Coudray-Lucas C, Prioux-Guyonneau M, Tassel A, Coq H M, Cohen Y, Wepierre J
Acta Pharmacol Toxicol (Copenh). 1981 Sep;49(3):215-22. doi: 10.1111/j.1600-0773.1981.tb00896.x.
The early and late effect of three anticholinesterase agents (physostigmine, paraoxon and soman) on core temperature and brain acetylcholinesterase (AcChE) inhibition are compared. The study was performed in adult male rats using sublethal doses of all drugs. AcChE activity was determined by hypothalamus, striatum, hippocampus, medulla oblongata-pons and rest of the brain. The co-existence of intoxication symptoms, hypothermia and AcChE inhibitions was clearly shown by the early effects. However, no relationship was found between the degree of hypothermia and that of inhibition whatever brain area. In contrast, late AcChE inhibition was not accompanied by symptoms and lowering of core temperature. Several hypotheses have been suggested to explain this phenomenon: de novo synthesis of enzyme, decreased sensitivity of neurotransmitter or return to normal of brain acetylcholine level through a negative feed back at the presynaptic level. The present data suggest that this latter assumption is the most likely.
比较了三种抗胆碱酯酶药物(毒扁豆碱、对氧磷和梭曼)对核心体温和脑乙酰胆碱酯酶(AcChE)抑制的早期和晚期效应。该研究在成年雄性大鼠中使用所有药物的亚致死剂量进行。通过下丘脑、纹状体、海马体、延髓-脑桥和脑的其余部分测定AcChE活性。早期效应清楚地表明了中毒症状、体温过低和AcChE抑制的共存。然而,无论在哪个脑区,均未发现体温过低程度与抑制程度之间存在关联。相比之下,晚期AcChE抑制并未伴有症状和核心体温降低。已经提出了几种假设来解释这一现象:酶的从头合成、神经递质敏感性降低或通过突触前水平的负反馈使脑乙酰胆碱水平恢复正常。目前的数据表明后一种假设最有可能。