Kamerling S, Weckman T, Donahoe J, Tobin T
Department of Veterinary Physiology, College of Veterinary Medicine, Louisiana State University, Baton Rouge 70803.
Equine Vet J. 1988 Mar;20(2):114-8. doi: 10.1111/j.2042-3306.1988.tb01471.x.
Current opiate receptor theory suggests that kappa agonists should provide good analgesia without producing marked central nervous system stimulation. U-50,488H is an experimental narcotic analgesic that is a selective kappa agonist. In the present study, U-50,488H produced good analgesia in horses using both the skin twitch and hoof withdrawal reflex assays. Further, the analgesia was relatively long lasting (120 mins) compared to other mu-agonists tested in horses. The locomotor response to U-50,488H was less than observed with ethylketazocine and butorphanol, and has yielded the smallest locomotor response of any of the narcotic analgesics tested to date. Other work showed that the autonomic responses to U-50,488H were less than those of other narcotic analgesics, and that the analgesic response to this drug was blocked by naloxone. Based on its ability to produce analgesia with little other stimulatory action, U-50,488H shows promise of becoming a useful narcotic analgesic in equine medicine.
当前的阿片受体理论表明，κ激动剂应能提供良好的镇痛效果，而不会产生明显的中枢神经系统刺激。U - 50,488H是一种实验性麻醉性镇痛药，是一种选择性κ激动剂。在本研究中，使用皮肤抽搐和蹄部退缩反射试验，U - 50,488H在马匹中产生了良好的镇痛效果。此外，与在马匹中测试的其他μ激动剂相比，这种镇痛效果持续时间相对较长（120分钟）。U - 50,488H引起的运动反应小于乙基酮佐辛和布托啡诺观察到的反应，并且是迄今为止测试的所有麻醉性镇痛药中运动反应最小的。其他研究表明，U - 50,488H引起的自主反应小于其他麻醉性镇痛药，并且该药物的镇痛反应可被纳洛酮阻断。基于其产生镇痛作用而几乎没有其他刺激作用的能力，U - 50,488H有望成为马医学中一种有用的麻醉性镇痛药。
