Pyrido pyrimidinones as selective agonists of the high affinity niacin receptor GPR109A: optimization of in vitro activity.
Bioorg Med Chem Lett
; 20(18): 5426-30, 2010 Sep 15.
Article
em En
| MEDLINE
| ID: mdl-20724150
ABSTRACT
Pyrido pyrimidinones are selective agonists of the human high affinity niacin receptor GPR109A (HM74A). They show no activity on the highly homologous low affinity receptor GPR109B (HM74). Starting from a high throughput screening hit the in vitro activity of the pyrido pyrimidinones was significantly improved providing lead compounds suitable for further optimization.
Texto completo:
1
Base de dados:
MEDLINE
Assunto principal:
Pirimidinonas
/
Receptores Nicotínicos
/
Receptores Acoplados a Proteínas G
/
Niacina
Limite:
Animals
Idioma:
En
Ano de publicação:
2010
Tipo de documento:
Article