2,3-Diarylthiophenes as selective EP1 receptor antagonists.
Bioorg Med Chem Lett
; 15(4): 1155-60, 2005 Feb 15.
Article
en En
| MEDLINE
| ID: mdl-15686932
ABSTRACT
The synthesis and the EP(1) receptor binding affinity of 2,3-diarylthiophene derivatives are described. The evaluation of the structure-activity relationship (SAR) in this series led to the identification of compounds 4, 7, and 12a, which exhibit high affinity for the human EP(1) receptor and a selectivity greater than 100-fold against the EP(2), EP(3), EP(4), DP, FP, and IP receptors and greater than 25-fold versus the TP receptor. These three antagonists present good pharmacokinetics in rats and significant differences in the way they are distributed in the brain.
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Banco de datos:
MEDLINE
Asunto principal:
Tiofenos
/
Receptores de Prostaglandina E
Límite:
Animals
/
Humans
Idioma:
En
Año:
2005
Tipo del documento:
Article