Spencer R L, Hruby V J, Burks T F
Department of Pharmacology, University of Arizona, Tucson.
J Pharmacol Exp Ther. 1990 Feb;252(2):696-705.
This paper focuses on the behavioral thermoregulatory effects of i.c.v. administration of [D-Ala2,MePhe4,Gly5-ol]enkephalin (DAMGO), cyclic [D-Pen2,D-Pen5]enkephalin (DPDPE) and U-50,488H, selective agonists for the mu, delta and kappa opioid receptors, respectively. Rats were tested in a thermally graded tunnel (thermocline) which allowed for simultaneous measurement of body temperature, ambient temperature selection and general ambulatory activity levels. DAMGO (0.3 micrograms) caused an increase in body temperature which was facilitated by the selection of a warm ambient temperature. Both DPDPE (30 micrograms) and U-50,488H (100 micrograms) caused decreases in body temperature which were accompanied by a selection of a cool ambient temperature. In each case there was evidence for a regulated change in body temperature, with DAMGO increasing thermoregulatory set point and DPDPE and U-50,488H decreasing set point. DAMGO and U-50,488H produced a depression of activity levels for the first 15 min after injection. DAMGO and DPDPE produced increases in activity levels which peaked after body temperature had returned toward base-line levels. These data characterize further the differentiable profiles of physiological effects produced by these three compounds. The central modulation of the control of body temperature by these opioid receptor agonists may reflect a role of endogenous opioids in thermoregulatory control.
本文重点研究了脑室内注射[D-丙氨酸2，甲硫氨酸脑啡肽4，甘氨酸5-醇]脑啡肽（DAMGO）、环[D-青霉胺2，D-青霉胺5]脑啡肽（DPDPE）和U-50,488H分别对μ、δ和κ阿片受体的选择性激动剂的行为体温调节作用。在一个温度梯度隧道（温度梯度仪）中对大鼠进行测试，该隧道允许同时测量体温、环境温度选择和一般活动水平。DAMGO（0.3微克）导致体温升高，选择温暖的环境温度会促进这种升高。DPDPE（30微克）和U-50,488H（100微克）均导致体温下降，同时伴有选择凉爽的环境温度。在每种情况下，都有证据表明体温发生了调节性变化，DAMGO提高了体温调节设定点，而DPDPE和U-50,488H降低了设定点。DAMGO和U-50,488H在注射后的前15分钟导致活动水平下降。DAMGO和DPDPE导致活动水平升高，在体温恢复到基线水平后达到峰值。这些数据进一步描述了这三种化合物产生的不同生理效应特征。这些阿片受体激动剂对体温控制的中枢调节可能反映了内源性阿片类物质在体温调节控制中的作用。
