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Structure-Activity Relationship of Imidazopyridinium Analogues as Antagonists of Neuropeptide S Receptor
NIH, Bethesda, MD, USA.
NIH, Bethesda, MD, USA.
NIH, Bethesda, MD, USA.
NIH, Bethesda, MD, USA.
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2013 (English)In: Journal of Medicinal Chemistry, ISSN 0022-2623, E-ISSN 1520-4804, Vol. 56, no 22, 9045-9056 p.Article in journal (Refereed) Published
Abstract [en]

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.

Place, publisher, year, edition, pages
American Chemical Society (ACS), 2013. Vol. 56, no 22, 9045-9056 p.
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Neurosciences
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URN: urn:nbn:se:liu:diva-101828DOI: 10.1021/jm400904mPubMedID: 24171469OAI: oai:DiVA.org:liu-101828DiVA: diva2:666743
Available from: 2013-11-24 Created: 2013-11-24 Last updated: 2017-12-06Bibliographically approved

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Thorsell, AnnikaHeilig, Markus

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