| Article ID | Journal | Published Year | Pages | File Type |
|---|---|---|---|---|
| 1370419 | Bioorganic & Medicinal Chemistry Letters | 2011 | 4 Pages |
Abstract
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.
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Related Topics
Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
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,