Details of the Drug-Related molecule(s) Expression Atlas

General Information of Drug (ID: DM9AKVR)

Drug Name
2-APB Drug Info
Synonyms 2-aminoethoxydiphenyl borate; 2-aminoethoxydiphenylborane
Indication
Disease Entry ICD 11 Status REF
Discovery agent N.A. Investigative [1]
Cross-matching ID
PubChem CID
1598
ChEBI ID
CHEBI:131184
CAS Number
CAS 524-95-8
TTD Drug ID
DM9AKVR

Molecule(s) Related to This Drug


Drug Therapeutic Target (DTT)
DTT Name DTT ID UniProt ID MOA REF
Long transient receptor potential channel 2 (TRPM2) TTEBMN7 TRPM2_HUMAN Blocker (channel blocker) [2]
Long transient receptor potential channel 3 (TRPM3) TTO3TD8 TRPM3_HUMAN Inhibitor (gating inhibitor) [3]
Long transient receptor potential channel 6 (TRPM6) TTV76RD TRPM6_HUMAN Activator [4]
Long transient receptor potential channel 7 (TRPM7) TTFPVZO TRPM7_HUMAN Activator [5]
Long transient receptor potential channel 8 (TRPM8) TTXDKTO TRPM8_HUMAN Blocker (channel blocker) [6]
Short transient receptor potential channel 1 (TRPC1) TTA76X0 TRPC1_HUMAN Blocker (channel blocker) [7]
Short transient receptor potential channel 2 (TRPC2) TTSJ9E7 Q3C1U7_HUMAN Blocker (channel blocker) [8]
Short transient receptor potential channel 3 (TRPC3) TTNVC34 TRPC3_HUMAN Blocker (channel blocker) [9]
Short transient receptor potential channel 4 (TRPC4) TTX0H5W TRPC4_HUMAN Blocker (channel blocker) [10]
Short transient receptor potential channel 5 (TRPC5) TT32NQ1 TRPC5_HUMAN Blocker (channel blocker) [3]
Short transient receptor potential channel 6 (TRPC6) TTRBT3W TRPC6_HUMAN Blocker (channel blocker) [11]
Short transient receptor potential channel 7 (TRPC7) TT06GRA TRPC7_HUMAN Blocker (channel blocker) [12]
Transient receptor potential cation channel V1 (TRPV1) TTMI6F5 TRPV1_HUMAN Activator [13]
Transient receptor potential cation channel V2 (TRPV2) TTBECWA TRPV2_HUMAN Activator [14]
Transient receptor potential cation channel V3 (TRPV3) TT946IA TRPV3_HUMAN Activator [15]
Transient receptor potential cation channel V6 (TRPV6) TTBK14N TRPV6_HUMAN Activator [16]

The Expression Level of Molecule(s) in Normal Tissue of Major ADME-Related Organs

Molecule Molecule Type Gene Name Liver Colon Kidney Small Intestine
Transient receptor potential cation channel V1 (TRPV1) DTT TRPV1 6.246 5.142 5.626 6.399
Transient receptor potential cation channel V6 (TRPV6) DTT TRPV6 2.536 2.655 1.07 2
Molecule Expression Atlas in Normal Tissue of Major ADME-related organs

The Expression Level of Molecule(s) between Disease Section and Healthy Individual Tissue

The Studied Disease Discovery agent
ICD Disease Classification N.A.
Molecule Name Molecule Type Gene Name p-value Fold-Change Z-score
Transient receptor potential cation channel V3 (TRPV3) DTT TRPV3 7.58E-01 5.28E-03 0.05
Molecular Expression Atlas between Disease Section and Healthy Individual Tissue

References

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).
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.
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.
4 Functional characterization of homo- and heteromeric channel kinases TRPM6 and TRPM7. J Gen Physiol. 2006 May;127(5):525-37.
5 LTRPC7 is a Mg.ATP-regulated divalent cation channel required for cell viability. Nature. 2001 May 31;411(6837):590-5.
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.
7 TRPC1 and TRPC5 form a novel cation channel in mammalian brain. Neuron. 2001 Mar;29(3):645-55.
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.
9 Mechanism of inhibition of TRPC cation channels by 2-aminoethoxydiphenylborane. Mol Pharmacol. 2005 Sep;68(3):758-62.
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).
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).
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).
13 2-aminoethoxydiphenyl borate is a common activator of TRPV1, TRPV2, and TRPV3. J Biol Chem. 2004 Aug 20;279(34):35741-8.
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.
15 2-aminoethoxydiphenyl borate activates and sensitizes the heat-gated ion channel TRPV3. J Neurosci. 2004 Jun 2;24(22):5177-82.
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).