Title of article
Allosteric potentiators of the metabotropic glutamate receptor 2 (mGlu2). Part 3: Identification and biological activity of indanone containing mGlu2 receptor potentiators
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 ,
Issue Information
روزنامه با شماره پیاپی سال 2005
Pages
7
From page
1565
To page
1571
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
Journal title
Bioorganic & Medicinal Chemistry Letters
Serial Year
2005
Journal title
Bioorganic & Medicinal Chemistry Letters
Record number
795436
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