New Dimeric Tetrapeptide Enkephalin AnaloguesHydrophilic Spacer Length and Configuration Affects Potency and Receptor Selectivity

Abstract

synthesized and tested in vitro for pi, d and x receptor affinities. They were found to have potent opioid receptor binding activity. The (25,35)-butanediol bridge configuration yield ed selectivity and high potency for pi and x receptors, while the (2/?,37?)-butanediol bridge configuration yielded high potency and selectivity for < 3 receptors. It thus appears that changes in the length and configuration of the polyhydroxyl bridge in dimeric enkephalin analogues can produce a shift in receptor selectivity profiles and therefore suggest the possibility of developing more selective drugs.