β-内啡肽诱导的镇痛作用受到β-内啡肽合成类似物的抑制。
beta-Endorphin-induced analgesia is inhibited by synthetic analogs of beta-endorphin.
作者信息
Nicolas P, Hammonds R G, Li C H
出版信息
Proc Natl Acad Sci U S A. 1984 May;81(10):3074-7. doi: 10.1073/pnas.81.10.3074.
Abstract
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 in vivo analgesic potency ratio has been demonstrated. A parallel shift of the dose-response curve for analgesia to the right was observed when either beta h-EP or [ Trp27 ] -beta h-EP was coinjected with various doses of [Gln8, Gly31 ]-beta h-EP-Gly-Gly-NH2, [Arg9,19,24,28,29]-beta h-EP, or [ Cys11 ,26, Phe27 , Gly31 ]-beta h-EP. It was estimated that the most potent antagonist, [Gln8, Gly31 ]-beta h-EP-Gly-NH2, is at least 200 times more potent than naloxone.
摘要
已证实，具有高体外阿片受体结合与体内镇痛效价比的合成β-人内啡肽（βh-EP）类似物对βh-EP诱导的镇痛具有竞争性拮抗作用。当βh-EP或[Trp27]-βh-EP与不同剂量的[Gln8，Gly31]-βh-EP-Gly-Gly-NH2、[Arg9,19,24,28,29]-βh-EP或[Cys11,26,Phe27,Gly31]-βh-EP共同注射时，观察到镇痛剂量-反应曲线平行右移。据估计，最有效的拮抗剂[Gln8，Gly31]-βh-EP-Gly-NH2的效力至少比纳洛酮高200倍。
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