Tortella F C, Holaday J W
Dept. of Medical Neurosciences, Walter Reed Army Inst. of Res., Washington, D.C. 20307-5100.
NIDA Res Monogr. 1986;75:539-42.
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.
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。
