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含二甲苯桥的DPDPE肽类似物的阿片受体活性与镇痛效力

Opioid Receptor Activity and Analgesic Potency of DPDPE Peptide Analogues Containing a Xylene Bridge.

作者信息

Stefanucci Azzurra, Novellino Ettore, Mirzaie Sako, Macedonio Giorgia, Pieretti Stefano, Minosi Paola, Szűcs Edina, Erdei Anna I, Zádor Ferenc, Benyhe Sándor, Mollica Adriano

机构信息

Dipartimento di Farmacia, Università di Chieti-Pescara "G. d'Annunzio", Via dei Vestini 31, 66100 Chieti, Italy.

Dipartimento di Farmacia, Università di Napoli "Federico II", Via D. Montesano, 49, 80131 Naples, Italy.

出版信息

ACS Med Chem Lett. 2017 Mar 14;8(4):449-454. doi: 10.1021/acsmedchemlett.7b00044. eCollection 2017 Apr 13.

DOI:10.1021/acsmedchemlett.7b00044
PMID:28435535
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC5392763/
Abstract

d-Pen,d-Pen enkephalin (DPDPE) is one of the most selective synthetic peptide agonists targeting the δ-opioid receptor. Three cyclic analogues of DPDPE containing a xylene bridge in place of disulfide bond have been synthesized and fully characterized as opioid receptors agonists. The activity was investigated showing a good affinity of - for μ- and δ-receptors. biological assays revealed that is the most potent analogue with the ability to maintain high level of analgesia from 15 to 60 min following intracerebroventricular (i.c.v.) administration, whereas DPDPE was slightly active until 45 min. Compound induced long lasting analgesia also after subcutaneous administration, whereas DPDPE was inactive.

摘要

D-青霉胺、D-青霉胺脑啡肽（DPDPE）是最具选择性的靶向δ-阿片受体的合成肽激动剂之一。已合成了三种含有二甲苯桥代替二硫键的DPDPE环类似物，并将其完全表征为阿片受体激动剂。研究了其活性，结果表明其对μ-和δ-受体具有良好的亲和力。生物学试验表明，[具体化合物]是最有效的类似物，在脑室内（i.c.v.）给药后15至60分钟能够维持高水平的镇痛效果，而DPDPE在45分钟之前仅有轻微活性。化合物[具体化合物]皮下给药后也能诱导持久的镇痛作用，而DPDPE则无活性。

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