GRN-529

GRN-529
Identifiers
	IUPAC name (4-(Difluoromethoxy)-3-(pyridin-2-ylethynyl)phenyl)(5H-pyrrolo[3,4-b]pyridin-6(7H)-yl)methanone;
CAS Number	1253291-12-1;
IUPHAR/BPS	6428;
ChemSpider	27471591;
Chemical and physical data
Formula	C22H15F2N3O2
Molar mass	391.11 g/mol g·mol−1
3D model (JSmol)	Interactive image;
	SMILES O=C(N1CC(C=CC=N2)=C2C1)C3=CC(C#CC4=CC=CC=N4)=C(OC(F)F)C=C3;
	InChI 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 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]

References

^ US Patent Application No. 20100273772 "96 dpi image of original application USPTO 2010273772" (PDF). Retrieved 26 May 2012.
^ 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.
^ 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.

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[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.

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[2]

[3]

See also

References