Discovery of 2,5-diarylnicotinamides as selective orexin-2 receptor antagonists (2-SORAs)

The orexin (or hypocretin) system has been identified as a novel target for the treatment of insomnia due to the wealth of biological and genetic data discovered over the past decade. Recently, clinical proof-of-concept was achieved for the treatment of primary insomnia using dual (OX1R/OX2R) orexin...

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Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2013-12, Vol.23 (24), p.6620-6624
Hauptverfasser:	Mercer, Swati P., Roecker, Anthony J., Garson, Susan, Reiss, Duane R., Meacham Harrell, C., Murphy, Kathy L., Bruno, Joseph G., Bednar, Rodney A., Lemaire, Wei, Cui, Donghui, Cabalu, Tamara D., Tang, Cuyue, Prueksaritanont, Thomayant, Hartman, George D., Young, Steven D., Winrow, Christopher J., Renger, John J., Coleman, Paul J.
Format:	Artikel
Sprache:	eng
Schlagworte:	Animals antagonists chemistry Dogs Drug Evaluation, Preclinical electroencephalography Half-Life Humans Hypocretin Insomnia Nicotinic Acids - chemical synthesis Nicotinic Acids - chemistry Nicotinic Acids - pharmacokinetics Nicotinic Acids - pharmacology Orexin Receptor Antagonists Orexin Receptors - metabolism pharmacology Protein Binding - drug effects Rat sleep EEG Rats Selective orexin-2 receptor antagonists sleep sleep disorders Structure-Activity Relationship
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