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Grn-529

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Title: Grn-529  
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Subject: A.C.E. mixture, LY-344,545, MMPIP, EGLU, LY-307,452
Collection: Alkynes, Benzamides, Mglu5 Receptor Antagonists, Organofluorides, Wyeth
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Grn-529

GRN-529
Systematic (IUPAC) name
(4-(Difluoromethoxy)-3-(pyridin-2-ylethynyl)phenyl)(5H-pyrrolo[3,4-b]pyridin-6(7H)-yl)methanone
Clinical data
Legal status
?
Identifiers
CAS number
ATC code ?
Chemical data
Formula C22H15F2N3O2 
Mol. mass 391.11 g/mol

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

References

  1. ^ US Patent Application No. 20100273772 "96 dpi image of original application USPTO 2010273772". 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.  
  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.  
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