Pillai N P, Ross D H
Pharmacol Biochem Behav. 1986 Sep;25(3):555-60. doi: 10.1016/0091-3057(86)90140-1.
The effects of morphine sulfate on rectal temperature and on Ca++-stimulated Mg++ATPase activity in crude synaptosomal fraction (P2) of cortex, hypothalamus and cerebellum were investigated in rat. Morphine (3-15 mg/kg, SC) produced hyperthermia at 30-120 min after the drug administration. The Ca++/Mg++ ATPase activity in hypothalamus and cortex was decreased while there was no change in Mg++ ATPase activity. The enzyme activity in cerebellum was not affected. The opiate antagonist naloxone hydrochloride (5 mg/kg, SC) antagonized the effect of morphine on rectal temperature and Ca++/Mg++ ATPase activity. The effects of different calcium channel antagonists (nimodipine 1 mg/kg, verapamil 2.5 mg/kg and diltiazem 10 mg/kg, SC) on the changes induced by morphine were also investigated. These antagonists not only antagonized morphine hyperthermia, but also the inhibitory effect of morphine on Ca++/Mg++ ATPase activity in hypothalamus. The calcium channel agonist BAY K8644 (3 mg/kg, SC) produced hypothermia and also stimulation of Ca++/Mg++ ATPase activity in hypothalamus. Naloxone failed to alter these effects of BAY K8644. These studies demonstrate that Ca++ transport in hypothalamus, as indicated by Ca++/Mg++ ATPase activity, plays an important role in thermoregulation and thermoregulatory changes induced by opiates.
研究了硫酸吗啡对大鼠皮层、下丘脑和小脑粗突触体部分（P2）直肠温度及钙离子刺激的镁离子 -ATP酶活性的影响。吗啡（3 - 15毫克/千克，皮下注射）在给药后30 - 120分钟产生体温过高。下丘脑和皮层中的钙离子/镁离子 -ATP酶活性降低，而镁离子 -ATP酶活性无变化。小脑的酶活性未受影响。阿片拮抗剂盐酸纳洛酮（5毫克/千克，皮下注射）拮抗了吗啡对直肠温度和钙离子/镁离子 -ATP酶活性的作用。还研究了不同钙通道拮抗剂（尼莫地平1毫克/千克、维拉帕米2.5毫克/千克和地尔硫卓10毫克/千克，皮下注射）对吗啡诱导变化的影响。这些拮抗剂不仅拮抗了吗啡引起的体温过高，还拮抗了吗啡对下丘脑钙离子/镁离子 -ATP酶活性的抑制作用。钙通道激动剂BAY K8644（3毫克/千克，皮下注射）产生体温过低，并刺激下丘脑钙离子/镁离子 -ATP酶活性。纳洛酮未能改变BAY K8644的这些作用。这些研究表明，如下丘脑钙离子/镁离子 -ATP酶活性所示，下丘脑的钙离子转运在体温调节及阿片类药物诱导的体温调节变化中起重要作用。
