| Literature DB >> 20510609 |
Jeffrey Y Melamed1, Amy E Zartman, Nathan R Kett, Anthony L Gotter, Victor N Uebele, Duane R Reiss, Cindra L Condra, Christine Fandozzi, Laura S Lubbers, Blake A Rowe, Georgia B McGaughey, Martin Henault, Rino Stocco, John J Renger, George D Hartman, Mark T Bilodeau, B Wesley Trotter.
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.Entities:
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Year: 2010 PMID： 20510609 DOI： 10.1016/j.bmcl.2010.04.143
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823