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Contents

   



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1 See also  




2 References  













RO4491533






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From Wikipedia, the free encyclopedia
  

RO4491533
Clinical data
ATC code
  • None
Legal status
Legal status
  • In general: non-regulated
Identifiers

  • 4-[3-(2,6-dimethylpyridin-4-yl)phenyl]-7-methyl-8-trifluoromethyl-1,3-dihydrobenzo[b][1,4]diazepin-2-one

CAS Number
PubChem CID
IUPHAR/BPS
ChemSpider
UNII
CompTox Dashboard (EPA)
Chemical and physical data
FormulaC24H20F3N3O
Molar mass423.439 g·mol−1
3D model (JSmol)

  • n3c(C)cc(cc3C)-c(ccc4)cc4C(=Nc1cc2C)CC(=O)Nc1cc2C(F)(F)F

  • InChI=1S/C24H20F3N3O/c1-13-7-21-22(11-19(13)24(25,26)27)30-23(31)12-20(29-21)17-6-4-5-16(10-17)18-8-14(2)28-15(3)9-18/h4-11H,12H2,1-3H3,(H,30,31)

  • Key:LYTVXCQQTLUEQR-UHFFFAOYSA-N

RO-4491533 is a drug developed by Hoffmann-La Roche which acts as a potent and selective negative allosteric modulator for group II of the metabotropic glutamate receptors (mGluR2/3), being equipotent at mGluR2 and mGluR3 but without activity at other mGluR subtypes. In animal studies, RO-4491533 produced antidepressant effects and reversed the effects of the mGluR2/3 agonist LY-379,268 with similar efficacy but slightly lower potency than the mGluR2/3 antagonist LY-341,495.[1] A number of related compounds are known, with similar effects in vitro and a fairly well characterized structure-activity relationship.[2]

See also[edit]

References[edit]

  1. ^ Campo B, Kalinichev M, Lambeng N, El Yacoubi M, Royer-Urios I, Schneider M, et al. (December 2011). "Characterization of an mGluR2/3 negative allosteric modulator in rodent models of depression". Journal of Neurogenetics. 25 (4): 152–66. doi:10.3109/01677063.2011.627485. PMID 22091727. S2CID 207440972.
  • ^ Hemstapat K, Da Costa H, Nong Y, Brady AE, Luo Q, Niswender CM, et al. (July 2007). "A novel family of potent negative allosteric modulators of group II metabotropic glutamate receptors". The Journal of Pharmacology and Experimental Therapeutics. 322 (1): 254–64. doi:10.1124/jpet.106.117093. PMID 17416742. S2CID 3820477.
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    • Retrieved from "https://en.wikipedia.org/w/index.php?title=RO4491533&oldid=1188795590"
    Categories: 
    ●Drugs not assigned an ATC code
     ●MGlu2 receptor antagonists
     ●MGlu3 receptor antagonists
     ●Trifluoromethyl compounds
     ●Benzodiazepines
     ●Glutamate receptor negative allosteric modulators
     ●Nervous system drug stubs
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