Leurs R - Search Results

1

Surface plasmon resonance biosensor based fragment screening using acetylcholine binding protein identifies ligand efficiency hot spots (LE hot spots) by deconstruction of nicotinic acetylcholine receptor α7 ligands.

de Kloe GE, Retra K, Geitmann M, Källblad P, Nahar T, van Elk R, Smit AB, van Muijlwijk-Koezen JE, Leurs R, Irth H, Danielson UH, de Esch IJ. de Kloe GE, et al. Among authors: leurs r. J Med Chem. 2010 Oct 14;53(19):7192-201. doi: 10.1021/jm100834y. J Med Chem. 2010. PMID: 20828128

2

Homologs of histamine as histamine H3 receptor antagonists: a new potent and selective H3 antagonist, 4(5)-(5-aminopentyl)-1H-imidazole.

Vollinga RC, Menge WM, Leurs R, Timmerman H. Vollinga RC, et al. Among authors: leurs r. J Med Chem. 1995 Jan 20;38(2):266-71. doi: 10.1021/jm00002a008. J Med Chem. 1995. PMID: 7830269

3

A new potent and selective histamine H3 receptor agonist, 4-(1H-imidazol-4-ylmethyl)piperidine.

Vollinga RC, de Koning JP, Jansen FP, Leurs R, Menge WM, Timmerman H. Vollinga RC, et al. Among authors: leurs r. J Med Chem. 1994 Feb 4;37(3):332-3. doi: 10.1021/jm00029a002. J Med Chem. 1994. PMID: 8308858 No abstract available.

4

Characterization of the binding site of the histamine H3 receptor. 1. Various approaches to the synthesis of 2-(1H-imidazol-4-yl)cyclopropylamine and histaminergic activity of (1R,2R)- and (1S,2S)-2-(1H-imidazol-4-yl)-cyclopropylamine.

De Esch IJ, Vollinga RC, Goubitz K, Schenk H, Appelberg U, Hacksell U, Lemstra S, Zuiderveld OP, Hoffmann M, Leurs R, Menge WM, Timmerman H. De Esch IJ, et al. Among authors: leurs r. J Med Chem. 1999 Apr 8;42(7):1115-22. doi: 10.1021/jm9810912. J Med Chem. 1999. PMID: 10197956 Free article.

5

Characterization of the binding site of the histamine H(3) receptor. 2. Synthesis, in vitro pharmacology, and QSAR of a series of monosubstituted benzyl analogues of thioperamide.

Windhorst AD, Timmerman H, Worthington EA, Bijloo GJ, Nederkoorn PH, Menge WM, Leurs R, Herscheid JD. Windhorst AD, et al. Among authors: leurs r. J Med Chem. 2000 May 4;43(9):1754-61. doi: 10.1021/jm981106w. J Med Chem. 2000. PMID: 10794692

6

Development of a pharmacophore model for histamine H3 receptor antagonists, using the newly developed molecular modeling program SLATE.

De Esch IJ, Mills JE, Perkins TD, Romeo G, Hoffmann M, Wieland K, Leurs R, Menge WM, Nederkoorn PH, Dean PM, Timmerman H. De Esch IJ, et al. Among authors: leurs r. J Med Chem. 2001 May 24;44(11):1666-74. doi: 10.1021/jm001109k. J Med Chem. 2001. PMID: 11356102

7

A selective human H(4)-receptor agonist: (-)-2-cyano-1-methyl-3-[(2R,5R)-5- [1H-imidazol-4(5)-yl]tetrahydrofuran-2-y] methylguanidine.

Hashimoto T, Harusawa S, Araki L, Zuiderveld OP, Smit MJ, Imazu T, Takashima S, Yamamoto Y, Sakamoto Y, Kurihara T, Leurs R, Bakker RA, Yamatodani A. Hashimoto T, et al. Among authors: leurs r. J Med Chem. 2003 Jul 3;46(14):3162-5. doi: 10.1021/jm0300025. J Med Chem. 2003. PMID: 12825954

8

Synthesis and structure-activity relationships of conformationally constrained histamine H(3) receptor agonists.

Kitbunnadaj R, Zuiderveld OP, De Esch IJ, Vollinga RC, Bakker R, Lutz M, Spek AL, Cavoy E, Deltent MF, Menge WM, Timmerman H, Leurs R. Kitbunnadaj R, et al. Among authors: leurs r. J Med Chem. 2003 Dec 4;46(25):5445-57. doi: 10.1021/jm030905y. J Med Chem. 2003. PMID: 14640553

9

Synthesis and pharmacological identification of neutral histamine H1-receptor antagonists.

Govoni M, Bakker RA, van de Wetering I, Smit MJ, Menge WM, Timmerman H, Elz S, Schunack W, Leurs R. Govoni M, et al. Among authors: leurs r. J Med Chem. 2003 Dec 18;46(26):5812-24. doi: 10.1021/jm030936t. J Med Chem. 2003. PMID: 14667234

10

Identification of 4-(1H-imidazol-4(5)-ylmethyl)pyridine (immethridine) as a novel, potent, and highly selective histamine H(3) receptor agonist.

Kitbunnadaj R, Zuiderveld OP, Christophe B, Hulscher S, Menge WM, Gelens E, Snip E, Bakker RA, Celanire S, Gillard M, Talaga P, Timmerman H, Leurs R. Kitbunnadaj R, et al. Among authors: leurs r. J Med Chem. 2004 May 6;47(10):2414-7. doi: 10.1021/jm049932u. J Med Chem. 2004. PMID: 15115383

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