μ（DAGO）和δ（DPDPE）脑啡肽对大鼠的抗惊厥作用。

Anticonvulsant effects of mu (DAGO) and delta (DPDPE) enkephalins in rats.

作者信息

Tortella F C, Echevarria E, Robles L, Mosberg H I, Holaday J W

机构信息

Department of Medical Neurosciences, Walter Reed Army Institute of Research, Washington, DC 20307.

出版信息

Peptides. 1988 Sep-Oct;9(5):1177-81. doi: 10.1016/0196-9781(88)90104-0.

DOI:10.1016/0196-9781(88)90104-0

PMID:2854247

Abstract

The effects of highly selective mu and delta opioid peptide agonists were determined in two rat models of experimentally-induced convulsions, the flurothyl threshold test and the maximal electroshock test. Intracerebroventricular injections of the mu selective enkephalin DAGO (0.3-2.2 nmol) resulted in a dose-related protection in both seizure models. Pretreatment with a low dose of naloxone (29 nmol) or the irreversible mu antagonist beta-FNA (21 nmol), but not the delta opioid antagonist ICI 154,129 (50 nmol), antagonized the anticonvulsant actions of DAGO. Intracerebroventricular injections of the delta selective enkephalin DPDPE (70-140 nmol) also resulted in seizure protection. These effects were selectively antagonized by the delta antagonist ICI 174,864 (2.8 nmol), but not by pretreatment with beta-FNA. Thus, using agonists and antagonists highly selective for mu and delta opioid receptors, anticonvulsant actions of enkephalin have been described against chemically- and electrically-induced convulsions in rats.

摘要

在两种实验性诱发惊厥的大鼠模型（氟烷阈值试验和最大电休克试验）中，测定了高选择性μ和δ阿片肽激动剂的作用。脑室内注射μ选择性脑啡肽DAGO（0.3 - 2.2纳摩尔）在两种癫痫模型中均产生了剂量相关的保护作用。用低剂量纳洛酮（29纳摩尔）或不可逆的μ拮抗剂β - FNA（21纳摩尔）预处理，但不是用δ阿片拮抗剂ICI 154,129（50纳摩尔）预处理，可拮抗DAGO的抗惊厥作用。脑室内注射δ选择性脑啡肽DPDPE（70 - 140纳摩尔）也产生了癫痫保护作用。这些作用被δ拮抗剂ICI 174,864（2.8纳摩尔）选择性拮抗，但β - FNA预处理无此作用。因此，使用对μ和δ阿片受体具有高度选择性的激动剂和拮抗剂，已描述了脑啡肽对大鼠化学诱导和电诱导惊厥的抗惊厥作用。