Synthesis and properties of dermorphin and an analog of β‐endorphin containing the dermorphin sequence

Abstract
Dermorphin (I) and [D‐Ala2, Phe3, Gly4, Tyr5, Pro6]‐βc‐EP (II) have been synthesized by the solid‐phase method (β‐EP, camel β‐endorphin). Positions I through 7 of II correspond to the sequence of I. Relative potencies of synthetic peptides in the mouse tail‐flick test for analgesia by the intracerebroventricular route were: human β‐endorphin, 100; camel β‐endorphin, 164; I, 450; II, 440. The dermorphin was about 670 times more potent than morphine in the assay. Peptide II represents a rare instance where the enkephalin moiety of β‐endorphin has been altered to produce a more potent analgesic.