κ激动剂-螺哌丁苯（U62066E）对某些阿片类药物在脊髓水平镇痛活性的影响。
The influence of the kappa agonist-spiradoline (U62066E) on the analgesic activity of some opioids at the spinal level.
作者信息
Stachura Z, Herman Z S
机构信息
Department of Clinical Pharmacology, Medical Academy, Katowice, Poland.
出版信息
Pol J Pharmacol. 1994 Jan-Apr;46(1-2):37-41.
Male Wistar rats were treated with morphine (MP) or pentazocine (PT) subcutaneously (sc) and then intrathecally (it) with a specific kappa receptor agonist spiradoline (U62066E). In another series of experiments methionine-(MENK) or leucine-enkephalin (LENK) were injected it with U62066E simultaneously. Then antinociceptive effect on thermal stimulus was measured 1 h using the tail immersion test. MP or LENK induced analgesia was enhanced by U62066E during the first 30 min of observation. MENK analgesic activity was potentiated by kappa receptor agonist only up to 5 min. U62066E acted biphasically on PT antinociceptive effect. These results suggest that kappa opioid receptors may participate in antinociceptive action of MP and LENK and in small degree for analgesic effect of PT and MENK at the spinal level.
将雄性Wistar大鼠皮下注射吗啡（MP）或喷他佐辛（PT），然后鞘内注射特异性κ受体激动剂螺旋哌丁苯（U62066E）。在另一系列实验中，将蛋氨酸脑啡肽（MENK）或亮氨酸脑啡肽（LENK）与U62066E同时进行鞘内注射。然后，使用尾部浸没法在1小时后测量对热刺激的镇痛作用。在观察的前30分钟内，U62066E增强了MP或LENK诱导的镇痛作用。MENK的镇痛活性仅在5分钟内被κ受体激动剂增强。U62066E对PT的镇痛作用呈双相性。这些结果表明，κ阿片受体可能参与MP和LENK的镇痛作用，并且在一定程度上参与PT和MENK在脊髓水平的镇痛作用。
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