- Structure-activity relationship of imidazopyridinium analogues as antagonists of neuropeptide s receptor
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The discovery and characterization of a novel chemical series of phosphorothioyl-containing imidazopyridines as potent neuropeptide S receptor antagonists is presented. The synthesis of analogues and their structure-activity relationship with respect to the Gq, Gs, and ERK pathways is detailed. The pharmacokinetics and in vivo efficacy of a potent analogue in a food intake rodent model are also included, underscoring its potential therapeutic value for the treatment of sleep, anxiety, and addiction disorders. This article not subject to U.S. Copyright. Published 2013 by the American Chemical Society.
- Patnaik, Samarjit,Marugan, Juan J.,Liu, Ke,Zheng, Wei,Southall, Noel,Dehdashti, Seameen J.,Thorsell, Annika,Heilig, Markus,Bell, Lauren,Zook, Michelle,Eskay, Bob,Brimacombe, Kyle R.,Austin, Christopher P.
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p. 9045 - 9056
(2014/01/06)
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- SMALL MOLECULE NEUROPEPTIDE S ANTAGONISTS FOR THE TREATMENT OF ADDICTIVE DISORDERS, MOOD, ANXIETY AND SLEEP DISORDERS
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Disclosed are compounds of General Formula I: wherein R1, R2, R3, X and Y are described herein, as well as pharmaceutically acceptable salts, solvates, and stereoisomers thereof. Pharmaceutical compositions comprising such compounds, as well as methods of
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