365565-85-1Relevant academic research and scientific papers
Novel morpholine ketone analogs as potent histamine H3 receptor inverse agonists with wake activity
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
, p. 1546 - 1549 (2012/04/04)
Structure-activity relationship on a novel ketone class of H3R 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.
