| Article ID | Journal | Published Year | Pages | File Type |
|---|---|---|---|---|
| 10594416 | Bioorganic & Medicinal Chemistry Letters | 2012 | 4 Pages |
Abstract
High throughput screening identified the pyridothienopyrimidinone 1 as a ligand for the metabotropic glutamate receptor 1 (mGluR1Â =Â 10Â nM). Compound 1 has an excellent in vivo profile; however, it displays unfavorable pharmacokinetic issues and metabolic stability. Therefore, using 1 as a template, novel analogues (10i) were prepared. These analogues displayed improved oral exposure and activity in the Spinal Nerve Ligation (SNL) pain model.
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Authors
Stephanie Brumfield, Peter Korakas, Lisa S. Silverman, Deen Tulshian, Julius J. Matasi, Li Qiang, Chad E. Bennett, Duane A. Burnett, William J. Greenlee, Chad E. Knutson, Wen-Lian Wu, T.K. Sasikumar, Martin Domalski, Rosalia Bertorelli,