RO4491533
Overview
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.[1]
Chemistry
- Formula
- C24H20F3N3O PC
- CAS number
- 579482-31-8 PC
- Molar mass (g/mol)
- 423.4 PC
- IUPAC name (computed by PubChem)
- 4-
[3- PC(2, 6- dimethyl- 4- pyridinyl) phenyl] - 7- methyl- 8- (trifluoromethyl) - 1, 3- dihydro- 1, 5- benzodiazepin- 2- one - SMILES
- CC1=CC2=C(C=C1C(F)
(F) PCF) NC(=O) CC(=N2) C3=CC=CC(=C3) C4=CC(=NC(=C4) C) C - InChIKey
- LYTVXCQQTLUEQR-
UHFFFAOYSA- PCN - PubChem CID
- 11158623
Harm reduction information
No harm reduction data is on file for this compound yet. That means no dose, timing or combination data from PsychonautWiki or TripSit. Please don't guess a dose from similar compounds. If you have taken it and feel unwell, contact emergency services or a poison control center.
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Sources
- Journal / agency 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. December 2011. doi:10.3109/01677063.2011.627485 · PMID 22091727
- Journal / agency 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. The Journal of Pharmacology and Experimental Therapeutics. July 2007. doi:10.1124/jpet.106.117093 · PMID 17416742
Text and values on this page are quoted from Wikipedia (CC BY-SA 4.0), PubChem (public domain). Each value links to the exact revision it came from.