Derivatives of beta-casomorphins with high analgesic potency.

  title={Derivatives of beta-casomorphins with high analgesic potency.},
  author={Hansj{\"u}rgen Matthies and Heidi Stark and Bianka Hartrodt and H L Ruethrich and H T Spieler and Andreas Barth and Klaus Neubert},
  volume={5 3},
Beta-casomorphin (5) Tyr-Pro-Phe-Pro-Gly, a partial sequence of bovine beta-casein with moderate opioid properties and mu-receptor affinity, was modified by substituting for the natural L-amino acids their D-analogs, and D-pipecolic acid, as well as by amidation of the C-terminal. Substitution of D-Pro or D-pipecolic acid for L-Pro4 considerably increased the analgesic action and the potency on guinea-pig ileum of beta-casomorphin (5) as well as of casomorphin [4] amide. The resulting D-Pro4… CONTINUE READING

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