1.
ACS Med Chem Lett
; 5(5): 550-5, 2014 May 08.
Artículo
en Inglés
| MEDLINE
| ID: mdl-24900878
RESUMEN
In connection with a program directed at potent and balanced dual NK1/NK3 receptor ligands, a focused exploration of an original class of peptidomimetic derivatives was performed. The rational design and molecular hybridization of a novel phenylalanine core series was achieved to maximize the in vitro affinity and antagonism at both human NK1 and NK3 receptors. This study led to the identification of a new potent dual NK1/NK3 antagonist with pK i values of 8.6 and 8.1, respectively.