摘要
镁已经显示出对神经性和炎症性疼痛动物模型的镇痛作用。它也被证明施加对人体的镇痛效果的条件下呈现急性(术后疼痛)和慢性(神经性)疼痛。众所周知,镁是一种生理拮抗剂的N-甲基-D-天冬氨酸(NMDA)受体离子通道和NMDA受体在中枢敏化中起关键作用,其主要机制,镁生产其镇痛作用被认为是脊髓NMDA受体阻断剂。此外,镁阻止钙通道和调节钾通道。一氧化氮(NO)通路的活化可能在硫酸镁体全身镇痛作用的重要作用,但不是对炎性疼痛的内脏模型。虽然有一段时间,肌肉,静脉注射和皮下注射硫酸镁在人类,腹腔注射啮齿动物产生局部疼痛的感觉,这一行动的机制是最近才阐明。结果表明,皮下注射等渗溶液,phadjusted(7.4)硫酸镁(6.2%)的大鼠产生局部外周疼痛外设通过TRPA1,激活TRPV1,TRPV4和NMDA受体和第疼痛动物模型的周边产品,镁被证明是通过作用于不同的离子通道和无通路,发挥镇痛和早期痛觉的影响,但确切机制仍有待研究。
关键词: 镁,疼痛模型,止疼药,NMDA受体,一氧化氮,TRP受体。
Current Medicinal Chemistry
Title:Magnesium in Pain Research: State of the Art
Volume: 24 Issue: 4
关键词: 镁,疼痛模型,止疼药,NMDA受体,一氧化氮,TRP受体。
摘要: Magnesium has been shown to produce an antinociceptive effect on animal models of neuropathic and inflammatory pain. It has also been shown to exert an analgesic effect on humans in conditions presenting acute (postoperative pain) and chronic (neuropathic) pain. As it is known that magnesium is a physiological antagonist of the N-methyl-Daspartate (NMDA) receptor ion channel, and that the NMDA receptor plays a key role in central sensitization, the primary mechanism through which magnesium produces its analgesic effect is believed to be blockade of the NMDA receptor in the spinal cord. In addition, magnesium blocks calcium channels and modulates potassium channels. The activation of the nitric oxide (NO) pathway could have an important role in the antinociceptive effects of systemic magnesium sulfate in the somatic, but not in the visceral model of inflammatory pain. Although it is known for some time that intramuscular, intravenous and subcutaneous injections of magnesium sulfate in humans, and intraperitoneal injection in rodents produce local pain sensation, the mechanism of this action was elucidated only recently. It was demonstrated that subcutaneous injection of an isotonic, pHadjusted (7.4) solution of magnesium sulfate (6.2%) to rats produces local peripheral pain via activation of peripheral TRPA1, TRPV1, TRPV4 and NMDA receptors and peripheral production of NO. In animal models of pain, magnesium has been shown to exert both antinociceptive and pronociceptive effects by acting on different ion channels and NO pathways, however, the precise mechanisms remain to be elucidated.
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Cite this article as:
Magnesium in Pain Research: State of the Art, Current Medicinal Chemistry 2017; 24 (4) . https://dx.doi.org/10.2174/0929867323666161213101744
DOI https://dx.doi.org/10.2174/0929867323666161213101744 |
Print ISSN 0929-8673 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-533X |
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