Identification of a novel RAMP-independent CGRP receptor antagonist.
Bioorg Med Chem Lett
; 21(22): 6705-8, 2011 Nov 15.
Article
em En
| MEDLINE
| ID: mdl-21982500
ABSTRACT
Identification of an HIV integrase inhibitor with micromolar affinity for the CGRP receptor led to the discovery of a series of structurally novel CGRP receptor antagonists. Optimization of this series produced compound 16, a low-molecular weight CGRP receptor antagonist with good pharmacokinetic properties in both rat and dog. In contrast to other nonpeptide antagonists, the activity of 16 was affected by the presence of divalent cations and showed evidence of an alternative, RAMP-independent CGRP receptor binding site.
Texto completo:
1
Coleções:
01-internacional
Temas:
Geral
Base de dados:
MEDLINE
Assunto principal:
Piridinas
/
Receptores de Peptídeo Relacionado com o Gene de Calcitonina
/
Inibidores de Integrase de HIV
/
Proteínas Modificadoras da Atividade de Receptores
/
Antagonistas do Receptor do Peptídeo Relacionado ao Gene de Calcitonina
Tipo de estudo:
Diagnostic_studies
Limite:
Animals
/
Humans
Idioma:
En
Revista:
Bioorg Med Chem Lett
Assunto da revista:
BIOQUIMICA
/
QUIMICA
Ano de publicação:
2011
Tipo de documento:
Article
País de afiliação:
Estados Unidos