Effects of intrathecal L- and N-type calcium channel blockers on the antinociception evoked by opioid agonists in the rat tail flick test.

E N Lia, W A Prado
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Abstract

The effects of intrathecal administration of nimodipine or omega-conotoxin GVIA (L- and N-type calcium channel blockers, respectively) alone or followed by DAMGO, DADLE or bremazocine (mu-, delta- and kappa-opioid agonists, respectively) were studied on the rat tail flick test. The N- (16 to 64 pmoles), but not the L-type blocker (60 to 240 pmoles) produced a dose and time-dependent increase in the latency for the tail-flick reflex. DAMGO (30 to 120 pmoles) or bremazocine (190 to 560 pmoles), but not DADLE (50 to 200 pmoles), produced a dose-dependent increase in the latency for the tail-flick reflex. The effect of the highest dose of DAMGO was smaller, while the effects of DADLE and bremazocine were not changed after nimodipine (60 pmoles). The effects of DADLE were significantly potentiated, while the effects of DAMGO and bremazocine were not changed after omega-conotoxin GVIA (16 pmoles). The intrathecal administration of an N-type calcium channel blocker with a delta-opioid agonist seems to be the most effective combination to produce antinociception in the rat tail flick test.

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鞘内L型和n型钙通道阻滞剂对大鼠尾弹试验中阿片激动剂引起的抗感觉的影响。
研究了尼莫地平或ω - concontoxin GVIA(分别为L型和n型钙通道阻滞剂)鞘内单独或随后使用DAMGO、DADLE或布雷马辛(分别为mu-、delta-和kappa-阿片受体激动剂)对大鼠尾轻击试验的影响。N-受体阻滞剂(16 ~ 64 pmol),而l型受体阻滞剂(60 ~ 240 pmol)不产生甩尾反射潜伏期的剂量和时间依赖性增加。DAMGO (30 - 120 pmol)或布雷马辛(190 - 560 pmol),而DADLE (50 - 200 pmol)则不会产生甩尾反射潜伏期的剂量依赖性增加。最高剂量DAMGO的作用较小,而在尼莫地平(60 pmol)后,DADLE和布雷马辛的作用没有变化。在omega- concontoxin GVIA (16 pmol)后,DADLE的作用显著增强,而DAMGO和布雷马辛的作用没有改变。在大鼠甩尾试验中,鞘内给予n型钙通道阻滞剂和阿片受体激动剂似乎是产生抗痛觉的最有效的组合。
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