Identification of a new series of non-peptidic NK3 receptor antagonists.
Bioorg Med Chem Lett
; 21(5): 1498-501, 2011 Mar 01.
Article
em En
| MEDLINE
| ID: mdl-21292483
ABSTRACT
The identification and structure-activity relationships of 2-aminomethyl-1-aryl cyclopropane carboxamides as novel NK(3) receptor antagonists are reported. The compound series was optimized to give analogues with low nanomolar binding to the NK(3) receptor and brain exposure, leading to activity in vivo in the senktide-induced hypoactivity model in gerbils.
Texto completo:
1
Base de dados:
MEDLINE
Assunto principal:
Ácidos Carboxílicos
/
Receptores da Neurocinina-3
/
Ciclopropanos
/
Amidas
Idioma:
En
Ano de publicação:
2011
Tipo de documento:
Article