GRN-529
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| Systematic (IUPAC) name | |
| (4-(Difluoromethoxy)-3-(pyridin-2-ylethynyl)phenyl)(5H-pyrrolo[3,4-b]pyridin-6(7H)-yl)methanone | |
| Clinical data | |
| Pregnancy cat. | ? |
| Legal status | ? |
| Identifiers | |
| CAS number | 1253291-12-1 |
| ATC code | ? |
| Chemical data | |
| Formula | C22H15F2N3O2 |
| Mol. mass | 391.11 g/mol |
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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 [edit]
References [edit]
- ^ US Patent Application No. 20100273772 "96 dpi image of original application USPTO 2010273772". 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 et al. (2012). "Negative allosteric modulation of metabolic glutamate receptor 5 results in broad spectrum activity relevant to treatment resistant depression". Neuropharmacology. doi:10.1016/j.neuropharm.2012.04.007. PMID 22551786.
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