The SAR development of dihydroimidazoisoquinoline derivatives as phosphodiesterase 10A inhibitors for the treatment of schizophrenia.
Bioorg Med Chem Lett
; 22(7): 2585-9, 2012 Apr 01.
Article
en En
| MEDLINE
| ID: mdl-22377514
ABSTRACT
The identification of potent and orally active dihydroimidazoisoquinolines as PDE 10A inhibitors is reported. The SAR development led to the discovery of compound 35 as a potent, selective, and orally active PDE10A inhibitor. Compound 35 inhibited MK-801-induced hyperactivity at 3mg/kg and displayed a 10-fold separation between the minimal effective doses for inhibition of MK-801-induced hyperactivity and hypolocomotion in rats.
Texto completo:
1
Bases de datos:
MEDLINE
Asunto principal:
Inhibidores de Fosfodiesterasa
/
Psicotrópicos
/
Hidrolasas Diéster Fosfóricas
/
Hipercinesia
/
Imidazoles
/
Isoquinolinas
Tipo de estudio:
Prognostic_studies
Límite:
Animals
/
Humans
/
Male
Idioma:
En
Revista:
Bioorg Med Chem Lett
Asunto de la revista:
BIOQUIMICA
/
QUIMICA
Año:
2012
Tipo del documento:
Article
País de afiliación:
Estados Unidos