Sorkin Linda S, Doom Carmen M, Maruyama Karly P, Nanigian Danielle B
Department of Anesthesiology, UCSD School of Medicine, 9500 Gilman Drive, La Jolla, CA 92093, USA.
Eur J Pharmacol. 2008 Jun 10;587(1-3):118-23. doi: 10.1016/j.ejphar.2008.03.033. Epub 2008 Apr 1.
Various animal models of pain are dependent on activation of different glutamate receptor subtypes. First degree burn of the paw elicits a secondary hyperalgesia that is dependent on Ca2+ permeable alpha-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA), but not N-methyl-D-aspartate (NMDA) receptors. The present study takes advantage of that specificity by examining the effects of spinal pretreatments of agents on this secondary hyperalgesia. Rats with indwelling intrathecal catheters were pretreated with agents prior to paw injury. Mechanical withdrawal thresholds were measured before, and for three h after the injury. Spinal pretreatment with cyclooxygenase (10 and 30 microg (S)-(+)-ibuprofen; and 3 and 30 microg ketorolac) and nitric oxide synthase (33 and 100 microg N(G) Nitro-L-arginine methyl ester hydrochloride (L-NAME) and 10 microg thiocitrulline) inhibitors resulted in no specific anti-allodynia. In contrast, ziconotide (0.3, 1.0 and 3 microg), the N-type voltage gated calcium channel antagonist was very effective in blocking burn-induced sensitivity at all doses used. l-type (Diltiazam 230 microg) and P-type (Agatoxin IVA 0.3 microg) calcium channel blockers produced intermediate effects. Thus, cyclooxygenase and nitric oxide synthase are assumed not to be downstream of Ca2+ permeable AMPA receptors. Voltage gated calcium channels blockers could exert their effects either pre- or post-synaptically.
各种疼痛动物模型依赖于不同谷氨酸受体亚型的激活。爪部一度烧伤会引发继发性痛觉过敏,这种继发性痛觉过敏依赖于钙离子通透的α-氨基-3-羟基-5-甲基-4-异恶唑丙酸(AMPA)受体,而非N-甲基-D-天冬氨酸(NMDA)受体。本研究利用了这种特异性,通过检测脊髓预处理药物对这种继发性痛觉过敏的影响来进行研究。对留置鞘内导管的大鼠在爪部损伤前进行药物预处理。在损伤前及损伤后3小时测量机械性撤足阈值。用环氧化酶抑制剂(10和30微克(S)-(+)-布洛芬;以及3和30微克酮咯酸)和一氧化氮合酶抑制剂(33和100微克N(G)-硝基-L-精氨酸甲酯盐酸盐(L-NAME)和10微克硫代瓜氨酸)进行脊髓预处理未产生特异性抗异常性疼痛作用。相比之下,N型电压门控钙通道拮抗剂齐考诺肽(0.3、1.0和3微克)在所用的所有剂量下都能非常有效地阻断烧伤诱导的敏感性。L型(230微克地尔硫卓)和P型(0.3微克蜘蛛毒素IVA)钙通道阻滞剂产生中等程度的作用。因此,推测环氧化酶和一氧化氮合酶不在钙离子通透的AMPA受体的下游。电压门控钙通道阻滞剂可在突触前或突触后发挥作用。