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Bioorg Med Chem Lett. 2010 Aug 1;20(15):4700-3. doi: 10.1016/j.bmcl.2010.04.143. Epub 2010 May 5.

Synthesis and evaluation of a new series of Neuropeptide S receptor antagonists.

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1
Department of Medicinal Chemistry, Merck Research Laboratories, West Point, PA, USA. jmelamed@synthonix.com

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.

PMID:
20510609
DOI:
10.1016/j.bmcl.2010.04.143
[Indexed for MEDLINE]
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