Extremely long-lasting antagonistic actions of nor-binaltorphimine (nor-BNI) in the mouse tail-flick test.
Extremely long-lasting antagonistic actions of nor-binaltorphimine (nor-BNI) in the mouse tail-flick test.
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发表时间：
1992-03
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通讯作者：
Peter J. Horan;J. Taylor;Henry I. Yamamura;F. Porreca
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作者：
Peter J. Horan;J. Taylor;Henry I. Yamamura;F. Porreca
采用小鼠甩尾试验作为终点，研究了κ受体拮抗剂nor-binaltorphimine（nor-BNI）对选择性阿片受体激动剂引起的镇痛作用的拮抗作用持续时间。Nor-BNI（1 nmol，i. c. v.，约20分钟）拮抗阿片κ激动剂（5 α，7 α，8 β）-（-）-N-甲基-N-（7-（1-吡咯烷基）-1-氧杂螺（4，5）癸-8-基）苯乙酰胺（U69，593）（70 nmol i. c. v.）或布马佐辛（25 nmol i. c. v.），但不拮抗μ阿片样物质选择性[D-Ala 2，NMePhe 4，Gly-ol]脑啡肽或δ阿片样物质选择性[D-Pen 2，D-Pen 5]脑啡肽产生的抗伤害感受。用nor-BNI（1 nmol i.c.v.）拮抗U69，593和布马佐辛的抗伤害感受作用长达28天。在所有的预处理时间，这些κ受体激动剂的镇痛剂量-反应线被移位到不同程度的权利，以平行的方式;增加的U69，593和布马佐辛镇痛剂量-反应线的位移在1和3天后，观察到一个单一的nor-BNI预处理，逐渐返回到控制水平后，在以后的时间预处理。将nor-BNI的剂量增加至10 nmol仅产生μ选择性激动剂[D-Ala 2，NMePhe 4，Gly-ol]脑啡肽和δ选择性激动剂[D-Pen 2，D-Pen 5]脑啡肽的等伤害感受剂量的短暂阻断（在nor-BNI预处理后20-30分钟）。（250字处删节）
The duration of antagonistic action of nor-binaltorphimine (nor-BNI), a kappa antagonist, of antinociception resulting from selective opioid agonists, was examined using the mouse tail-flick assay as the endpoint. Nor-BNI (1 nmol, i.c.v. at -20 min) antagonized equiantinociceptive doses of the opioid kappa agonists (5 alpha,7 alpha,8 beta)-(-)-N-methyl-N-(7-(1-pyrrolidinyl)-1-oxaspiro (4,5)dec-8-yl) benzeneacetamide (U69,593) (70 nmol i.c.v.) or bremazocine (25 nmol i.c.v.), but did not antagonize antinociception produced by the mu opioid-selective [D-Ala2, NMePhe4, Gly-ol]enkephalin or the delta opioid-selective [D-Pen2, D-Pen5]enkephalin. Pretreatment with nor-BNI (1 nmol i.c.v.) antagonized the antinociceptive effects of U69,593 and bremazocine for up to 28 days. At all pretreatment times, the antinociceptive dose-response lines for these kappa agonists were displaced to the right to various degrees in a parallel fashion; an increasing rightward displacement of the U69,593 and bremazocine antinociceptive dose-response lines was observed at 1 and 3 days after a single nor-BNI pretreatment, with a gradual return toward the control level at later times after pretreatment. Increasing the dose of nor-BNI to 10 nmol produced only a transient blockade of equiantinociceptive doses of the mu selective agonist [D-Ala2, NMePhe4, Gly-ol]enkephalin and the delta selective agonist [D-Pen2, D-Pen5]enkephalin (at 20-30 min post-nor-BNI pretreatment).(ABSTRACT TRUNCATED AT 250 WORDS)