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GRN-529

From Wikipedia, the free encyclopedia
Chemical compound
Pharmaceutical compound
GRN-529
Identifiers
  • (4-(Difluoromethoxy)-3-(pyridin-2-ylethynyl)phenyl)(5H-pyrrolo[3,4-b]pyridin-6(7H)-yl)methanone
CAS Number
PubChemCID
IUPHAR/BPS
ChemSpider
UNII
CompTox Dashboard(EPA)
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

GRN-529 is a drug that was developed byWyeth as anegative allosteric modulator of themetabotropic glutamate receptor 5 (mGluR5).[1]

A study conducted byPfizer 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 inanimal models of depression. It is theorized to work by reducing glutamate receptor hyperactivity.[3]

See also

[edit]

References

[edit]
  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.

External links

[edit]
  • "GRN-529".Adis Insight. Springer Nature Switzerland AG.
Group I
mGluR1Tooltip Metabotropic glutamate receptor 1
mGluR5Tooltip Metabotropic glutamate receptor 5
Group II
mGluR2Tooltip Metabotropic glutamate receptor 2
mGluR3Tooltip Metabotropic glutamate receptor 3
Group III
mGluR4Tooltip Metabotropic glutamate receptor 4
mGluR6Tooltip Metabotropic glutamate receptor 6
mGluR7Tooltip Metabotropic glutamate receptor 7
mGluR8Tooltip Metabotropic glutamate receptor 8
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