AR420626

AR420626
Identifiers
  • N-(2,5-dichlorophenyl)-4-(furan-2-yl)-2-methyl-5-oxo-4,6,7,8-tetrahydro-1H-quinoline-3-carboxamide
CAS Number
PubChem CID
ChemSpider
ChEMBL
Chemical and physical data
FormulaC21H18Cl2N2O3
Molar mass417.29 g·mol−1
3D model (JSmol)
  • CC1=C(C(C2=C(N1)CCCC2=O)C3=CC=CO3)C(=O)NC4=C(C=CC(=C4)Cl)Cl
  • InChI=1S/C21H18Cl2N2O3/c1-11-18(21(27)25-15-10-12(22)7-8-13(15)23)20(17-6-3-9-28-17)19-14(24-11)4-2-5-16(19)26/h3,6-10,20,24H,2,4-5H2,1H3,(H,25,27)
  • Key:GGTYQECCGLBHGS-UHFFFAOYSA-N

AR420626 is an experimental drug which acts as a reasonably potent and highly selective agonist for the free fatty acid receptor FFAR3 (GPR41).[1][2] It has been used to research the role of FFAR3 in various disease processes such as diabetes,[3] asthma,[4] eczema[4] and some forms of cancer,[5] as well as regulation of gastrointestinal hormone release.[6]

Further reading

  • Said H, Akiba Y, Narimatsu K, Maruta K, Kuri A, Iwamoto KI, et al. (August 2017). "FFA3 Activation Stimulates Duodenal Bicarbonate Secretion and Prevents NSAID-Induced Enteropathy via the GLP-2 Pathway in Rats". Digestive Diseases and Sciences. 62 (8): 1944–1952. doi:10.1007/s10620-017-4600-4. PMC 5511769. PMID 28523577.
  • Yoshioka Y, Tachibana Y, Uesaka T, Hioki H, Sato Y, Fukumoto T, et al. (June 2022). "Uts2b is a microbiota-regulated gene expressed in vagal afferent neurons connected to enteroendocrine cells producing cholecystokinin". Biochemical and Biophysical Research Communications. 608: 66–72. Bibcode:2022BBRC..608...66Y. doi:10.1016/j.bbrc.2022.03.117. hdl:20.500.14094/90009216. PMID 35390674.

References

  1. ^ Hudson BD, Christiansen E, Murdoch H, Jenkins L, Hansen AH, Madsen O, et al. (August 2014). "Complex pharmacology of novel allosteric free fatty acid 3 receptor ligands". Molecular Pharmacology. 86 (2): 200–210. doi:10.1124/mol.114.093294. PMID 24870406.
  2. ^ Ulven ER, Quon T, Sergeev E, Barki N, Brvar M, Hudson BD, et al. (April 2020). "Structure-Activity Relationship Studies of Tetrahydroquinolone Free Fatty Acid Receptor 3 Modulators". Journal of Medicinal Chemistry. 63 (7): 3577–3595. doi:10.1021/acs.jmedchem.9b02036. PMC 7307922. PMID 32141297.
  3. ^ Lee DH, Heo KS, Myung CS (July 2023). "Gαi -coupled GPR41 activation increases Ca2+ influx in C2C12 cells and shows a therapeutic effect in diabetic animals". Obesity. 31 (7). Silver Spring, Md.: 1871–1883. doi:10.1002/oby.23786. PMID 37309717.
  4. ^ a b Lee YJ, Son SE, Im DS (January 2024). "Free fatty acid 3 receptor agonist AR420626 reduces allergic responses in asthma and eczema in mice". International Immunopharmacology. 127 111428. doi:10.1016/j.intimp.2023.111428. PMID 38159551.
  5. ^ Mikami D, Kobayashi M, Uwada J, Yazawa T, Kamiyama K, Nishimori K, et al. (2020). "AR420626, a selective agonist of GPR41/FFA3, suppresses growth of hepatocellular carcinoma cells by inducing apoptosis via HDAC inhibition". Therapeutic Advances in Medical Oncology. 12: 1758835920913432. doi:10.1177/1758835920913432. PMC 7517987. PMID 33014144.
  6. ^ Kaji I, Akiba Y, Furuyama T, Adelson DW, Iwamoto K, Watanabe M, et al. (January 2018). "Free fatty acid receptor 3 activation suppresses neurogenic motility in rat proximal colon". Neurogastroenterology and Motility. 30 (1). doi:10.1111/nmo.13157. PMC 5739952. PMID 28714277.
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