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Page 1
Rational design, synthesis, and structure-activity relationship of benzoxazolones: new potent mglu5 receptor antagonists based on the fenobam structure.
Ceccarelli SM, Jaeschke G, Buettelmann B, Huwyler J, Kolczewski S, Peters JU, Prinssen E, Porter R, Spooren W, Vieira E. Ceccarelli SM, et al. Among authors: porter r. Bioorg Med Chem Lett. 2007 Mar 1;17(5):1302-6. doi: 10.1016/j.bmcl.2006.12.006. Epub 2006 Dec 15. Bioorg Med Chem Lett. 2007. PMID: 17189691
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: porter r. 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. 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
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. J Med Chem. 2015 Feb 12;58(3):1358-71. doi: 10.1021/jm501642c. Epub 2015 Feb 2. J Med Chem. 2015. PMID: 25565255
Pharmacology of basimglurant (RO4917523, RG7090), a unique metabotropic glutamate receptor 5 negative allosteric modulator in clinical development for depression.
Lindemann L, Porter RH, Scharf SH, Kuennecke B, Bruns A, von Kienlin M, Harrison AC, Paehler A, Funk C, Gloge A, Schneider M, Parrott NJ, Polonchuk L, Niederhauser U, Morairty SR, Kilduff TS, Vieira E, Kolczewski S, Wichmann J, Hartung T, Honer M, Borroni E, Moreau JL, Prinssen E, Spooren W, Wettstein JG, Jaeschke G. Lindemann L, et al. Among authors: porter rh. J Pharmacol Exp Ther. 2015 Apr;353(1):213-33. doi: 10.1124/jpet.114.222463. Epub 2015 Feb 9. J Pharmacol Exp Ther. 2015. PMID: 25665805
CTEP: a novel, potent, long-acting, and orally bioavailable metabotropic glutamate receptor 5 inhibitor.
Lindemann L, Jaeschke G, Michalon A, Vieira E, Honer M, Spooren W, Porter R, Hartung T, Kolczewski S, Büttelmann B, Flament C, Diener C, Fischer C, Gatti S, Prinssen EP, Parrott N, Hoffmann G, Wettstein JG. Lindemann L, et al. Among authors: porter r. J Pharmacol Exp Ther. 2011 Nov;339(2):474-86. doi: 10.1124/jpet.111.185660. Epub 2011 Aug 17. J Pharmacol Exp Ther. 2011. PMID: 21849627
Metabolite identification via LC-SPE-NMR-MS of the in vitro biooxidation products of a lead mGlu5 allosteric antagonist and impact on the improvement of metabolic stability in the series.
Ceccarelli SM, Schlotterbeck G, Boissin P, Binder M, Buettelmann B, Hanlon S, Jaeschke G, Kolczewski S, Kupfer E, Peters JU, Porter RH, Prinssen EP, Rueher M, Ruf I, Spooren W, Stämpfli A, Vieira E. Ceccarelli SM, et al. ChemMedChem. 2008 Jan;3(1):136-44. doi: 10.1002/cmdc.200700203. ChemMedChem. 2008. PMID: 17994660
2,111 results