Beta-endorphin-(1-27) is a naturally occurring antagonist to etorphine-induced analgesia.
Beta-endorphin-(1-27) is a naturally occurring antagonist to etorphine-induced analgesia.
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Beta-endorphin-(1-27) 是一种天然存在的埃托啡诱导镇痛拮抗剂。
DOI：
10.1073/pnas.82.10.3178
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发表时间：
1985
影响因子：
11.1
通讯作者：
Li,CH
中科院分区：
文献类型：
--
作者：
Nicolas,P;Li,CH
强效阿片肽 β-内啡肽存在于大脑和垂体中，具有两个相关片段：β-内啡肽-(1-27) 和 β-内啡肽-(1-26)。这些片段保留了大量的阿片受体结合活性，但实际上没有镇痛活性。当同时注射到小鼠脑室内时，β-内啡肽-(1-27) 可抑制 β-内啡肽诱导的和埃托啡诱导的镇痛。在存在 β-内啡肽-(1-27) 的情况下，埃托啡或 β-内啡肽的剂量反应曲线的平行移动表明在相同位点通过竞争产生拮抗作用。其效力比阿片拮抗剂纳洛酮强4-5倍。每只动物剂量高达 500 pmol 时，β-内啡肽-(1-26) 不会拮抗埃托啡或 β-内啡肽的镇痛作用。
The potent opioid peptide beta-endorphin is found in the brain and pituitary with two related fragments, beta-endorphin-(1-27) and beta-endorphin-(1-26). The fragments retain substantial opioid-receptor binding activity but are virtually inactive analgesically. beta-Endorphin-(1-27) inhibits beta-endorphin-induced and etorphine-induced analgesia when coinjected intracerebroventricularly into mice. Antagonism by competition at the same site(s) is suggested from parallel shifts of the dose-response curves of etorphine or beta-endorphin in the presence of beta-endorphin-(1-27). Its potency is 4-5 times greater than that of the opiate antagonist naloxone. beta-Endorphin-(1-26) does not antagonize the antinociceptive action of etorphine or beta-endorphin in doses up to 500 pmol per animal.