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Synthesis and evaluation of pyridazinone-phenethylamine derivatives as selective and orally bioavailable histamine H3 receptor antagonists with robust wake-promoting activity. | LitMetric
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Synthesis and evaluation of pyridazinone-phenethylamine derivatives as selective and orally bioavailable histamine H3 receptor antagonists with robust wake-promoting activity.

Reddeppa Reddy Dandu John A Gruner Joanne R Mathiasen Lisa D Aimone Greg Hostetler Caitlyn Benfield Robert J Bendesky Val R Marcy Rita Raddatz Robert L Hudkins

Bioorg Med Chem Lett

Discovery Research, Cephalon, Inc., 145 Brandywine Parkway, West Chester, PA 19380, USA.

Published: November 2011

A series of pyridazinone-phenethylamine derivatives with moderate to low nanomolar affinity for rat and human H(3)R are described. These analogs exhibited excellent selectivity and metabolic stability, with acceptable rat pharmacokinetic properties. In vivo, 7 and 11 demonstrated potent H(3)R functional antagonism in the rat dipsogenia model and robust wake-promoting activity in the rat electroencephalogram/electromyography (EEG/EMG) model.

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http://dx.doi.org/10.1016/j.bmcl.2011.08.104DOI Listing

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