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Selective Modulation of Gq/Gs pathways by Naphtho Pyrano Pyrimidines as antagonists of the Neuropeptide S Receptor.

TitleSelective Modulation of Gq/Gs pathways by Naphtho Pyrano Pyrimidines as antagonists of the Neuropeptide S Receptor.
Publication TypeJournal Article
Year of Publication2010
AuthorsMcCoy JG, Marugan JJ, Liu K, Zheng W, Southall N, Huang W, Heilig M, Austin CP
JournalACS Chem Neurosci
Volume1
Issue8
Pagination559-574
Date Published2010 Aug 18
ISSN1948-7193
Abstract

Antagonists of the Neuropeptide S Receptor have been postulated as promising therapeutics in the treatment of respiratory, sleep, anxiety, and addictive disorders. Here we present the SAR of a new series of orthosteric antagonists. Neuropeptide S Receptor signaling is coupled to both Gq and Gs proteins, and we observe that different analogues in this structural series can selectively antagonize these two pathways. Many G-protein coupled receptors transduce signals through multiple pathways. Selective antagonism of these pathways may lead the way to the development of more targeted pharmacological profiles and therapies.

DOI10.1021/cn100040h
Alternate JournalACS Chem Neurosci
PubMed ID21116448
PubMed Central IDPMC2992437
Grant ListZIA HG200319-06 / HG / NHGRI NIH HHS / United States