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Basic Information
ID: ALA1949633
Journal: Bioorg Med Chem Lett
Title: Novel morpholine ketone analogs as potent histamine H3 receptor inverse agonists with wake activity.
Authors: Sundar BG, Bailey TR, Dunn D, Hostetler GA, Chatterjee S, Bacon ER, Yue C, Schweizer D, Aimone LD, Gruner JA, Lyons J, Raddatz R, Lesur B.
Abstract: Structure-activity relationship on a novel ketone class of H(3)R antagonists/inverse agonists is disclosed. Compound 4 showed excellent target potency, selectivity and brain penetration. Evaluation of antagonist 4 in the rat EEG/EMG model demonstrated robust wake activity thereby establishing preclinical proof of concept.
CiteXplore: 22297111