Title | Selective Modulation of Gq/Gs pathways by Naphtho Pyrano Pyrimidines as antagonists of the Neuropeptide S Receptor. |
Publication Type | Journal Article |
Year of Publication | 2010 |
Authors | McCoy JG, Marugan JJ, Liu K, Zheng W, Southall N, Huang W, Heilig M, Austin CP |
Journal | ACS Chem Neurosci |
Volume | 1 |
Issue | 8 |
Pagination | 559-574 |
Date Published | 2010 Aug 18 |
ISSN | 1948-7193 |
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. |
DOI | 10.1021/cn100040h |
Alternate Journal | ACS Chem Neurosci |
PubMed ID | 21116448 |
PubMed Central ID | PMC2992437 |
Grant List | ZIA HG200319-06 / HG / NHGRI NIH HHS / United States |