No abstract

No abstract

In connection with a program directed at potent and balanced dual NK 1 /NK 3 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 NK 1 and NK 3 receptors. This study led to the identification of a new potent dual NK 1 /NK 3 antagonist with pK i values of 8.6 and 8.1, respectively.