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RO4938581, a novel cognitive enhancer acting at GABAA alpha5 subunit-containing receptors.
Ballard TM, Knoflach F, Prinssen E, Borroni E, Vivian JA, Basile J, Gasser R, Moreau JL, Wettstein JG, Buettelmann B, Knust H, Thomas AW, Trube G, Hernandez MC. Ballard TM, et al. Among authors: prinssen e. Psychopharmacology (Berl). 2009 Jan;202(1-3):207-23. doi: 10.1007/s00213-008-1357-7. Epub 2008 Oct 21. Psychopharmacology (Berl). 2009. PMID: 18936916
Failed trials for central nervous system disorders do not necessarily invalidate preclinical models and drug targets.
Bespalov A, Steckler T, Altevogt B, Koustova E, Skolnick P, Deaver D, Millan MJ, Bastlund JF, Doller D, Witkin J, Moser P, O'Donnell P, Ebert U, Geyer MA, Prinssen E, Ballard T, Macleod M. Bespalov A, et al. Among authors: prinssen e. Nat Rev Drug Discov. 2016 Jul;15(7):516. doi: 10.1038/nrd.2016.88. Epub 2016 Jun 17. Nat Rev Drug Discov. 2016. PMID: 27312728 No abstract available.
Characterization of (R,S)-5,7-di-tert-butyl-3-hydroxy-3-trifluoromethyl-3H-benzofuran-2-one as a positive allosteric modulator of GABAB receptors.
Malherbe P, Masciadri R, Norcross RD, Knoflach F, Kratzeisen C, Zenner MT, Kolb Y, Marcuz A, Huwyler J, Nakagawa T, Porter RH, Thomas AW, Wettstein JG, Sleight AJ, Spooren W, Prinssen EP. Malherbe P, et al. Among authors: prinssen ep. Br J Pharmacol. 2008 Jun;154(4):797-811. doi: 10.1038/bjp.2008.135. Epub 2008 Apr 21. Br J Pharmacol. 2008. PMID: 18536733 Free PMC article.
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: prinssen e. 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
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: prinssen e. 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
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: prinssen e. J Med Chem. 2015 Feb 12;58(3):1358-71. doi: 10.1021/jm501642c. Epub 2015 Feb 2. J Med Chem. 2015. PMID: 25565255
79 results