1197359-90-2Relevant academic research and scientific papers
Synthesis and evaluation of pyridazinone.phenethylamine derivatives as selective and orally bioavailable histamine H3 receptor antagonists with robust wake-promoting activity
Dandu, Reddeppa Reddy,Gruner, John A.,Mathiasen, Joanne R.,Aimone, Lisa D.,Hostetler, Greg,Benfield, Caitlyn,Bendesky, Robert J.,Marcy, Val R.,Raddatz, Rita,Hudkins, Robert L.
, p. 6362 - 6365 (2011/11/29)
A series of pyridazinone-phenethylamine derivatives with moderate to low nanomolar affinity for rat and human H3R are described. These analogs exhibited excellent selectivity and metabolic stability, with acceptable rat pharmacokinetic properties. In vivo, 7 and 11 demonstrated potent H3R functional antagonism in the rat dipsogenia model and robust wake-promoting activity in the rat electroencephalogram/electromyography (EEG/EMG) model.
SUBSTITUTED PYRIDAZINONE DERIVATIVES AS HISTAMINE-3 (H3) RECEPTOR LIGANDS
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Page/Page column 78-79, (2009/12/27)
The present invention provides compounds according to Formulas I, II, III, IV, V, VI, VII or VIII; their use as H3 antagonists/inverse agonists, processes for their preparation, and pharmaceutical compositions thereof
