The histamine-releasing effect of dynorphin and other peptides possessing Arg-Pro sequences.
The basic opioid peptide dynorphin was tested for histamine-releasing activity on peritoneal rat mast cells. Dynorphin was found to induce a dose-dependent histamine release from the mast cells. The threshold concentration was 2 X 10(-7) M and release was maximal (40% of total) at 2 X 10(-6) M of the peptide. The dynorphin-induced histamine release was a very rapid process completed within 10 seconds at 37 degrees C. The release was independent of extracellular calcium. Experiments with naloxone and a specific kappa-agonist (U-50,488H) gave results indicating that the dynorphin induced histamine release was probably not mediated through opioid kappa-receptors. A couple of other Arg-Pro containing peptides of different origin were also screened for histamine-releasing activity. Most of these peptides elicited a more or less pronounced histamine release, provided the peptide contained more than 5 amino acids, suggesting that the Arg-Pro sequence is of importance for the histamine-releasing effect of peptides such as dynorphin.
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D000595:Amino Acid Sequence; D000818:Animals; D001120:Arginine; D004305:Dose-Response Relationship, Drug; D004399:Dynorphins / Q000494:pharmacology*; D006636:Histamine Release / Q000187:drug effects*; D066298:In Vitro Techniques; D008297:Male; D009270:Naloxone / Q000494:pharmacology; D009496:Neurotensin / Q000494:pharmacology; D009842:Oligopeptides / Q000494:pharmacology; D010455:Peptides / Q000494:pharmacology*; D011392:Proline; D051381:Rats; D011919:Rats, Inbred Strains; D011957:Receptors, Opioid / Q000187:drug effects; D013722:Teprotide
D009842:Oligopeptides; D010455:Peptides; D011957:Receptors, Opioid; D009270:Naloxone; D009496:Neurotensin; D004399:Dynorphins; D001120:Arginine; D011392:Proline; D013722:Teprotide