902747-04-0Relevant articles and documents
Synthesis and SAR development of novel mGluR1 antagonists for the treatment of chronic pain
Brumfield, Stephanie,Korakas, Peter,Silverman, Lisa S.,Tulshian, Deen,Matasi, Julius J.,Qiang, Li,Bennett, Chad E.,Burnett, Duane A.,Greenlee, William J.,Knutson, Chad E.,Wu, Wen-Lian,Sasikumar, T. K.,Domalski, Martin,Li, Cheng,Bertorelli, Rosalia,Grilli, Mariagrazia,Lozza, Gianluca,Reggiani, Angelo
, p. 7223 - 7226,4 (2012/12/12)
High throughput screening identified the pyridothienopyrimidinone 1 as a ligand for the metabotropic glutamate receptor 1 (mGluR1 = 10 nM). Compound 1 has an excellent in vivo profile; however, it displays unfavorable pharmacokinetic issues and metabolic