Abstract Two partially modified retro-inverso analogues of Leu-enkephalin in which the peptide bond between Gly 3-Phe 4 was reversed resulted from the incorporation of the Gly 3 ψ (NH-CO) Phe 4 unit. The presence of racemic 2-benzylmalonyl residue led to diastereomeric mixtures of analogues; H-Tyr-D-Ala-gGly-(RS)-mPhe-Leu-NH 2 (I) and H-Tyr- Gly-gGly-(RS)-mPhe-Leu-NH 2 (II). Analogue I was more potent than analogue II in the ...