Author/Authors :
Céline Bonnefous، نويسنده , , Jean-Michel Vernier، نويسنده , , John H. Hutchinson، نويسنده , , Michael F. Gardner، نويسنده , , Merryl Cramer، نويسنده , , Joyce K. James، نويسنده , , Blake A. Rowe، نويسنده , , Lorrie P. Daggett، نويسنده , , Herve Schaffhauser، نويسنده , , Theodore M. Kamenecka، نويسنده ,
Abstract :
We have identified and synthesized a series of biphenyl-carboxylic acid indanones as allosteric potentiators of the metabotropic glutamate receptor 2. Structure–activity relationship studies directed toward improving the potency and the brain to plasma ratio of the initial lead led to the discovery of 5 and 23 (EC50 = 111 and 5 nM, respectively).
Keywords :
mGluR2 , Indanone , CNS , Schizophrenia
