Abstract : Administration of Neuropeptide S (NPS) has been shown to produce arousal that is independent of nov
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Abstract : Administration of Neuropeptide S (NPS) has been shown to produce arousal that is independent of novelty and to induce wakefulness by suppressing all stages of sleep as demonstrated by EEG recordings in rat. Medicinal chemistry efforts have identified a quinolinone class of potent NPSR antagonists that readily cross the blood-brain barrier. We detail here optimization efforts resulting in the identification of a potent NPSR antagonist which dose-dependently and specifically inhibited (125)I-NPS binding in the CNS when administered to rats.Copyright 2010 Elsevier Ltd. All rights reserved.PMID 20510609 PubMed - indexed for MEDLINEMeSH Terms SubstancesMeSH TermsAnimalsBlood-Brain Barrier/metabolismCentral Nervous System/metabolismHumansIodine Radioisotopes/chemistryProtein BindingQuinolones/chemical synthesisQuinolones/chemistryQuinolones/pharmacologyRatsReceptors Neuropeptide/antagonists amp inhibitors*Receptors Neuropeptide/metabolismStructure-Activity RelationshipSubstancesIodine RadioisotopesQuinolonesReceptors NeuropeptideLinkOut - more resourcesFull Text SourcesElsevier ScienceEBSCOOhioLINK Electronic Journal CenterSwets Information Services Supplemental Content Related citations Tricyclic imidazole antagonists of the Neuropeptide S Receptor. Bioorg Med Chem Lett. 2010 Tricyclic imidazole antagonists of the Neuropeptide S Receptor.Trotter BW Nanda KK Manley PJ Uebele VN Condra CL Gotter AL Menzel K Henault M Stocco R Renger JJ et al. Bioorg Med Chem Lett. 2010 Aug 1 20(15)4704-8. Epub 2010 Apr 13. Discovery of a potent CNS-penetrant orexin receptor antagonist based on an nn-disubstituted-14-diazepane scaffold that promotes sleep in rats. ChemMedChem. 2009 Discovery of a potent CNS-penetrant orexin receptor antagonist based on an nn-disubstituted-14-diazepane scaffold that promotes sleep in rats.Whitman DB Cox CD Breslin MJ Brashear KM Schreier JD Bogusky MJ Bednar RA Lemaire W Bruno JG Hartman GD et al. ChemMedChem. 2009 Jul 4(7)1069-74. Neuropeptide S a neuropeptide promoting arousal and anxiolytic-like effects. Neuron. 2004 Neuropeptide S a neuropeptide promoting arousal and anxiolytic-like effects.Xu YL Reinscheid RK Huitron-Resendiz S Clark SD Wang Z Lin SH Brucher FA Zeng J Ly NK Henriksen SJ et al. Neuron. 2004 Aug 19 43(4)487-97. Review Neuropeptide S a novel modulator of stress and arousal. Stress. 2007 Review Neuropeptide S a novel modulator of stress and arousal.Okamura N Reinscheid RK. Stress. 2007 Aug 10(3)221-6. Review Neuropeptide S and its receptor a newly deorphanized G protein-coupled receptor system. Neuroscientist. 2005 Review Neuropeptide S and its receptor a newly deorphanized G protein-coupled receptor system.Reinscheid RK Xu YL. Neuroscientist. 2005 Dec 11(6)532-8. See reviews... See all... All links from this record Related Citations Calculated set of PubMed citations closely related to the selected article(s) retrieved using a word weight algorithm. Related articles are displayed in ranked order from most to least relevant with the “linked from” citation displayed first. Substance (MeSH Keyword) PubChem chemical substance (submitted) records that are classified under the same Medical Subject Headings (MeSH) controlled vocabulary as the current articles. Recent activity Clear Turn Off Turn On Synthesis and evaluation of a new series of Neuropeptide S receptor antagonists. Synthesis and evaluation of a new series of Neuropeptide S receptor antagonists.Bioorg Med Chem Lett. 2010 Aug 1 20(15)4700-3. Epub 2010 May 5 . PubMed Your browsing activity is empty. Activity recording is turned off. Turn recording back on See more... You are here NCBI gt Literature gt PubMed Write to the Help Desk Simple NCBI Directory Getting Started NCBI Education NCBI Help Manual NCBI Handbook Training amp Tutorials Resources Chemicals amp BioassaysData amp SoftwareDNA amp RNADomains amp StructuresGenes amp ExpressionGenetics amp MedicineGenomes amp MapsHomologyLiteratureProteinsSequence AnalysisTaxonomyTraining amp TutorialsVariation Popular PubMed Nucleotide BLAST PubMed Central Gene Bookshelf Protein OMIM Genome SNP Structure Featured GenBank Reference Sequences Map Viewer Genome Projects Human Genome Mouse Genome Influenza Virus Primer-BLAST Sequence Read Archive NCBI Information About NCBI Research at NCBI NCBI Newsletter NCBI FTP Site NCBI on Facebook NCBI on Twitter NCBI on YouTube NIH DHHS USA.gov Copyright | Disclaimer | Privacy | Accessibility | Contact National Center for Biotechnology Information U.S. National Library of Medicine 8600 Rockville Pike Bethesda MD 20894 USA
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