Piperidyl amides as novel, potent and orally active mGlu5 receptor antagonists with anxiolytic-like activity.
Bioorg Med Chem Lett
; 20(1): 184-8, 2010 Jan 01.
Article
en En
| MEDLINE
| ID: mdl-19931453
ABSTRACT
High throughput screening led to the identification of nicotinamide derivative 2 as a structurally novel mGluR5 antagonist. Optimization of the modular scaffold led to the discovery of 16m, a compound with high affinity for mGluR5 and excellent selectivity over other glutamate receptors. Compound 16m exhibits a favorable PK profile in rats, robust anxiolytic-like effects in three different animal models of fear and anxiety, as well as a good PK/PD correlation.
Texto completo:
1
Colección:
01-internacional
Base de datos:
MEDLINE
Asunto principal:
Péptidos
/
Ansiolíticos
/
Receptores de Glutamato Metabotrópico
/
Amidas
/
Aminopiridinas
Límite:
Animals
/
Humans
Idioma:
En
Revista:
Bioorg Med Chem Lett
Asunto de la revista:
BIOQUIMICA
/
QUIMICA
Año:
2010
Tipo del documento:
Article
País de afiliación:
Suiza