Journal
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 14, Issue 16, Pages 4225-4229Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2004.06.032
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Orexins, also termed hypocretins, consist of two neuropeptide agonists (orexin A and B) interacting with two known G-protein coupled receptors (OX1R and OX2R). In addition to other biological functions, the orexin-2 receptor is thought to be an important modulator of sleep and wakefulness. Herein we describe a series of novel, selective OX2R antagonists consisting of substituted 4-phenyl-[1,3]dioxanes. One such antagonist is compound 9, 1-(2,4-dibromo-phenyl)-3-((4S,5s)-2,2-dimethyl-4-phenyl[1,3]dioxan-5-yl)-urea, which is bound by the OX2R with a pK(i) of 8.3, has a pK(b) of 7.9, and is 600-fold selective for the OX2R over the OX1R. (C) 2004 Elsevier Ltd. All rights reserved.
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