Identification of pyridazin-3-one derivatives as potent, selective histamine H3 receptor inverse agonists with robust wake activity.
Bioorg Med Chem Lett
; 21(18): 5493-7, 2011 Sep 15.
Article
em En
| MEDLINE
| ID: mdl-21782432
ABSTRACT
H(3)R structure-activity relationships on a novel class of pyridazin-3-one H(3)R 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 H(3)R antagonism in vivo in the rat dipsogenia model and demonstrated robust wake activity in the rat EEG/EMG model.
Texto completo:
1
Base de dados:
MEDLINE
Assunto principal:
Piridazinas
/
Vigília
/
Agonistas dos Receptores Histamínicos
/
Ingestão de Líquidos
Tipo de estudo:
Diagnostic_studies
Limite:
Animals
/
Humans
/
Male
Idioma:
En
Ano de publicação:
2011
Tipo de documento:
Article