Dehydro‐enkephalins

The Gly3 residue in Gly2- and D-Ala2-enkephalins has been replaced by delta Ala3 and Ser3 in order to examine the effect on binding to the delta and mu opiate receptors. [D-Ala2, delta Ala3, Leu5]-enkephalin maintains most of its receptor binding affinities for both sites. It is suggested that the proper conjunctions of positions 2 and 3 of the enkephalin sequence are important to receptor preference and that position 3 may have a very specific interaction with the delta receptor. The in vivo analgesic and CNS activities of the peptides are also discussed.