Chemistry:GRN-529

From HandWiki
Short description: Chemical compound
GRN-529
Identifiers
CAS Number
PubChem CID
IUPHAR/BPS
ChemSpider
UNII
Chemical and physical data
FormulaC22H15F2N3O2
Molar mass391.378 g·mol−1
3D model (JSmol)

GRN-529 is a 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. ↑ O'Neil SV, Zegarelli BJ, Springer DM, Li DZ, "Bisaryl Alkynylamides as Negative Allosteric Modulators of Metabotropic Glutamate Receptor 5 (MGLUR5)", US patent 2010273772, published 28 October 2010, assigned to Wyeth
  2. ↑ "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. April 2012. doi:10.1126/scitranslmed.3003501. PMID 22539775. 
  3. ↑ "Negative allosteric modulation of metabotropic glutamate receptor 5 results in broad spectrum activity relevant to treatment resistant depression". Neuropharmacology 66: 202–14. March 2013. doi:10.1016/j.neuropharm.2012.04.007. PMID 22551786.