Synthesis and properties of beta h-endorphin analogs containing the dynorphin-(1-13) sequence.
Two analogs of beta h-endorphin containing dynorphin-(5-13) or dynorphin-(6-13) sequence have been synthesized by the solid-phase method. Biological activities of the analogs have also been investigated. It was found that the opiate activity is about three times more than beta h-endorphin in the guinea pig ileum assay. Both analgesic potency and opiate receptor-binding activity of the analogs are lower when compared with beta h-endorphin. However, the analogs have interesting behavioral effects in mice.
D000700:Analgesics; D000818:Animals; D001522:Behavior, Animal / Q000187:drug effects; D004399:Dynorphins; D004723:Endorphins / Q000138:chemical synthesis* / Q000378:metabolism / Q000494:pharmacology; D006168:Guinea Pigs; D007082:Ileum / Q000187:drug effects; D066298:In Vitro Techniques; D008297:Male; D051379:Mice; D009119:Muscle Contraction / Q000187:drug effects; D010446:Peptide Fragments; D011957:Receptors, Opioid / Q000378:metabolism
D000700:Analgesics; D004723:Endorphins; D010446:Peptide Fragments; D011957:Receptors, Opioid; C026843:dynorphin (1-13); D004399:Dynorphins