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Metabotropic glutamate receptor 5 negative allosteric modulators: discovery of 2-chloro-4-[1-(4-fluorophenyl)-2,5-dimethyl-1H-imidazol-4-ylethynyl]pyridine (basimglurant, RO4917523), a promising novel medicine for psychiatric diseases.
Jaeschke G, Kolczewski S, Spooren W, Vieira E, Bitter-Stoll N, Boissin P, Borroni E, Büttelmann B, Ceccarelli S, Clemann N, David B, Funk C, Guba W, Harrison A, Hartung T, Honer M, Huwyler J, Kuratli M, Niederhauser U, Pähler A, Peters JU, Petersen A, Prinssen E, Ricci A, Rueher D, Rueher M, Schneider M, Spurr P, Stoll T, Tännler D, Wichmann J, Porter RH, Wettstein JG, Lindemann L. Jaeschke G, et al. Among authors: wichmann j. J Med Chem. 2015 Feb 12;58(3):1358-71. doi: 10.1021/jm501642c. Epub 2015 Feb 2. J Med Chem. 2015. PMID: 25565255
Synthesis and biological evaluation of fenobam analogs as mGlu5 receptor antagonists.
Jaeschke G, Porter R, Büttelmann B, Ceccarelli SM, Guba W, Kuhn B, Kolczewski S, Huwyler J, Mutel V, Peters JU, Ballard T, Prinssen E, Vieira E, Wichmann J, Spooren W. Jaeschke G, et al. Among authors: wichmann j. Bioorg Med Chem Lett. 2007 Mar 1;17(5):1307-11. doi: 10.1016/j.bmcl.2006.12.033. Epub 2006 Dec 15. Bioorg Med Chem Lett. 2007. PMID: 17196387
Fenobam: a clinically validated nonbenzodiazepine anxiolytic is a potent, selective, and noncompetitive mGlu5 receptor antagonist with inverse agonist activity.
Porter RH, Jaeschke G, Spooren W, Ballard TM, Büttelmann B, Kolczewski S, Peters JU, Prinssen E, Wichmann J, Vieira E, Mühlemann A, Gatti S, Mutel V, Malherbe P. Porter RH, et al. Among authors: wichmann j. J Pharmacol Exp Ther. 2005 Nov;315(2):711-21. doi: 10.1124/jpet.105.089839. Epub 2005 Jul 22. J Pharmacol Exp Ther. 2005. PMID: 16040814
Synthesis and characterization of 1,3-dihydro-benzo[b][1,4]diazepin-2-one derivatives: Part 3. New potent non-competitive metabotropic glutamate receptor 2/3 antagonists.
Woltering TJ, Wichmann J, Goetschi E, Adam G, Kew JN, Knoflach F, Ballard TM, Huwyler J, Mutel V, Gatti S. Woltering TJ, et al. Among authors: wichmann j. Bioorg Med Chem Lett. 2008 Apr 15;18(8):2725-9. doi: 10.1016/j.bmcl.2008.02.076. Epub 2008 Mar 5. Bioorg Med Chem Lett. 2008. PMID: 18374569
Synthesis and characterization of 1,3-dihydro-benzo[b][1,4]diazepin-2-one derivatives: Part 4. In vivo active potent and selective non-competitive metabotropic glutamate receptor 2/3 antagonists.
Woltering TJ, Wichmann J, Goetschi E, Knoflach F, Ballard TM, Huwyler J, Gatti S. Woltering TJ, et al. Among authors: wichmann j. Bioorg Med Chem Lett. 2010 Dec 1;20(23):6969-74. doi: 10.1016/j.bmcl.2010.09.125. Epub 2010 Oct 21. Bioorg Med Chem Lett. 2010. PMID: 20971004
Discovery of the imidazo[1,5-a][1,2,4]-triazolo[1,5-d][1,4]benzodiazepine scaffold as a novel, potent and selective GABA(A) alpha5 inverse agonist series.
Achermann G, Ballard TM, Blasco F, Broutin PE, Büttelmann B, Fischer H, Graf M, Hernandez MC, Hilty P, Knoflach F, Koblet A, Knust H, Kurt A, Martin JR, Masciadri R, Porter RH, Stadler H, Thomas AW, Trube G, Wichmann J. Achermann G, et al. Among authors: wichmann j. Bioorg Med Chem Lett. 2009 Oct 1;19(19):5746-52. doi: 10.1016/j.bmcl.2009.07.153. Epub 2009 Aug 4. Bioorg Med Chem Lett. 2009. PMID: 19726184
390 results