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强啡肽A(1-13):大鼠三氟乙醚试验中的体内阿片类拮抗剂作用及非阿片类抗惊厥作用

Dynorphin A (1-13): in vivo opioid antagonist actions and non-opioid anticonvulsant effects in the rat flurothyl test.

作者信息

Tortella F C, Holaday J W

机构信息

Dept. of Medical Neurosciences, Walter Reed Army Inst. of Res., Washington, D.C. 20307-5100.

出版信息

NIDA Res Monogr. 1986;75:539-42.

PMID:2893282
Abstract

Dynorphin A (1-13) acutely elevated the seizure threshold (ST) to the convulsant flurothyl, and this action was not blocked by naloxone. Increases in ST were also observed following i.c.v. injections of the non-opioid fragment dynorphin A (3-13). Pretreatment with dynorphin A (1-13), but not dynorphin A (3-13), non-competitively blocked the anticonvulsant effect of the mu selective opioid DAGO. Furthermore, pretreatment with dynorphin A (1-13) antagonized the delta antagonist properties of naloxone or ICI 154,129 in this seizure model. Thus, in addition to its non-opioid anticonvulsant effects, dynorphin A (1-13) exhibits unique antagonist actions which appear to be specific for the active opioid fragment.

摘要

强啡肽A(1 - 13)能使对惊厥剂氟烷的癫痫发作阈值(ST)急性升高,且这一作用不受纳洛酮阻断。脑室内注射非阿片类片段强啡肽A(3 - 13)后也观察到ST升高。用强啡肽A(1 - 13)预处理,但不用强啡肽A(3 - 13)预处理,可非竞争性地阻断μ选择性阿片类药物DAGO的抗惊厥作用。此外,在该癫痫模型中,用强啡肽A(1 - 13)预处理可拮抗纳洛酮或ICI 154,129的δ拮抗剂特性。因此,除了其非阿片类抗惊厥作用外,强啡肽A(1 - 13)还表现出独特的拮抗剂作用,这些作用似乎对活性阿片类片段具有特异性。

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