RO4491533

RO4491533

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
IUPHAR/BPS	6226
Chemical data
Formula	C24H20F3N3O
Molar mass	423.430 g/mol
SMILES n3c(C)cc(cc3C)-c(ccc4)cc4C(=Nc1cc2C)CC(=O)Nc1cc2C(F)(F)F

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 (mGluR_2/3), 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 mGluR_2/3 agonist LY-379,268 with similar efficacy but slightly lower potency than the mGluR_2/3 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

• Decoglurant

References

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