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RO4491533
Clinical data
ATC code	None;
Legal status
Legal status	In general: non-regulated;
Identifiers
	IUPAC name 4-[3-(2,6-dimethylpyridin-4-yl)phenyl]-7-methyl-8-trifluoromethyl-1,3-dihydrobenzo[b][1,4]diazepin-2-one;
CAS Number	579482-31-8 ;
PubChem CID	11158623;
IUPHAR/BPS	6226;
ChemSpider	9333726;
UNII	HF59BT62UG;
CompTox Dashboard (EPA)	DTXSID601030327 ;
Chemical and physical data
Formula	C24H20F3N3O
Molar mass	423.439 g·mol−1
3D model (JSmol)	Interactive image;
	SMILES n3c(C)cc(cc3C)-c(ccc4)cc4C(=Nc1cc2C)CC(=O)Nc1cc2C(F)(F)F;
	InChI 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 (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]

References

^ 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.