Effects of the calcium release inhibitor dantrolene and the Ca2+-ATPase inhibitor thapsigargin on spinal nociception in rats
Effects of the calcium release inhibitor dantrolene and the Ca2+-ATPase inhibitor thapsigargin on spinal nociception in rats
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DOI：
10.1159/000056087
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发表时间：
2001-01-01
期刊：
影响因子：
3.1
通讯作者：
Menéndez, L
中科院分区：
文献类型：
--
作者：
Alvarez-Vega, M;Baamonde, A;Menéndez, L
在几次大鼠镇痛试验中，描述了鞘内给药丹曲林和塔塔sigargin产生的效果，丹曲林减少细胞内钙储存的释放，塔塔sigargin能够抑制网状Ca2+- atp酶，避免细胞内钙储存，丹曲林（30-300 nmol/大鼠）和塔塔sigargin （3-30 nmol/大鼠）减少伤害性行为(咬、抓、舔；NK1受体激动剂septide（0.5杯）产生的BSL，不影响AMPA（2杯）或NMDA（4杯）诱导的BSL。此外，两种药物在甩尾试验中均引起镇痛，而在福尔马林试验中没有引起镇痛，thapsigargin诱导的抗痛觉作用比dantrolene产生的更强烈和持久，这些结果似乎表明细胞内钙稳态的调节可能是一个有趣的靶点，以诱导脊髓镇痛。版权所有(C) 2001 S. Karger AG，巴塞尔
The effects produced by the intrathecal administration of dantrolene and thapsigargin, measured in several analgesic tests in the rat are described, Dantrolene decreases the release of calcium from intracellular stores and thapsigargin is able to inhibit the reticular Ca2+-ATPase, avoiding intracellular calcium storage, Dantrolene (30-300 nmol/rat) and thapsigargin (3-30 nmol/rat) reduced the nociceptive behavior (biting, scratching, licking; BSL) produced by the NK1 receptor agonist septide (0.5 mug), without affecting the BSL induced by AMPA (2 mug) or NMDA (4 mug), Also, both drugs elicited analgesia in the tail-flick test but not in the formalin test, The antinociceptive effects induced by thapsigargin were more intense and long-lasting than those produced by dantrolene, These results seem to indicate that the intracellular modulation of calcium homeostasis could be an interesting target in order to induce spinal analgesia. Copyright (C) 2001 S. Karger AG, Basel.