Activation of the G-protein-coupled receptor 119: a conformation-based hypothesis for understanding agonist response.
J Med Chem
; 54(6): 1948-52, 2011 Mar 24.
Article
em En
| MEDLINE
| ID: mdl-21361292
ABSTRACT
The synthesis and properties of the bridged piperidine (oxaazabicyclo) compounds 8, 9, and 11 are described. A conformational analysis of these structures is compared with the representative GPR119 ligand 1. These results and the differences in agonist pharmacology are used to formulate a conformation-based hypothesis to understand activation of the GPR119 receptor. We also show for these structures that the agonist pharmacology in rat masks the important differences in human pharmacology.
Texto completo:
1
Bases de dados:
MEDLINE
Assunto principal:
Pirimidinas
/
Receptores Acoplados a Proteínas G
/
Compostos Azabicíclicos
Limite:
Animals
/
Humans
Idioma:
En
Revista:
J Med Chem
Assunto da revista:
QUIMICA
Ano de publicação:
2011
Tipo de documento:
Article
País de afiliação:
Estados Unidos