Chemistry:GRN-529

From HandWiki
Short description: Chemical compound
GRN-529
GRN-529.svg
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. 

External links