Drug Information

Drug General Information
Drug ID
D00HCI
Former ID
DIB018541
Drug Name
2-APB
Synonyms
2-APB; 2-aminoethoxydiphenyl borate; 2-aminoethoxydiphenylborane
Drug Type
Small molecular drug
Indication Discovery agent Investigative [539562]
Formula
C14H16BNO
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
InChIKey
BLZVCIGGICSWIG-UHFFFAOYSA-N
PubChem Compound ID
1598
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
Target and Pathway
Target(s) Short transient receptor potential channel 1 Target Info Blocker (channel blocker) [526026]
Vanilloid receptor 1 Target Info Activator [527108]
Short transient receptor potential channel 6 Target Info Blocker (channel blocker) [543855]
TRP cation channel C5 Target Info Blocker (channel blocker) [527498]
TRPV2 Target Info Activator [528975]
Short transient receptor potential channel 3 Target Info Blocker (channel blocker) [527578]
TRPM6 Target Info Activator [528155]
Long transient receptor potential channel 2 Target Info Blocker (channel blocker) [529260]
Transient receptor potential channel 6, subfamily V Target Info Activator [543864]
Transient receptor potential cation channel subfamily V member 3 Target Info Activator [527098]
TRPM3 Target Info Inhibitor (gating inhibitor) [527498]
TRPM8 protein Target Info Blocker (channel blocker) [531642]
TRPC2 Target Info Blocker (channel blocker) [526896]
TRPC7 Target Info Blocker (channel blocker) [543856]
TRPM7 Target Info Activator [526076]
TRPC4 Target Info Blocker (channel blocker) [543853]
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 na&#xef
Signaling events mediated by PTP1B
TCR signaling in na&#xef
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 539562(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 526026TRPC1 and TRPC5 form a novel cation channel in mammalian brain. Neuron. 2001 Mar;29(3):645-55.
Ref 526076LTRPC7 is a Mg.ATP-regulated divalent cation channel required for cell viability. Nature. 2001 May 31;411(6837):590-5.
Ref 526896A 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 5270982-aminoethoxydiphenyl borate activates and sensitizes the heat-gated ion channel TRPV3. J Neurosci. 2004 Jun 2;24(22):5177-82.
Ref 5271082-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 527498Block of TRPC5 channels by 2-aminoethoxydiphenyl borate: a differential, extracellular and voltage-dependent effect. Br J Pharmacol. 2005 Jun;145(4):405-14.
Ref 527578Mechanism of inhibition of TRPC cation channels by 2-aminoethoxydiphenylborane. Mol Pharmacol. 2005 Sep;68(3):758-62. Epub 2005 Jun 2.
Ref 528155Functional characterization of homo- and heteromeric channel kinases TRPM6 and TRPM7. J Gen Physiol. 2006 May;127(5):525-37.
Ref 528975Pharmacological 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 529260Inhibition of the transient receptor potential cation channel TRPM2 by 2-aminoethoxydiphenyl borate (2-APB). Br J Pharmacol. 2008 Mar;153(6):1324-30.
Ref 531642Effects 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 543853(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 543855(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 543856(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 543864(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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