Agonist-based, receptor-type selective opioid peptides containing an alkylating moiety

Our team has a long-held tradition of synthesizing agonist-based opioid peptides containing an alkylating moiety (e.g. 1-3) to facilitate, among other projects, the isolation of opioid receptor(s) (4). The presented data represent a kind of summary of these synthetic and pharmacological activities, producing Tyr-D-Ala-Gly-MePhe-chloromeihyl ketone (DAMCK), Tyr-D-Ala-Gly-PheAsp-β-chloromethyl ketone (DAACK) and Melphalan 1 -D-Ala-Gly-Phe-Leu-OH (Mel 1 -DALE) and their nearest non-alkylating structural relatives, with a more detailed description of the latter pair which represent the most recent developments