Identification of pyridazin-3-one derivatives as potent, selective histamine H₃ receptor inverse agonists with robust wake activity.

Volume: 21, Issue: 18, Pages: 5493 - 5497
Published: Sep 15, 2011
Abstract
null null H3R structure–activity relationships on a novel class of pyridazin-3-one H3R antagonists/inverse agonists are disclosed. Modifications of the pyridazinone core, central phenyl ring and linker led to the identification of molecules with excellent target potency, selectivity and pharmacokinetic properties. Compounds 13 and 21 displayed potent functional H3R antagonism in vivo in the rat dipsogenia model and demonstrated robust wake...
Paper Details
Title
Identification of pyridazin-3-one derivatives as potent, selective histamine H₃ receptor inverse agonists with robust wake activity.
Published Date
Sep 15, 2011
Volume
21
Issue
18
Pages
5493 - 5497
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