Antinociceptive and anti-inflammatory activities of nicotinamide and its isomers in different experimental models
Antinociceptive and anti-inflammatory activities of nicotinamide and its isomers in different experimental models
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DOI：
10.1016/j.pbb.2011.07.003
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发表时间：
2011-10-01
影响因子：
3.6
通讯作者：
Coelho, Marcio M.
中科院分区：
文献类型：
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作者：
Godin, Adriana M.;Ferreira, Wallace C.;Coelho, Marcio M.
虽然有证据表明烟酰胺具有抗炎活性，但尚未评价其在伤害性疼痛和炎性疼痛模型中的作用。此外，没有关于烟酰胺异构体、吡啶酰胺和异烟酰胺潜在抗炎和抗伤害活性的信息。经口（p.o.）给予烟酰胺（1000 mg/kg，~ 1 h）抑制小鼠中福尔马林诱导的伤害感受性反应的第一和第二阶段。在伤害性疼痛模型中，将小鼠暴露于热板（50 ℃），烟酰胺（1000 mg/kg，约1 h）也呈现出抗伤害性活性。烟酰胺（500 mg/kg，-1和3 h）也抑制大鼠（炎性疼痛模型）中角叉菜胶诱导的机械性异常性疼痛。除了抑制伤害性反应外，烟酰胺（500或1000 mg/kg，-1和3 h）还抑制角叉菜胶诱导的小鼠和大鼠足肿胀。P.O.吡啶酰胺（125 mg/kg，~ 1 h）和异烟酰胺（500或1000 mg/kg，~ 1 h）的给药抑制了小鼠中由福尔马林诱导的伤害感受性反应的第二阶段。异烟酰胺（500或1000 mg/kg，~ 1 h）和吡啶酰胺（125 mg/kg，~ 1 h和3 h）也能抑制角叉菜胶引起的小鼠足肿胀。这些结果首次证明了烟酰胺及其异构体在伤害性疼痛和炎性疼痛模型中的活性，并为其抗炎活性提供了支持。证明烟酰胺的新活性是重要的，因为它可能有助于扩大其在治疗其他病理条件中的用途。(C)2011 Elsevier Inc. All rights reserved.
Although there is evidence for the anti-inflammatory activity of nicotinamide, there is no evaluation of its effects in models of nociceptive and inflammatory pain. In addition, there is no information about the potential anti-inflammatory and antinociceptive activities of the nicotinamide isomers, picolinamide and isonicotinamide. Per os (p.o.) administration of nicotinamide (1000 mg/kg, -1 h) inhibited the first and second phases of the nociceptive response induced by formalin in mice. In the model of nociceptive pain, exposure of mice to a hot-plate (50 degrees C), nicotinamide (1000 mg/kg, -1 h) also presented antinociceptive activity. Nicotinamide (500 mg/kg, -1 and 3 h) also inhibited the mechanical allodynia induced by carrageenan in rats, a model of inflammatory pain. In addition to inhibiting the nociceptive response, nicotinamide (500 or 1000 mg/kg, -1 and 3 h) inhibited the paw edema induced by carrageenan in mice and rats. P.o. administration of picolinamide (125 mg/kg, -1 h) and isonicotinamide (500 or 1000 mg/kg, -1 h) inhibited the second phase of the nociceptive response induced by formalin in mice. The paw edema induced by carrageenan in mice was also inhibited by isonicotinamide (500 or 1000 mg/kg, -1 h) and picolinamide (125 mg/kg, -1 h and 3 h). The results represent the first demonstration of the activity of nicotinamide and its isomers in models of nociceptive and inflammatory pain and provide support to their anti-inflammatory activity. The demonstration of new activities for nicotinamide is important as it may contribute to expand its use in the treatment of other pathological conditions. (C) 2011 Elsevier Inc. All rights reserved.