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Novel morpholine ketone analogs as potent histamine H3 receptor inverse agonists with wake activity |
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| Authors: | Sundar Babu G Bailey Thomas R Dunn Derek Hostetler Greg A Chatterjee Sankar Bacon Edward R Yue Christoph Schweizer Dominique Aimone Lisa D Gruner John A Lyons Jacquelyn Raddatz Rita Lesur Brigitte |
| Institution: | Discovery Research, Cephalon, Inc., West Chester, PA 19380, USA. bgsundar@yahoo.com |
| 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. |
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