Allosteric potentiators of the metabotropic glutamate receptor 2 (mGlu2). Part 3: Identification and biological activity of indanone containing mGlu2 ...

Basic Information

ID: ALA1142032

Journal: Bioorg Med Chem Lett

Title: Allosteric potentiators of the metabotropic glutamate receptor 2 (mGlu2). Part 3: Identification and biological activity of indanone containing mGlu2 receptor potentiators.

Authors: Pinkerton AB, Cube RV, Hutchinson JH, James JK, Gardner MF, Rowe BA, Schaffhauser H, Rodriguez DE, Campbell UC, Daggett LP, Vernier JM.

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.

CiteXplore: 15745798

DOI: 10.1016/j.bmcl.2005.01.077

Patent ID: