Analgesic effects of intracerebroventricular administration of calcium channel blockers in mice.

H F Miranda, T Pelissier, F Sierralta
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引用次数: 30

Abstract

1. The antinociceptive action of calcium channel blockers administered intracerebroventricularly to mice using the acetic acid writhing test was studied. 2. The drugs produced dose-dependent inhibition of the number of writhes induced by the intraperitoneal administration of 10 ml/kg of 0.6% acetic acid. 3. The CaCBs may be ranked from most to least potent as follows: verapamil > nimodipine > diltiazem > flunarizine > nifedipine > cinnarizine. 4. Since naloxone pretreatment was not able to inhibit the antinociception produced by CaCBs an opioid mechanism of action is excluded. 5. It is suggested that CaCBs can induce analgesia through a decrease in cellular Ca2+ availability, increasing the nociceptive threshold.

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小鼠脑室内钙通道阻滞剂的镇痛作用。
1. 采用醋酸扭体实验研究了钙通道阻滞剂脑室内给药对小鼠的抗痛觉作用。2. 药物对腹腔注射0.6%醋酸10 ml/kg诱导的扭体数量有剂量依赖性抑制作用。3.cacb的效价由高到低依次为:维拉帕米>尼莫地平>地尔硫卓>氟桂利嗪>硝苯地平>桂利嗪。4. 由于纳洛酮预处理不能抑制cacb产生的抗痛觉作用,因此排除了阿片作用机制。5. 这表明,CaCBs可以通过降低细胞Ca2+可用性,增加伤害阈值来诱导镇痛。
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