From bradykinin B2 receptor antagonists to orally active and selective bradykinin B1 receptor antagonists.
J Med Chem
; 55(6): 2574-84, 2012 Mar 22.
Article
em En
| MEDLINE
| ID: mdl-22369198
ABSTRACT
The bradykinin (BK) B1 receptor is an attractive target for the treatment of chronic pain and inflammation. Starting from a dual B1 and B2 antagonist, novel antagonists were designed that display low-nanomolar affinity for human B1 receptor and selectivity over B2. Initially, potent imidazoline derivatives were studied, but these compounds suffered from low bioavailability. This issue could be overcome by the use of less basic amino derivatives leading to orally active compounds.
Texto completo:
1
Coleções:
01-internacional
Base de dados:
MEDLINE
Assunto principal:
Piperazinas
/
Piperidinas
/
Antagonistas de Receptor B1 da Bradicinina
/
Antagonistas de Receptor B2 da Bradicinina
/
Analgésicos
Limite:
Animals
/
Humans
/
Male
Idioma:
En
Ano de publicação:
2012
Tipo de documento:
Article