GRN-529

GRN-529 is a drug that was developed by Wyeth as a negative allosteric modulator of the metabotropic glutamate receptor 5 (mGluR5).[1]

GRN-529
Identifiers
  • (4-(Difluoromethoxy)-3-(pyridin-2-ylethynyl)phenyl)(5H-pyrrolo[3,4-b]pyridin-6(7H)-yl)methanone
CAS Number
PubChem CID
IUPHAR/BPS
ChemSpider
UNII
Chemical and physical data
FormulaC22H15F2N3O2
Molar mass391.378 g·mol−1
3D model (JSmol)
  • O=C(N1CC(C=CC=N2)=C2C1)C3=CC(C#CC4=CC=CC=N4)=C(OC(F)F)C=C3
  • InChI=1S/C22H15F2N3O2/c23-22(24)29-20-9-7-16(12-15(20)6-8-18-5-1-2-10-25-18)21(28)27-13-17-4-3-11-26-19(17)14-27/h1-5,7,9-12,22H,13-14H2
  • Key:JITMSIRHBAVREW-UHFFFAOYSA-N

A study conducted by Pfizer found that GRN-529 reduced repetitive behaviors without sedation and partially increased sociability in mouse models of autism. [2]

Another study conducted by Pfizer found a therapeutically relevant effect in animal models of depression. It is theorized to work by reducing glutamate receptor hyperactivity.[3]

See also

References
  1. US 2010273772, O'Neil SV, Zegarelli BJ, Springer DM, Li DZ, "Bisaryl Alkynylamides as Negative Allosteric Modulators of Metabotropic Glutamate Receptor 5 (MGLUR5)", published 28 October 2010, assigned to Wyeth
  2. Silverman JL, Smith DG, Rizzo SJ, Karras MN, Turner SM, Tolu SS, et al. (April 2012). "Negative allosteric modulation of the mGluR5 receptor reduces repetitive behaviors and rescues social deficits in mouse models of autism". Science Translational Medicine. 4 (131): 131ra51. doi:10.1126/scitranslmed.3003501. PMC 4904784. PMID 22539775.
  3. Hughes ZA, Neal SJ, Smith DL, Sukoff Rizzo SJ, Pulicicchio CM, Lotarski S, et al. (March 2013). "Negative allosteric modulation of metabotropic glutamate receptor 5 results in broad spectrum activity relevant to treatment resistant depression". Neuropharmacology. 66: 202–14. doi:10.1016/j.neuropharm.2012.04.007. PMID 22551786. S2CID 26417328.
  • "GRN-529". Adis Insight. Springer Nature Switzerland AG.
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