Allosteric potentiators of the metabotropic glutamate receptor 2 (mGlu2). Part 1: Identification and synthesis of phenyl-tetrazolyl acetophenones |
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| Authors: | Pinkerton Anthony B Cube Rowena V Hutchinson John H Rowe Blake A Schaffhauser Hervé Zhao Xiumin Daggett Lorrie P Vernier Jean-Michel |
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| Affiliation: | Merck Research Laboratories, MRLSDB2, 3535 General Atomics Court, San Diego, CA 92121, USA. anthony_pinkerton@merck.com |
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| Abstract: | We have identified and synthesized a series of aryl-tetrazoyl acetophenones as positive allosteric potentiators of the metabotropic glutamate receptor 2. Structure activity relationship studies directed toward improving the potency and level of potentiation led to the discovery of 22 (EC(50)=93nM, 128% potentiation). |
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