ||
| BioCyc Pathway | Eumelanin biosynthesis | ||||
| KEGG Pathway | Neuroactive ligand-receptor interaction | ||||
| Inflammatory mediator regulation of TRP channelshsa04970:Salivary secretion | |||||
| Mineral absorptionhsa04750:Inflammatory mediator regulation of TRP channelshsa04750:Inflammatory mediator regulation of TRP channels | |||||
| NetPath Pathway | IL2 Signaling PathwayNetPath_14:IL2 Signaling Pathway | ||||
| PANTHER Pathway | Alzheimer disease-presenilin pathwayP00004:Alzheimer disease-presenilin pathwayP00004:Alzheimer disease-presenilin pathway | ||||
| Pathway Interaction Database | Trk receptor signaling mediated by the MAPK pathway | ||||
| Trk receptor signaling mediated by PI3K and PLC-gammaendothelinpathway:Endothelins | |||||
| Nephrin/Neph1 signaling in the kidney podocyte | |||||
| EPO signaling pathway | |||||
| PAR1-mediated thrombin signaling eventspi3kplctrkpathway:Trk receptor signaling mediated by PI3K and PLC-gammatcr_pathway: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 messengersR-HSA-3295583:TRP channelsR-HSA-114508:Effects of PIP2 hydrolysis | |||||
| Role of second messengers in netrin-1 signalingR-HSA-3295583:TRP channels | |||||
| Role of second messengers in netrin-1 signalingR-HSA-114508:Effects of PIP2 hydrolysis | |||||
| Role of second messengers in netrin-1 signalingR-HSA-3295583:TRP channelsR-HSA-3295583:TRP channelsR-HSA-3295583:TRP channelsR-HSA-3295583:TRP channels | |||||
| WikiPathways | Signaling by the B Cell Receptor (BCR) | ||||
| Netrin-1 signalingWP2572:Primary Focal Segmental Glomerulosclerosis FSGS | |||||
| Platelet homeostasis | |||||
| Netrin-1 signaling | |||||
| GPCR downstream signaling | |||||
| Effects of PIP2 hydrolysisWP1868:Netrin-1 signalingWP1885:Platelet homeostasis | |||||
| Effects of PIP2 hydrolysisWP2877:Vitamin D Receptor Pathway | |||||
| miR-targeted genes in lymphocytes - TarBase | |||||
| References | |||||
| REF 1 | (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 | TRPC1 and TRPC5 form a novel cation channel in mammalian brain. Neuron. 2001 Mar;29(3):645-55. | ||||
| REF 3 | 2-aminoethoxydiphenyl borate is a common activator of TRPV1, TRPV2, and TRPV3. J Biol Chem. 2004 Aug 20;279(34):35741-8. Epub 2004 Jun 11. | ||||
| REF 4 | (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 5 | 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 6 | Pharmacological characterization and molecular determinants of the activation of transient receptor potential V2 channel orthologs by 2-aminoethoxydiphenyl borate. Mol Pharmacol. 2007 Nov;72(5):1258-68. Epub 2007 Aug 2. | ||||
| REF 7 | Mechanism of inhibition of TRPC cation channels by 2-aminoethoxydiphenylborane. Mol Pharmacol. 2005 Sep;68(3):758-62. Epub 2005 Jun 2. | ||||
| REF 8 | Functional characterization of homo- and heteromeric channel kinases TRPM6 and TRPM7. J Gen Physiol. 2006 May;127(5):525-37. | ||||
| REF 9 | 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 10 | (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). | ||||
| REF 11 | 2-aminoethoxydiphenyl borate activates and sensitizes the heat-gated ion channel TRPV3. J Neurosci. 2004 Jun 2;24(22):5177-82. | ||||
| REF 12 | 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 13 | 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 14 | (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 15 | LTRPC7 is a Mg.ATP-regulated divalent cation channel required for cell viability. Nature. 2001 May 31;411(6837):590-5. | ||||
| REF 16 | (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). | ||||
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