促肾上腺皮质激素片段在体外模拟吗啡的作用。
Adrenocorticotrophic hormone fragments mimic the effect of morphine in vitro.
作者信息
Plomp G J, Van Ree J M
出版信息
Br J Pharmacol. 1978 Oct;64(2):223-7. doi: 10.1111/j.1476-5381.1978.tb17293.x.
Abstract
1 Fragments of the N terminal part of adrenocorticotrophic hormone (ACTH) inhibited the electrically evoked contractions of the mouse vas deferens. This inhibition could be antagonized by naloxone. 2 The same fragments displaced radiolabelled morphine from morphine antiserum. 3 Structure-activity relationship studies showed that in both assay systems the active core is located within the sequence ACTH 7--10. 4 It is postulated that the Trp9 residue and the peptide bond between Trp9 and Gly10 are particularly important for interaction of ACTH fragments with morphine receptors.
摘要
1 促肾上腺皮质激素（ACTH）N端部分的片段可抑制小鼠输精管的电诱发收缩。这种抑制作用可被纳洛酮拮抗。2 相同的片段可从吗啡抗血清中置换出放射性标记的吗啡。3 构效关系研究表明，在这两种检测系统中，活性核心位于ACTH 7-10序列内。4 据推测，Trp9残基以及Trp9和Gly10之间的肽键对于ACTH片段与吗啡受体的相互作用尤为重要。
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