Fisher B, Zornow M H, Yaksh T L, Peterson B M
Department of Anesthesiology, University of California, San Diego, La Jolla 92093.
Eur J Pharmacol. 1991 Jan 10;192(2):221-5. doi: 10.1016/0014-2999(91)90046-s.
Dexmedetomidine is a highly selective alpha 2-adrenoceptor agonist. In this study, the intrathecal administration of dexmedetomidine into the rat lumbar subarachnoid space produced dose-dependent, prolonged antinociception as measured by hot plate and tail flick testing. Intrathecal administration of 3 or 10 micrograms of dexmedetomidine increased hot plate and tail flick latencies to cutoff values within 15 min of injection. Animals receiving 1 microgram of intrathecal dexmedetomidine did not show any significant antinociception when compared to saline controls. The intrathecal administration of the alpha 2-adrenoceptor antagonist, idazoxan, ablated all measurable antinociception produced by the prior injection of 10 micrograms of dexmedetomidine.
右美托咪定是一种高度选择性的α2肾上腺素能受体激动剂。在本研究中,将右美托咪定鞘内注射到大鼠腰段蛛网膜下腔,通过热板法和甩尾试验测量,产生了剂量依赖性的、持久的镇痛作用。鞘内注射3或10微克右美托咪定可使热板法和甩尾试验的潜伏期在注射后15分钟内增加至截止值。与生理盐水对照组相比,接受1微克鞘内注射右美托咪定的动物未表现出任何显著的镇痛作用。鞘内注射α2肾上腺素能受体拮抗剂咪唑克生,消除了先前注射10微克右美托咪定产生的所有可测量的镇痛作用。