beta-Endorphin-induced analgesia is inhibited by synthetic analogs of beta-endorphin

摘要: Competitive antagonism of human beta-endorphin (beta h-EP)-induced analgesia by synthetic beta h-EP analogs with high in vitro opiate receptor binding to vivo analgesic potency ratio has been demonstrated. A parallel shift the dose-response curve for right was observed when either or [ Trp27 ] -beta coinjected various doses [Gln8, Gly31 ]-beta h-EP-Gly-Gly-NH2, [Arg9,19,24,28,29]-beta h-EP, Cys11 ,26, Phe27 , h-EP. It estimated that most potent antagonist, h-EP-Gly-NH2, is at least 200 times more than naloxone.