Author/Authors :
Anthony B. Pinkerton، نويسنده , , Rowena V. Cube، نويسنده , , John H. Hutchinson، نويسنده , , Joyce K. James، نويسنده , , Michael F. Gardner، نويسنده , , Blake A. Rowe، نويسنده , , Herve Schaffhauser، نويسنده , , Dana E. Rodriguez، نويسنده , , Una C. Campbell، نويسنده , , Lorrie P. Daggett، نويسنده , , Jean-Michel Vernier، نويسنده ,
Abstract :
We have identified and synthesized a series of phenyl-tetrazolyl and 4-thiopyridyl indanones as allosteric potentiators of the metabotropic glutamate receptor 2. Structure activity relationship studies directed toward improving the potency and level of potentiation, as well as PK properties, led to the discovery of 28 (EC50 = 186 nM), which displayed activity in a rodent model for schizophrenia.
Keywords :
GPCRs , mGlu receptors , glutamate , Allosteric , Schizophrenia
