[Identification of a functionally important dipeptide in sequences of atypical opioid peptides].
The occurrence of individual amino acids and dipeptide fragments in the sequences of 60 known atypical opioid peptides was analyzed. An expressed predominance of Tyr-Pro fragment suggested a high probability of analgesic activity for this dipeptide, and it was experimentally studied. It was shown on somatic and visceral pain sensitivity models that, on the i.p. administration of Tyr-Pro at doses of 1.0-10 mg/kg of body mass, it exhibits an analgesic activity eliminated by naloxone and naloxone methiodide. However, in tests on ileum preparations of guinea pig and mouse vas deferens in vitro, Tyr-Pro was devoid of opioid activity, which proved its indirect influence on opioid receptors.
Guzevatykh
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D000595:Amino Acid Sequence; D000701:Analgesics, Opioid / Q000494:pharmacology; D000818:Animals; D016384:Consensus Sequence; D004151:Dipeptides / Q000737:chemistry* / Q000494:pharmacology; D006168:Guinea Pigs; D066298:In Vitro Techniques; D008297:Male; D051379:Mice; D008969:Molecular Sequence Data; D009119:Muscle Contraction / Q000187:drug effects; D009130:Muscle, Smooth / Q000187:drug effects / Q000502:physiology; D009292:Narcotic Antagonists; D018847:Opioid Peptides / Q000737:chemistry*; D010147:Pain Measurement; D051381:Rats; D043884:Receptor, Cannabinoid, CB1 / Q000037:antagonists & inhibitors / Q000502:physiology; D011957:Receptors, Opioid / Q000502:physiology; D000094942:Nociceptin Receptor
D000701:Analgesics, Opioid; D004151:Dipeptides; D009292:Narcotic Antagonists; D018847:Opioid Peptides; D043884:Receptor, Cannabinoid, CB1; D011957:Receptors, Opioid; D000094942:Nociceptin Receptor