Rational design and synthesis of an orally active indolopyridone as a novel conformationally constrained cannabinoid ligand possessing antiinflammatory properties.
J Med Chem
; 46(11): 2110-6, 2003 May 22.
Article
em En
| MEDLINE
| ID: mdl-12747783
ABSTRACT
A series of unique indazoles and pyridoindolones have been rationally designed and synthesized as novel classes of cannabinoid ligands based on a proposed bioactive amide conformation. This has led to the discovery of the novel indolopyridone 3a as a conformationally constrained cannabinoid ligand that displays high affinity for the CB2 receptor (K(i)(CB2) = 1.0 nM) and possesses antiinflammatory properties when administered orally in an in vivo murine inflammation model.
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Coleções:
01-internacional
Base de dados:
MEDLINE
Assunto principal:
Piridonas
/
Receptores de Droga
/
Canabinoides
/
Anti-Inflamatórios não Esteroides
/
Indóis
/
Norbornanos
Tipo de estudo:
Prognostic_studies
Limite:
Animals
/
Female
/
Humans
Idioma:
En
Ano de publicação:
2003
Tipo de documento:
Article