RO4491533
Chemical compound
- None
- In general: non-regulated
- 4-[3-(2,6-dimethylpyridin-4-yl)phenyl]-7-methyl-8-trifluoromethyl-1,3-dihydrobenzo[b][1,4]diazepin-2-one
- 579482-31-8
Y
- 11158623
- 6226
- 9333726
- HF59BT62UG
- Interactive image
- 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 (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]
See also
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.
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| mGluR1Tooltip Metabotropic glutamate receptor 1 |
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| mGluR5Tooltip Metabotropic glutamate receptor 5 |
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| mGluR2Tooltip Metabotropic glutamate receptor 2 |
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| mGluR3Tooltip Metabotropic glutamate receptor 3 |
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| mGluR4Tooltip Metabotropic glutamate receptor 4 |
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| mGluR6Tooltip Metabotropic glutamate receptor 6 |
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| mGluR7Tooltip Metabotropic glutamate receptor 7 | |
| mGluR8Tooltip Metabotropic glutamate receptor 8 |
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See also: Receptor/signaling modulators • Ionotropic glutamate receptor modulators • Glutamate metabolism/transport modulators
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