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SUMMARYSolid phase syntheses of analogues of the opioid heptapeptide dermorphin (H-Tyr-DAla-Phe-Gly-Tyr-Pro-Ser-NH2) containing in the first position 3-aminotyrosine, 3-nitrotyrosine, 4-aminophenylalanine, or nucleoamino acids, 3-(uracilyl-1)alanine, 3-(thyminyl-1)alanine and 3-(6-methyluracilyl-1)alanine are described. The receptor binding properties and analgesic activity of the analogues were examined in comparison with dermorphin. All analogues showed low opioid activity in the binding assays with respect to Ix-and g-receptors. The peptide containing 3-(thyminyl-1)alanine demonstrated a high analgesic activity in different tests when administered intracisternally in mice.