Identification of a novel RAMP-independent CGRP receptor antagonist.
Bioorg Med Chem Lett
; 21(22): 6705-8, 2011 Nov 15.
Article
en 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
Colección:
01-internacional
Banco de datos:
MEDLINE
Asunto principal:
Piridinas
/
Receptores de Péptido Relacionado con el Gen de Calcitonina
/
Inhibidores de Integrasa VIH
/
Proteínas Modificadoras de la Actividad de Receptores
/
Antagonistas del Receptor Peptídico Relacionado con el Gen de la Calcitonina
Tipo de estudio:
Diagnostic_studies
Límite:
Animals
/
Humans
Idioma:
En
Revista:
Bioorg Med Chem Lett
Asunto de la revista:
BIOQUIMICA
/
QUIMICA
Año:
2011
Tipo del documento:
Article
País de afiliación:
Estados Unidos