神经病理性疼痛
药代动力学
痛觉过敏
医学
坐骨神经
麻醉
药理学
香兰素
痛觉超敏
生物利用度
止痛药
神经痛
化学
内科学
伤害
生物化学
受体
作者
Francis Beaudry,Andréanne Ross,Pablo Lema,Pascal Vachon
摘要
Abstract The analgesic effects of vanillin on neuropathic pain was evaluated using thermal sensitivity and mechanical allodynia using the sciatic nerve constriction model ( n = 30 rats). To determine the pharmacokinetics of vanillin, rats ( n = 6/administration route) received either 20 or 100 mg/kg of vanillin i.v. and p.o., respectively. For the pharmacodynamic study, baseline levels for hyperalgesia and allodynia were taken for 5 days prior to surgery. Following surgery each group ( n = 6 rats/group) received either vanillin (50 mg/kg or 100 mg/kg), morphine (2 mg/kg or 6 mg/kg) or the vehicle only. Pharmacokinetic results following p.o. administrations are C max 290.24 ng/mL, T max 4 h, relative clearance 62.17 L/h/kg and T 1/2 10.3 h. The bioavailability is 7.6%. Mechanical allodynia was decreased on treatment days 1, 2, 3, 5 ( p < 0.003) and not on day 4 ( p > 0.02) with 50 mg/kg vanillin, whereas at 100 mg/kg p.o. a decrease was noted only on days 7 and 8 ( p < 0.003). No effect on hyperalgesia was seen following vanillin administration. In conclusion, vanillin is bioavailable and seems to have an alleviating effect on mechanical allodynia, and not on hyperalgesia, when evaluated with a chronic constriction nerve injury rat model of neuropathic pain. Copyright © 2009 John Wiley & Sons, Ltd.
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