[Synthesis and enzymatic degradation of beta-casomorphin-5 (author's transl)].
The authors describe the synthesis of beta-casomorphine-5 (Tyr-Pro-Phe-Pro-Gly) by segment condensation and stepwise building-up. Intracerebroventricular application of the pentapeptide to the rat produces a long-lasting analgesia against thermal stimuli (which can be inhibited by naloxone) and counteracts the extinction of a passive avoidance reaction for no less than 4 days following post-shock application. beta-Casomorphin-5 is very rapidly degraded by dipeptidylpeptidase IV; the degradation starts from the N-terminus giving dipeptides. The degradation products are competitive inhibitors of this enzyme.
D000700:Analgesics; D000818:Animals; D001362:Avoidance Learning / Q000187:drug effects; D001711:Biotransformation; D004723:Endorphins / Q000037:antagonists & inhibitors / Q000138:chemical synthesis* / Q000378:metabolism; D005108:Extinction, Psychological / Q000187:drug effects; D007276:Injections, Intraventricular; D007700:Kinetics; D009270:Naloxone / Q000494:pharmacology; D010446:Peptide Fragments; D051381:Rats
D000700:Analgesics; D004723:Endorphins; D010446:Peptide Fragments; D009270:Naloxone; C034812:beta-casomorphin 5
Synthese und enzymatischer Abbau von beta-Casomorphin-5.