Peptides having potent antagonist and agonist bioactivities at melanocortin receptors

Abstract

Cyclic lactam peptides, seven amino acids in length, having D-2'-naphthylalanine (D-2'-Nal) or D-para-iodo-phenylalanine D-(p-I)Phe at position 4 of the peptide provided potent and specific antagonists of the two neural melanocortin receptors and of the peripheral receptor. In particular, the peptide ##STR1## was found to be a potent antagonist of the MC3 and MC4 receptors with partial agonist activity, and a full agonist of the MC1 and MC5 receptors; the peptide ##STR2## was found to be a potent antagonist of the MC3 and MC4 receptors with partial agonist activity. Both peptides have antagonist activities in the classical frog skin bioassay for pigmentation at the MC1 receptor.

Dependencies are inferred from the claim text.