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]
Structure
Download
2D MOL
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
PubChem Substance ID
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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