1226997-30-3Relevant academic research and scientific papers
Synthesis and evaluation of a new series of Neuropeptide S receptor antagonists
Melamed, Jeffrey Y.,Zartman, Amy E.,Kett, Nathan R.,Gotter, Anthony L.,Uebele, Victor N.,Reiss, Duane R.,Condra, Cindra L.,Fandozzi, Christine,Lubbers, Laura S.,Rowe, Blake A.,McGaughey, Georgia B.,Henault, Martin,Stocco, Rino,Renger, John J.,Hartman, George D.,Bilodeau, Mark T.,Trotter, B. Wesley
scheme or table, p. 4700 - 4703 (2010/10/02)
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 125I-NPS binding in the CNS when administered to rats.
QUINOLONE NEUROPEPTIDE S RECEPTOR ANTAGONISTS
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Page/Page column 51; 52, (2010/06/15)
The present invention is directed to quinolone compounds which are antagonists of neuropeptide S receptors, and which are useful in the treatment or prevention of neurological and psychiatric disorders and diseases in which the neuropeptide S receptor is involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which the neuropeptide S receptor is involved.
