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Allosteric potentiators of the metabotropic glutamate receptor 2 (mGlu2). Part 3: Identification and biological activity of indanone containing mGlu2 receptor potentiators |
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| Authors: | Pinkerton Anthony B Cube Rowena V Hutchinson John H James Joyce K Gardner Michael F Rowe Blake A Schaffhauser Hervé Rodriguez Dana E Campbell Una C Daggett Lorrie P Vernier Jean-Michel |
| Institution: | Merck Research Laboratories, MRLSDB2, 3535 General Atomics Court, San Diego, CA 92121, USA. anthony_pinkerton@merck.com |
| 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. |
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