化学
烟碱激动剂
尼古丁
乙酰胆碱受体
长时程增强
药理学
烟碱乙酰胆碱受体
烟碱拮抗剂
乙酰胆碱
胆碱能的
受体
α-4β-2烟碱受体
神经科学
生物
生物化学
作者
Ahmed Sultan,Kun Yang,Dmytro Isaev,Eslam El Nebrisi,Nurulain Syed,Nadia Khan,Christopher F. Howarth,Bassem Sadek,Murat Öz
出处
期刊:Toxicology
[Elsevier]
日期:2017-06-01
卷期号:384: 23-32
被引量:11
标识
DOI:10.1016/j.tox.2017.04.005
摘要
Effects of thujone, a major ingredient of absinthe, wormwood oil and some herbal medicines, were tested on the function of α7 subunit of the human nicotinic acetylcholine (α7 nACh) receptor expressed in Xenopus oocytes using the two-electrode voltage-clamp technique. Thujone reversibly inhibited ACh (100μM)-induced currents with an IC50 value of 24.7μM. The effect of thujone was not dependent on the membrane potential and did not involve Ca2+-dependent Cl- channels expressed endogenously in oocytes. Inhibition by thujone was not reversed by increasing ACh concentrations. Moreover, specific binding of [125I] α-bungarotoxin was not altered by thujone. Further experiments in SH-EP1 cells expressing human α7 nACh receptor indicated that thujone suppressed choline induced Ca2+ transients in a concentration-dependent manner. In rat hippocampal CA3-dentate gyrus synapses, nicotine-induced enhancement of long-term potentiation was also inhibited by thujone. Furthermore, the results observed in in-vivo one-trial passive avoidance paradigm show that thujone (1.25mg/kg, i.p.) significantly impaired nicotine-induced enhancement of learning and memory in Wistar rats. Collectively, our results indicate that thujone inhibits the function of the α7-nACh receptor and impairs cellular and behavioral correlates of cholinergic modulation of learning and memory.
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