Synthesis and evaluation of a new series of Neuropeptide S receptor antagonists.
Bioorg Med Chem Lett
; 20(15): 4700-3, 2010 Aug 01.
Article
em En
| MEDLINE
| ID: mdl-20510609
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.
Texto completo:
1
Base de dados:
MEDLINE
Assunto principal:
Receptores de Neuropeptídeos
Limite:
Animals
/
Humans
Idioma:
En
Ano de publicação:
2010
Tipo de documento:
Article