Design, Synthesis, and Optimization of Balanced Dual NK1/NK3 Receptor Antagonists.

ABSTRACT: 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.

SUBMITTER: Hanessian S 

PROVIDER: S-EPMC4027792 | biostudies-literature | 2014 May

REPOSITORIES: biostudies-literature