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所选类皮啡肽的阿片受体结合特征

Opioid receptor binding profile of selected dermorphin-like peptides.

作者信息

Rossi A C, de Castiglione R, Perseo G

出版信息

Peptides. 1986 Sep-Oct;7(5):755-9. doi: 10.1016/0196-9781(86)90091-4.

Abstract

The receptor binding profile of a selected group of dermorphin-like peptides was determined and correlated with the results of the guinea pig ileum (GPI) and mouse vas deferens (MVD) bioassays and with the currently used antinociception tests in the rat. For the peptides with the characteristic dermorphin D-Ala2-Phe3-Gly4 sequence, a linear negative correlation was found between the reciprocal of sodium shift and relative affinity for the mu-type opioid receptor. For the same peptides, a positive correlation was evidenced between relative potency on GPI and MVD and relative affinity for mu- and delta-type receptors, respectively.

摘要

测定了一组选定的类皮啡肽的受体结合谱,并将其与豚鼠回肠(GPI)和小鼠输精管(MVD)生物测定结果以及目前在大鼠中使用的抗伤害感受试验结果进行了关联。对于具有特征性皮啡肽D-Ala2-Phe3-Gly4序列的肽,发现钠移位倒数与对μ型阿片受体的相对亲和力之间呈线性负相关。对于相同的肽,分别证明了在GPI和MVD上的相对效价与对μ型和δ型受体的相对亲和力之间呈正相关。

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