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Bioorg Med Chem Lett
; 18(2): 716-20, 2008 Jan 15.
Artículo
en Inglés
| MEDLINE
| ID: mdl-18061443
RESUMEN
Antagonism of the bradykinin B(1) receptor represents a potential treatment for chronic pain and inflammation. Novel antagonists incorporating alpha-hydroxy amides were designed that display low-nanomolar affinity for the human bradykinin B(1) receptor and good bioavailability in the rat and dog. In addition, these functionally active compounds show high passive permeability and low susceptibility to phosphoglycoprotein mediated efflux, predictive of good CNS exposure.