Handler C M, Geller E B, Adler M W
Department of Pharmacology, Temple University School of Medicine, Philadelphia, PA 19140.
Pharmacol Biochem Behav. 1992 Dec;43(4):1209-16. doi: 10.1016/0091-3057(92)90504-9.
The effect of selective mu-, kappa-, and delta-agonists on brain surface temperature (Tb), oxygen consumption (Vo2), and heat exchange (Q) was studied in unrestrained, male Sprague-Dawley rats using whole-body calorimetry. Hyperthermia, produced by PL-017 (1.86 nM) given ICV, resulted from increased Vo2 and reduced Q during the first 15-45 min postinjection. Tb returned to control levels due to a combination of increased Q and reduced Vo2. PL-017-induced hyperthermia was abolished by the mu-selective antagonist CTAP (0.75 nM). Dynorphin A1-17 (4.65 nM), a kappa-selective agonist, reduced both Vo2 and Q, resulting in hypothermia that was blocked by the kappa-selective antagonist nor-binaltorphimine (25 nM). The delta-selective agonist DPDPE (4.64 nM) caused no significant changes in Tb, Vo2, or Q. The data indicate that central stimulation of the mu- and kappa-opioid receptors affects both oxidative metabolism and heat exchange, which result in a change in Tb. These alterations can be prevented with selective opioid antagonist pretreatment.
利用全身量热法,在无束缚的雄性斯普拉格-道利大鼠中研究了选择性μ、κ和δ激动剂对脑表面温度(Tb)、氧消耗(Vo2)和热交换(Q)的影响。脑室内注射PL-017(1.86 nM)所产生的体温过高,是由于注射后最初15 - 45分钟内Vo2增加和Q降低所致。由于Q增加和Vo2降低的共同作用,Tb恢复到对照水平。μ选择性拮抗剂CTAP(0.75 nM)消除了PL-017诱导的体温过高。κ选择性激动剂强啡肽A1-17(4.65 nM)降低了Vo2和Q,导致体温过低,κ选择性拮抗剂nor-binaltorphimine(25 nM)可阻断这种体温过低。δ选择性激动剂DPDPE(4.64 nM)对Tb、Vo2或Q没有显著影响。数据表明,μ和κ阿片受体的中枢刺激会影响氧化代谢和热交换,进而导致Tb发生变化。这些改变可以通过选择性阿片拮抗剂预处理来预防。