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Items: 20

1.

Zebrafish behavioral profiling identifies multitarget antipsychotic-like compounds.

Bruni G, Rennekamp AJ, Velenich A, McCarroll M, Gendelev L, Fertsch E, Taylor J, Lakhani P, Lensen D, Evron T, Lorello PJ, Huang XP, Kolczewski S, Carey G, Caldarone BJ, Prinssen E, Roth BL, Keiser MJ, Peterson RT, Kokel D.

Nat Chem Biol. 2016 Jul;12(7):559-66. doi: 10.1038/nchembio.2097. Epub 2016 May 30.

2.

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.

J Pharmacol Exp Ther. 2015 Apr;353(1):213-33. doi: 10.1124/jpet.114.222463. Epub 2015 Feb 9.

PMID:
25665805
3.

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.

J Med Chem. 2015 Feb 12;58(3):1358-71. doi: 10.1021/jm501642c. Epub 2015 Feb 2.

PMID:
25565255
4.

3-Amido-3-aryl-piperidines: A Novel Class of Potent, Selective, and Orally Active GlyT1 Inhibitors.

Pinard E, Alberati D, Alvarez-Sanchez R, Brom V, Burner S, Fischer H, Hauser N, Kolczewski S, Lengyel J, Mory R, Saladin C, Schulz-Gasch T, Stalder H.

ACS Med Chem Lett. 2014 Feb 4;5(4):428-33. doi: 10.1021/ml500005m. eCollection 2014 Apr 10.

5.

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.

J Pharmacol Exp Ther. 2011 Nov;339(2):474-86. doi: 10.1124/jpet.111.185660. Epub 2011 Aug 17.

PMID:
21849627
6.

G protein-coupled receptor transmembrane binding pockets and their applications in GPCR research and drug discovery: a survey.

Kratochwil NA, Gatti-McArthur S, Hoener MC, Lindemann L, Christ AD, Green LG, Guba W, Martin RE, Malherbe P, Porter RH, Slack JP, Winnig M, Dehmlow H, Grether U, Hertel C, Narquizian R, Panousis CG, Kolczewski S, Steward L.

Curr Top Med Chem. 2011;11(15):1902-24.

PMID:
21470172
7.

Functional heterogeneity of nociceptin/orphanin FQ receptors revealed by (+)-5a Compound and Ro 64-6198 in rat periaqueductal grey slices.

Liao YY, Teng SF, Lin LC, Kolczewski S, Prinssen EP, Lee LJ, Ho IK, Chiou LC.

Int J Neuropsychopharmacol. 2011 Aug;14(7):977-89. doi: 10.1017/S146114571000129X. Epub 2010 Oct 29.

PMID:
21029514
8.

Asymmetric synthesis and receptor pharmacology of the group II mGlu receptor ligand (1S,2R,3R,5R,6S)-2-amino-3-hydroxy-bicyclo[3.1.0]hexane-2,6-dicarboxylic acid-HYDIA.

Woltering TJ, Adam G, Huguenin P, Wichmann J, Kolczewski S, Gatti S, Bourson A, Kew JN, Richards G, Kemp JA, Mutel V, Knoflach F.

ChemMedChem. 2008 Feb;3(2):323-35.

PMID:
18058780
9.

Cyclic guanidines as dual 5-HT5A/5-HT7 receptor ligands: optimising brain penetration.

Peters JU, Lübbers T, Alanine A, Kolczewski S, Blasco F, Steward L.

Bioorg Med Chem Lett. 2008 Jan 1;18(1):262-6. Epub 2007 Oct 30.

PMID:
18023344
10.

Cyclic guanidines as dual 5-HT5A/5-HT7 receptor ligands: structure-activity relationship elucidation.

Peters JU, Lübbers T, Alanine A, Kolczewski S, Blasco F, Steward L.

Bioorg Med Chem Lett. 2008 Jan 1;18(1):256-61. Epub 2007 Oct 30.

PMID:
17998160
11.

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.

ChemMedChem. 2008 Jan;3(1):136-44.

PMID:
17994660
12.

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.

Bioorg Med Chem Lett. 2007 Mar 1;17(5):1307-11. Epub 2006 Dec 15.

PMID:
17196387
13.

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.

Bioorg Med Chem Lett. 2007 Mar 1;17(5):1302-6. Epub 2006 Dec 15.

PMID:
17189691
14.

Arylmethoxypyridines as novel, potent and orally active mGlu5 receptor antagonists.

Büttelmann B, Peters JU, Ceccarelli S, Kolczewski S, Vieira E, Prinssen EP, Spooren W, Schuler F, Huwyler J, Porter RH, Jaeschke G.

Bioorg Med Chem Lett. 2006 Apr 1;16(7):1892-7. Epub 2006 Jan 24.

PMID:
16439120
15.

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.

J Pharmacol Exp Ther. 2005 Nov;315(2):711-21. Epub 2005 Jul 22.

PMID:
16040814
16.

Novel hexahydrospiro[piperidine-4,1'-pyrrolo[3,4-c]pyrroles]: highly selective small-molecule nociceptin/orphanin FQ receptor agonists.

Kolczewski S, Adam G, Cesura AM, Jenck F, Hennig M, Oberhauser T, Poli SM, Rössler F, Röver S, Wichmann J, Dautzenberg FM.

J Med Chem. 2003 Jan 16;46(2):255-64.

PMID:
12519064
17.

Parallel solution- and solid-phase synthesis of spirohydantoin derivatives as neurokinin-1 receptor ligands.

Bleicher KH, Wüthrich Y, De Boni M, Kolczewski S, Hoffmann T, Sleight AJ.

Bioorg Med Chem Lett. 2002 Sep 16;12(18):2519-22.

PMID:
12182851
18.

A synthetic agonist at the orphanin FQ/nociceptin receptor ORL1: anxiolytic profile in the rat.

Jenck F, Wichmann J, Dautzenberg FM, Moreau JL, Ouagazzal AM, Martin JR, Lundstrom K, Cesura AM, Poli SM, Roever S, Kolczewski S, Adam G, Kilpatrick G.

Proc Natl Acad Sci U S A. 2000 Apr 25;97(9):4938-43.

19.

Synthesis of heterocyclic enol ethers and their use as group 2 metabotropic glutamate receptor antagonists.

Kolczewski S, Adam G, Stadler H, Mutel V, Wichmann J, Woltering T.

Bioorg Med Chem Lett. 1999 Aug 2;9(15):2173-6.

PMID:
10465539
20.

Structure-activity relationships of substituted 5H-thiazolo[3,2-a]pyrimidines as group 2 metabotropic glutamate receptor antagonists.

Wichmann J, Adam G, Kolczewski S, Mutel V, Woltering T.

Bioorg Med Chem Lett. 1999 Jun 7;9(11):1573-6.

PMID:
10386938

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