Literature DB >> 17884493

Syntheses and optimization of new GS39783 analogues as positive allosteric modulators of GABA B receptors.

Sébastien Guery1, Philipp Floersheim, Klemens Kaupmann, Wolfgang Froestl.   

Abstract

The optimization of GS39783 into potent, selective, and safe positive allosteric modulators of GABA(B) receptors is presented.

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Year:  2007        PMID: 17884493      PMCID: PMC2278029          DOI: 10.1016/j.bmcl.2007.09.023

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN: 0960-894X            Impact factor:   2.823


  15 in total

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Review 4.  Is the GABA B heterodimer a good drug target?

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9.  Behavioral characterization of the novel GABAB receptor-positive modulator GS39783 (N,N'-dicyclopentyl-2-methylsulfanyl-5-nitro-pyrimidine-4,6-diamine): anxiolytic-like activity without side effects associated with baclofen or benzodiazepines.

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10.  N,N'-Dicyclopentyl-2-methylsulfanyl-5-nitro-pyrimidine-4,6-diamine (GS39783) and structurally related compounds: novel allosteric enhancers of gamma-aminobutyric acidB receptor function.

Authors:  Stephan Urwyler; Mario F Pozza; Kurt Lingenhoehl; Johannes Mosbacher; Christina Lampert; Wolfgang Froestl; Manuel Koller; Klemens Kaupmann
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  22 in total

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4.  Both GABA(B) receptor activation and blockade exacerbated anhedonic aspects of nicotine withdrawal in rats.

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Review 5.  Computational Advances for the Development of Allosteric Modulators and Bitopic Ligands in G Protein-Coupled Receptors.

Authors:  Zhiwei Feng; Guanxing Hu; Shifan Ma; Xiang-Qun Xie
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8.  Discriminative stimulus effects of the GABAB receptor-positive modulator rac-BHFF: comparison with GABAB receptor agonists and drugs of abuse.

Authors:  Wouter Koek; Kejun Cheng; Kenner C Rice
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9.  Comparison of the effects of the GABAB receptor positive modulator BHF177 and the GABAB receptor agonist baclofen on anxiety-like behavior, learning, and memory in mice.

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10.  Positive modulation of GABA(B) receptors decreased nicotine self-administration and counteracted nicotine-induced enhancement of brain reward function in rats.

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