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VU-0238429

From Wikipedia, the free encyclopedia
Chemical compound
Pharmaceutical compound
VU-0238429
Identifiers
  • 1-(4-methoxybenzyl)-5-(trifluoromethoxy)indole-2,3-dione
CAS Number
PubChemCID
ChemSpider
UNII
ChEMBL
CompTox Dashboard(EPA)
Chemical and physical data
FormulaC17H12F3NO4
Molar mass351.281 g·mol−1
3D model (JSmol)
  • c2cc(OC)ccc2CN(C(=O)C1=O)c3ccc(cc13)OC(F)(F)F

  • COc1ccc(cc1)CN2c3ccc(cc3C(=O)C2=O)OC(F)(F)F
  • InChI=1S/C17H12F3NO4/c1-24-11-4-2-10(3-5-11)9-21-14-7-6-12(25-17(18,19)20)8-13(14)15(22)16(21)23/h2-8H,9H2,1H3 checkY
  • Key:CKLGZXFOLMHCMC-UHFFFAOYSA-N checkY
  (verify)

VU-0238429 is a drug which acts as a selectivepositive allosteric modulator for themuscarinic acetylcholine receptor M5. It was the first selective ligand developed for the M5 subtype,[1] and is structurally derived from olderM1-selective positive allosteric modulators such asVU-0119498.[2][3] Replacing theO-methyl- by aphenyl group further improves the receptor subtype selectivity.[4]

References

[edit]
  1. ^Bridges TM, Marlo JE, Niswender CM, Jones CK, Jadhav SB, Gentry PR, et al. (June 2009)."Discovery of the first highly M5-preferring muscarinic acetylcholine receptor ligand, an M5 positive allosteric modulator derived from a series of 5-trifluoromethoxy N-benzyl isatins".Journal of Medicinal Chemistry.52 (11):3445–3448.doi:10.1021/jm900286j.PMC 3875304.PMID 19438238.
  2. ^Conn PJ, Jones CK, Lindsley CW (March 2009)."Subtype-selective allosteric modulators of muscarinic receptors for the treatment of CNS disorders".Trends in Pharmacological Sciences.30 (3):148–155.doi:10.1016/j.tips.2008.12.002.PMC 2907736.PMID 19201489.
  3. ^Bridges TM, Kennedy JP, Hopkins CR, Conn PJ, Lindsley CW (October 2010)."Heterobiaryl and heterobiaryl ether derived M5 positive allosteric modulators".Bioorganic & Medicinal Chemistry Letters.20 (19):5617–5622.doi:10.1016/j.bmcl.2010.08.042.PMC 3179183.PMID 20801651.
  4. ^Bridges TM, Phillip Kennedy J, Noetzel MJ, Breininger ML, Gentry PR, Conn PJ, Lindsley CW (March 2010)."Chemical lead optimization of a pan Gq mAChR M1, M3, M5 positive allosteric modulator (PAM) lead. Part II: development of a potent and highly selective M1 PAM".Bioorganic & Medicinal Chemistry Letters.20 (6):1972–1975.doi:10.1016/j.bmcl.2010.01.109.PMC 2834874.PMID 20156687.
mAChRsTooltip Muscarinic acetylcholine receptors
Agonists
Antagonists
Precursors
(andprodrugs)
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