Abstract

In the present study, seven novel dimeric analogues of endomorphin-2 with longer spacers were designed and synthesized. Through dimerization, their affinity for δ-opioid receptor was mostly increased, especially the δ-opioid receptor preferred dimeric analogue, DEM12. The results were confirmed by the in vitro bioassay. The structure-activity relationships were also discussed.

Keywords: Endomorphin-2, Dimerization, analogue, Structure-activity relationships, Opioid receptor, balanced agonist