8-Sulfonyl-substituted tetrahydro-1H-pyrido[4,3-b]indoles as 5-HT6 receptor antagonists.
Eur J Med Chem
; 45(2): 782-9, 2010 Feb.
Article
em En
| MEDLINE
| ID: mdl-19939513
ABSTRACT
A series of novel 8-sulfonyl-substituted 2,3,4,5-tetrahydro-1H-pyrido[4,3-b]indoles (THPI) has been synthesized and their ability to interact with 5-HT(6) receptors evaluated in cell-based and radioligand binding assays. Amongst evaluated THPIs, compounds 9.HCl and 20.HCl have been identified as the most potent 5-HT(6) receptor antagonists with K(i) values equal to 2.1 nM and 5.7 nM and IC(50) values (functional assay) equal to 15 nM and 78 nM, respectively. Affinities of these two compounds for several serotonin receptors in the competitive radioligand binding assays as well as their specificity profiles against a panel of therapeutic targets have been determined.
Texto completo:
1
Coleções:
01-internacional
Base de dados:
MEDLINE
Assunto principal:
Antagonistas da Serotonina
/
Sulfonas
/
Receptores de Serotonina
/
Indóis
Limite:
Humans
Idioma:
En
Revista:
Eur J Med Chem
Ano de publicação:
2010
Tipo de documento:
Article
País de afiliação:
Federação Russa