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(b) Johnson, M. P.; Baez, M.; Jagdmann, G. E.; Britton, T. C.; Large, T. H.; Callagaro, D. O.; Tizzano, J. P.; Monn, J. A.; Schoepp, D. D. Discovery of allosteric potentiators for the metabotropic glutamate 2 receptor: synthesis and subtype selectivity of N-(4-(2-methoxyphenoxy)phenyl)-N-(2,2,2- trifluoroethylsulfonyl)pyrid-3-ylmethylamine. J. Med. Chem. 2003, 46, 3189-3192.
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(a) O'Brien, J. A.; Lemaire, W.; Chen, T.-B.; Chang, R. S. L.; Jacobson, M. A.; Ha, S. N.; Lindsley, C. W.; Sur, C.; Pettibone, D. J.; Conn, J.; Wiliams, D. L. A family of highly selective allosteric modulators of the metabotropic glutamate receptor subtype 5 (mGluR5). Mol. Pharmacol. 2003, 64 (3), 731.
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(b) O'Brien, J. A.; Lemaire, W.; Wittman, M.; Jacobson, M. A.; Ha, S. N.; Wisnoski, D. D.; Lindsley, C. W.; Schaffhauser, H. J.; Sur, C.; Duggan, M. E.; Pettibone, D. J.; Conn, P. J.; Wiliams, D. L. 'A novel, selective allosteric modulator potentitaes the activity of native metabotropic glutamate receptor subtype 5 (mGluR5) in rat forebrain. J. Pharmacol. Exp. Ther. 2004, 309 (2), 568-577.
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8644289050
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note
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Unfortunately, we did not have access to an mGluR6 cell line, so we could not evaluate selectivity vs mGluR5 in this instance.
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17
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Kinney, G. G.; O'Brien, J. A.; Lemaire, W.; Burno, M.; Bickel, D. J.; Clements, M. K.; Wisnoski, D. W.; Lindsley, C. W.; Tiller, P. R.; Smith, S.; Jacobson, M. A.; Sur, S.; Duggan, M. E.; Pettibone, D. J.; Williams, D. L., Jr. A novel selective allosteric modulator of Metabotropic glutamate receptor subtype 5 (mGluR5) has an antipsychotic profile in rats behavioral models. J. Neurosci., submitted.
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Regan, J.; Breitfelder, S.; Cirillo, P.; Gilmore, T.; Graham, A. G.; Hickey, E.; Klaus, B.; Madweed, J.; Moriak, M.; Moss, N.; Pargellis, C.; Pav, S.; Proto, A.; Swinamer, A.; Tong, L.; Torcellini, C. Pyrazole urea-based inhibitors of p38 MAP kinase: from lead compound to clinical candidate. J. Med. Chem. 2002, 45, 2994-3008.
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8644287997
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50 of 9.7 μM.
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21
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