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• W1968355890 abstract "We report the optimization of a series of non-MPEP site metabotropic glutamate receptor 5 (mGlu 5 ) positive allosteric modulators (PAMs) based on a simple acyclic ether series. Modifications led to a gain of MPEP site interaction through incorporation of a chiral amide in conjunction with a nicotinamide core. A highly potent PAM, 8v (VU0404251), was shown to be efficacious in a rodent model of psychosis. These studies suggest that potent PAMs within topologically similar chemotypes can be developed to preferentially interact or not interact with the MPEP allosteric binding site." @default.
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• W1968355890 date "2012-10-01" @default.
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• W1968355890 title "Optimization of an ether series of mGlu5 positive allosteric modulators: Molecular determinants of MPEP-site interaction crossover" @default.
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• W1968355890 doi "https://doi.org/10.1016/j.bmcl.2012.08.043" @default.
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