Highly potent, non-basic 5-HT6 ligands. Site mutagenesis evidence for a second binding mode at 5-HT6 for antagonism.
Bioorg Med Chem Lett
; 20(11): 3436-40, 2010 Jun 01.
Article
em En
| MEDLINE
| ID: mdl-20434910
ABSTRACT
A series of 5-HT(6) ligands derived from (R)-1-(amino)methyl-6-(phenyl)sulfonyltetralin was prepared that yielded several non-basic analogs having sub-nanomolar affinity. Ligand structure-activity relationships, receptor point mutation studies, and molecular modeling of these novel ligands all combined to reveal a new alternative binding mode to 5-HT(6) for antagonism.
Texto completo:
1
Coleções:
01-internacional
Base de dados:
MEDLINE
Assunto principal:
Receptores de Serotonina
Idioma:
En
Ano de publicação:
2010
Tipo de documento:
Article