二甲苯胺噻唑中枢镇痛作用的研究  

A STUDY ON CENTRAL ANALGESIC EFFECT OF XYLAZOLE

作　　者：梁德勇[1] 叶燕燕[1] 莫孝荣[1] 吉长福[1] 朱丽霞[1] 

机构地区：[1]中国中医研究院针灸研究所,北京100700

出　　处：《中国疼痛医学杂志》2002年第4期215-218,共4页Chinese Journal of Pain Medicine

摘　　要：本实验用辐射热照射甩尾法测定大鼠痛阈 ,观察到脑室注射二甲苯胺噻唑具有明显的量效相关的镇痛效应 ,其镇痛效应与肾上腺素α2 受体激动剂可乐定的相似 ,且可被α2 受体拮抗剂育亨宾阻断 ,说明二甲苯胺噻唑可能通过肾上腺素α2 受体产生镇痛效应。二甲苯胺噻唑的镇痛效应还可被咪唑啉受体拮抗剂苯恶唑阻断 ,提示其中还可能有咪唑啉受体参与。本实验还观察到兴奋性氨基酸拮抗剂氯胺酮和钙离子络合剂EDTA可加强二甲苯胺噻唑的镇痛效应 ,减少其用量并减轻其副作用。为开发肾上腺素α2 受体激动剂类非成瘾性镇痛药提供新的途径。The analgesic effects of Xylazole, a newly synthesized analgesic and muscle relaxing agent, were investigated by tail flick latency tests in rats. It was found that intra cerebroventricular injection (icv) of Xylazole in doses of 3～300 mg/5ml produces dose dependent analgesic effects. This analgesic effect was similar to that of clonidine, an agonist of α 2 adreno receptors (α 2 AR), and was blocked by yohimbine, an antagonist for α 2 AR, suggesting that xylazole induced analgesic effect might be mediated by α 2AR. Xylazole analgesia could also be antagonized by idazoxan, an antagonist for imidazoline receptor (IR). It means that IR may also be involved in xylazole analgesia. In addition, xylazole analgesia was much strengthened by pretreatment with icv ketamine, a non specific antagonist of excitatory amino acid receptors, or icv EDTA, a calcium chelator. So xylazole combined with ketamine or EDTA for minimizing the side effects, may be developed as a non-addicted analgesic drug.

关 键 词：二甲苯胺噻唑 中枢 镇痛作用 研究 肾上腺素能α2受体 咪唑啉受体 

分 类 号：R614[医药卫生—麻醉学]