1086423-99-5Relevant articles and documents
Synthesis of (3,4-dimethoxyphenoxy)alkylamino acetamides as orexin-2 receptor antagonists
Cole, Andrew G.,Stroke, Ilana L.,Qin, Lan-Ying,Hussain, Zahid,Simhadri, Srilatha,Brescia, Marc-Raleigh,Waksmunski, Frank S.,Strohl, Barbara,Tellew, John E.,Williams, John P.,Saunders, John,Appell, Kenneth C.,Henderson, Ian,Webb, Maria L.
, p. 5420 - 5423 (2008)
The discovery and synthesis of a series of (dimethoxyphenoxy)alkylamino acetamides as orexin-2 receptor antagonists from a small-molecule combinatorial library using a high-throughput calcium mobilization functional assay (HEK293-human OX2-R cell line) is described. Active compounds show a good correlation between high-throughput single concentration screening data and measured IC50s. Specific examples exhibit IC50 values of ～20 nM using human orexin A as the peptide agonist for the orexin-2 receptor.
