Saeki S, Yaksh T L
Department of Anesthesiology, University of California, San Diego, La Jolla.
J Pharmacol Exp Ther. 1992 Feb;260(2):795-802.
In halothane (0.9%)-anesthetized rats, the immersion of the tail in 52.5 degrees C or 60 degrees C water for 15 sec resulted in a short-latencied tail jerk and a subsequent tachycardia and elevation in blood pressure. The i.t. administration of the alpha-2 agonists, dexmedetomidine (DMET), clonidine (CLON) and ST-91, resulted in a dose-dependent increase in the somatomotor reflex latency and a reduction in the magnitude of the increase in the magnitude of the cardiovascular response, with the ordering of activity on all endpoints at all temperatures being: DMET greater than CLON greater than or equal to ST-91. Increasing the stimulus intensity from 52.5 to 60 degrees C resulted in right shifts in the dose-response curves for all agents with the magnitude of shift being: 1) greatest on the blood pressure and least on the tail flick, and 2) greatest for ST-91 and CLON and least for DMET. Thus, the dose ratio (ED50 at 60 degrees C/ED50 at 52.5 degrees C) for these three agents on the tail flick and blood pressure response was, respectively, 1.1 and 1.8 for DMET, 1.1 and 4.3 for CLON and 4.8 and 9.7 for ST-91 (mean +/- S.E.). On resting blood pressure, i.t. DMET and CLON produced a dose-dependent hypotension and bradycardia. ST-91 had no consistent dose-dependent effect.(ABSTRACT TRUNCATED AT 250 WORDS)
在氟烷(0.9%)麻醉的大鼠中,将尾巴浸入52.5摄氏度或60摄氏度的水中15秒会导致潜伏期较短的甩尾动作,随后出现心动过速和血压升高。鞘内注射α2激动剂右美托咪定(DMET)、可乐定(CLON)和ST-91,会导致躯体运动反射潜伏期剂量依赖性增加,心血管反应幅度增加量减少,在所有温度下对所有终点的活性排序为:DMET大于CLON大于或等于ST-91。将刺激强度从52.5摄氏度增加到60摄氏度,所有药物的剂量-反应曲线均右移,位移幅度为:1)血压最大,甩尾最小;2)ST-91和CLON最大,DMET最小。因此,这三种药物对甩尾和血压反应的剂量比(60摄氏度时的ED50/52.5摄氏度时的ED50),DMET在甩尾和血压反应上分别为1.1和1.8,CLON为1.1和4.3,ST-91为4.8和9.7(平均值±标准误)。关于静息血压,鞘内注射DMET和CLON会产生剂量依赖性低血压和心动过缓。ST-91没有一致的剂量依赖性效应。(摘要截短于250字)