Human leumorphin is a potent, kappa opioid receptor agonist.
The opioid activity and opioid receptor type specificity of synthetic human leumorphin were studied in vitro. Human leumorphin inhibited the contraction of the myenteric plexus-longitudinal muscle preparation of the guinea pig ileum and was similar in opioid potency to porcine leumorphin. This action of human leumorphin was antagonized less effectively by naloxone than by the opiate antagonist Mr 2266. Human leumorphin also inhibited the contraction of the rabbit vas deferens which has only the kappa-type opioid receptor. It is concluded that human leumorphin has potent opioid activity and acts as an agonist at the kappa-type opioid receptor, like porcine leumorphin and other peptides derived from preproenkephalin B.
D000818:Animals; D001575:Benzomorphans / Q000494:pharmacology; D003864:Depression, Chemical; D004399:Dynorphins / Q000031:analogs & derivatives / Q000494:pharmacology; D004723:Endorphins / Q000494:pharmacology; D004745:Enkephalins / Q000037:antagonists & inhibitors / Q000494:pharmacology*; D006168:Guinea Pigs; D006801:Humans; D007082:Ileum / Q000187:drug effects; D008297:Male; D009270:Naloxone / Q000494:pharmacology; D011498:Protein Precursors / Q000037:antagonists & inhibitors / Q000494:pharmacology*; D011817:Rabbits; D011957:Receptors, Opioid / Q000187:drug effects*; D017473:Receptors, Opioid, kappa; D013552:Swine; D014649:Vas Deferens / Q000187:drug effects
D001575:Benzomorphans; D004723:Endorphins; D004745:Enkephalins; D011498:Protein Precursors; D011957:Receptors, Opioid; D017473:Receptors, Opioid, kappa; D009270:Naloxone; C027247:MR 2266; D004399:Dynorphins; C036200:rimorphin; C033660:preproenkephalin