RO4491533

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RO4491533
RO4491533 structure.png
Systematic (IUPAC) name
4-[3-(2,6-dimethylpyridin-4-yl)phenyl]-7-methyl-8-trifluoromethyl-1,3-dihydrobenzo[b][1,4]diazepin-2-one
Clinical data
Legal status Non-regulated
Identifiers
CAS number 579482-31-8
ATC code None
PubChem CID 11158623
Chemical data
Formula C24H20F3N3O 
Mol. mass 423.430 g/mol

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]

References[edit]

  1. ^ Campo B, Kalinichev M, Lambeng N, El Yacoubi M, Royer-Urios I, Schneider M, Legrand C, Parron D, Girard F, Bessif A, Poli S, Vaugeois JM, Le Poul E, Celanire S. Characterization of an mGluR2/3 negative allosteric modulator in rodent models of depression. Journal of Neurogenetics. 2011 Dec;25(4):152-66. PMID 22091727
  2. ^ Hemstapat K, Da Costa H, Nong Y, Brady AE, Luo Q, Niswender CM, Tamagnan GD, Conn PJ. A novel family of potent negative allosteric modulators of group II metabotropic glutamate receptors. Journal of Pharmacology and Experimental Therapeutics. 2007 Jul;322(1):254-64. PMID 17416742