GRN-529

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GRN-529
GRN-529.svg
Identifiers
CAS Number
IUPHAR/BPS
ChemSpider
Chemical and physical data
Formula C22H15F2N3O2
Molar mass 391.11 g/mol
3D model (Jmol)

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

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[edit]

References[edit]

  1. ^ US Patent Application No. 20100273772 "96 dpi image of original application USPTO 2010273772" (PDF). Retrieved 26 May 2012. 
  2. ^ Silverman, J. L.; Smith, D. G.; Rizzo, S. J. S.; Karras, M. N.; Turner, S. M.; Tolu, S. S.; Bryce, D. K.; Smith, D. L.; et al. (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. PMID 22539775. 
  3. ^ Hughes, ZA; Neal, SJ; Smith, DL; Sukoff Rizzo, SJ; Pulicicchio, CM; Lotarski, S; Lu, S; Dwyer, JM; Brennan, J; Olsen, M.; Bender, C.N.; Kouranova, E.; Andree, T.H.; Harrison, J.E.; Whiteside, G.T.; Springer, D.; O'Neil, S.V.; Leonard, S.K.; Schechter, L.E.; Dunlop, J.; Rosenzweig-Lipson, S.; Ring, R.H. (2012). "Negative allosteric modulation of metabolic glutamate receptor 5 results in broad spectrum activity relevant to treatment resistant depression". Neuropharmacology. 66: 202. doi:10.1016/j.neuropharm.2012.04.007. PMID 22551786.