[Dermorphin: synthesis of analogs and structuro-functional relations]

The review analyzes structure-activity relations among dermorphin analogues. Dermorphin (Tyr-D-Ala-Phe-Gly-Tyr-Pro-Ser-NH2) is one of natural opioid peptides having a unique structure and exerting a very potent and prolonged antinociceptive effect. Methods of dermorphin synthesis are summarized together with data on more than 300 dermorphin-like peptides: the physico-chemical characteristics and data on opioid tests in vitro and in vivo are discussed. Based on these studies, conclusions have been drawn on the functional role of each amino acid residue in the dermorphin molecule and on modifications leading to analogues with high and differential opioid activity.