Departament of Pharmacology, Universidade Federal de Santa Catarina, Florianópolis 88040-900, SC, Brazil Departament of Chemistry, Universidade Federal de Santa Catarina, Florianópolis 88040-900, SC, Brazil.
Pain. 2010 Mar;148(3):431-437. doi: 10.1016/j.pain.2009.12.002. Epub 2009 Dec 28.
This study investigated the role of TRPA1 in the development and maintenance of mechanical and cold hyperalgesia in persistent inflammation induced by Complete Freund's Adjuvant (CFA) in mice. The intraplantar (i.pl.) injection of CFA induced a long lasting (28 days) hyperalgesia for both mechanical and thermal (cold) stimuli. The intraperitoneal (i.p., 30-300 mg/kg), intraplantar (i.pl., 100 microg/site) or intrathecal (i.t., 10 microg/site) injection of the TRPA1 selective antagonist HC-030031 significantly reduced the mechanical hyperalgesia evaluated by the von Frey hair test. The effect of HC-030031 was evidenced on the day after CFA injection and was kept throughout the test. However, the intracerebroventricular (i.c.v., 10 microg/site) injection of HC-030031 did not interfere with CFA-induced hyperalgesia. Treatment with HC-030031 (300 mg/kg, i.p.) completely inhibited the noxious cold hyperalgesia induced by tetrafluoroethane in mice that received CFA. The pre-treatment with the TRPA1 oligonucleotide antisense (AS-ODN, i.t.) consistently prevented both mechanical and cold hyperalgesia. Interestingly, both TRPA1 protein expression and mRNA were over-expressed in spinal cord and dorsal root ganglia (DRG) of mice treated with CFA, an effect that was fully prevented by the pre-treatment with the TRPA1 antagonist HC-030031. Collectively, the present results showed that TRPA1 present at either peripheral or spinal sites play a relevant role in the development and maintenance of both mechanical and cold hyperalgesia during CFA-induced inflammation. Thus, TRPA1 selective antagonists represent promising candidates to treat hyperalgesia in persistent inflammatory states.
本研究探讨了瞬时受体电位通道 A1(TRPA1)在完全弗氏佐剂(CFA)诱导的慢性炎症中机械性和冷超敏反应的发展和维持中的作用。CFA 皮内注射引起机械性和热(冷)刺激的长期(28 天)超敏反应。TRPA1 选择性拮抗剂 HC-030031 的腹腔内(i.p.,30-300mg/kg)、皮内(i.pl.,100μg/部位)或鞘内(i.t.,10μg/部位)注射显著减轻 von Frey 毛发试验评估的机械性痛觉过敏。HC-030031 的作用在 CFA 注射后第 1 天显现,并在整个试验过程中持续存在。然而,HC-030031 的脑室内(i.c.v.,10μg/部位)注射不干扰 CFA 诱导的痛觉过敏。HC-030031(300mg/kg,i.p.)治疗完全抑制了接受 CFA 的小鼠中四氟乙烷诱导的有害冷超敏反应。TRPA1 寡核苷酸反义(AS-ODN,i.t.)预处理一致地预防了机械性和冷超敏反应。有趣的是,CFA 处理的小鼠脊髓和背根神经节(DRG)中 TRPA1 蛋白表达和 mRNA 均过度表达,该作用被 TRPA1 拮抗剂 HC-030031 的预处理完全阻止。总之,本研究结果表明,外周或脊髓部位的 TRPA1 在 CFA 诱导的炎症期间机械性和冷超敏反应的发展和维持中发挥重要作用。因此,TRPA1 选择性拮抗剂是治疗持续性炎症状态下痛觉过敏的有前途的候选药物。