单 位：
佛山科学技术学院动物医学系;国家医药监督管理局药品审评中心
摘 要：
以小鼠热板法和小鼠扭体法研究了赛拉唑的镇痛作用 ,通过放射配体受体结合实验和脑内单胺类递质测定 ,分析了赛拉唑的镇痛作用机理。结果显示 ,在小鼠扭体实验中 ,赛拉唑可明显减少腹腔注射乙酸所致扭体反应次数 ,在小鼠热板实验中也可降低动物痛阈 ,其镇痛作用均呈剂量依赖性 ,相应的 ED50 值分别为0 .95和 4.2 5mg/ kg;预先给予 α2 拮抗剂育亨宾可对抗其镇痛作用 ,而 α1拮抗剂哌唑嗪则不能。放射配体受体结合实验表明 ,腹腔注射赛拉唑后 1 5、3 0和 6 0 min,小鼠脑膜 α2 受体与 [3 H]标记的α2 受体激动剂可乐宁的特异性结合均受到抑制。赛拉唑尚可抑制α-MPT引起的小鼠脑内单胺类物质尤其是 NA含量下降。上述结果提示 ,赛拉唑为中枢神经系统突触前膜 α2 受体激动剂 ,其镇痛作用机理与激动脑内 α2 受体有关
译 名：
Studies on Antinociceptive Activity and Mechanism of Action of Xylazole
作 者：
WANG Min-ru 1,XIAO Hui-lai 2 (1.Department of Veterinary Medicine, Foshan University, Nanhai,528231,China; 2.Center of Drug Evaluation, State Drug Administration, Beijing,100050,China)
关键词：
xylazole;antinociceptive activity;α 2-adrenerogic agonist;mice
摘 要：
Both in acetic acid-induced writhing test and hot plate test in mice, xylazole had a dose-dependent antinociceptive activity with ED 50values of 0.95 and 4.25 mg/kg, respectively. The antinociceptive effect of xylazole was antagonized by pretreatment of α 2-antagonist yohimbine. The ex vivo receptor binding study in mice showed that xylazole induced analgesia was significantly correlated to clonidine displacement in brain membranes. Xylazole could induce an inhibition of noradrenaline turnover as measured by α-MPT method in mice. The results suggest that the antinociceptive activity of xylazole be mediated through α 2-adrenoceptors in brain.
