Bicyclic heteroarylpiperazines as selective brain penetrant 5-HT6 receptor antagonists.
Bioorg Med Chem Lett
; 15(21): 4867-71, 2005 Nov 01.
Article
en En
| MEDLINE
| ID: mdl-16143522
ABSTRACT
Starting from the potent and selective but poorly brain penetrant 5-HT6 receptor antagonist SB-271046, a successful strategy for improving brain penetration was adopted involving conformational constraint with concomitant reduction in hydrogen bond count. This provided a series of bicyclic heteroarylpiperazines with high 5-HT6 receptor affinity. 5-Chloroindole 699929 combined high 5-HT6 receptor affinity with excellent brain penetration and also had good oral bioavailability in both rat and dog.
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Banco de datos:
MEDLINE
Asunto principal:
Piperazinas
/
Antagonistas de la Serotonina
/
Encéfalo
/
Receptores de Serotonina
Límite:
Animals
Idioma:
En
Año:
2005
Tipo del documento:
Article