Identification of a new series of non-peptidic NK3 receptor antagonists.

Abstract The identification and structure–activity relationships of 2-aminomethyl-1-aryl cyclopropane carboxamides as novel NK 3 receptor antagonists are reported. The compound series was optimized to give analogues with low nanomolar binding to the NK 3 receptor and brain exposure, leading to activity in vivo in the senktide-induced hypoactivity model in gerbils.