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首页> 外文期刊>Pharmacology, Biochemistry and Behavior >Kappa antinociceptive activity of spiradoline in the cold-water tail-flick assay in rats.
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Kappa antinociceptive activity of spiradoline in the cold-water tail-flick assay in rats.

机译：在大鼠冷水甩尾试验中，螺阿达林的Kappa抗伤害感受活性。

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摘要

Spiradoline (U62066E) a racemic mixture of the two enantiomers U63639(+) and U63640(-), appears to have kappa opioid receptor activity, but the contribution of each enantiomer toward this activity is still in question. To determine the activity of each enantiomer in comparison to the racemic mixture, the three forms were tested in the cold-water tail-flick (CWTF) assay in male Sprague-Dawley rats. Antinociception by spiradoline was completely antagonized by naloxone 0.50 mg/kg, a dose five times that required to antagonize antinociception by fentanyl in this same assay. In a second series of tests, fentanyl-induced antinociception was markedly reduced, while spiradoline-induced antinociception was essentially unchanged. in methadone-tolerant animals. Of the enantiomers, only U63640 produced antinociception, whereas U63639 failed to affect the nociceptive response. Additionally, spiradoline failed to produce antinociception in animals pretreated with norbinaltorphimine (kappa receptor specific), but antinociception was not affected in animals pretreated with beta-funaltrexamine (mu receptor specific). These results show that spiradoline is a full antinociceptive agonist in the CWTF assay and that the effects of the drug are mediated through kappa opioid receptors.
机译：螺旋体（U62066E）是两种对映体U63639（+）和U63640（-）的外消旋混合物，似乎具有κ阿片受体活性，但每种对映体对该活性的贡献仍存在疑问。为了确定与外消旋混合物相比每种对映异构体的活性，在冷水甩尾法（CWTF）中对雄性Sprague-Dawley大鼠进行了三种形式的测试。 spiradoline的抗伤害感受被纳洛酮0.50 mg / kg完全拮抗，该剂量是同一试验中芬太尼拮抗抗伤害感受所需剂量的五倍。在第二系列的测试中，芬太尼诱导的抗伤害感受明显降低，而螺菌灵诱导的抗伤害感受基本保持不变。在耐美沙酮的动物中。在对映异构体中，只有U63640产生抗伤害感受，而U63639则不影响伤害感受性反应。此外，螺菌灵在用降冰片碱（kappa受体特异性）预处理的动物中未能产生抗伤害作用，但在用β-富纳曲明（μ受体特异性）预处理的动物中抗伤害作用不受影响。这些结果表明，螺环素在CWTF分析中是一种完全的镇痛激动剂，并且该药物的作用是通过κ阿片受体介导的。

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