RO4491533

In this article, we will explore and analyze in depth RO4491533, a topic that has captured the attention of people from different backgrounds and interests. With the intention of providing a complete and enlightening vision, we will address different aspects related to RO4491533, from its origin and evolution to its impact on current society. Through a multidisciplinary approach, we will examine its relevance in various contexts and how it has shaped the way we perceive and understand the world around us. Likewise, we will give a voice to experts and protagonists in the field, whose experiences and knowledge will enrich the understanding of RO4491533 and its meaning today.

RO4491533
Clinical data
ATC code
  • None
Legal status
Legal status
  • In general: non-regulated
Identifiers
  • 4--7-methyl-8-trifluoromethyl-1,3-dihydrobenzodiazepin-2-one
CAS Number
PubChem CID
IUPHAR/BPS
ChemSpider
UNII
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. A number of related compounds are known, with similar effects in vitro and a fairly well characterized structure-activity relationship.

See also

References

  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.
  2. ^ 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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