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Bioorg Med Chem Lett
; 21(21): 6362-5, 2011 Nov 01.
Article
in English
| MEDLINE
| ID: mdl-21944855
ABSTRACT
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.