Medrano S, Ochoa E L, McNamee M G
Instituto de Biologia Celular, Facultad de Medicina, Universidad de Buenos Aires, Argentina.
Neurochem Int. 1987;11(2):175-81. doi: 10.1016/0197-0186(87)90007-6.
The antiviral drug amantadine is also a potent neuromuscular blocking agent. When the nicotinic receptor from a Torpedinidae species is reconstituted into soybean liposomes, the binding of ?-bungarotoxin is not altered although the carbamylcholine induced radioactive cation influx is blocked. By studying cation fluxes in amantadine preincubated membranes previously exposed to different concentrations of carbamylcholine for different periods of time, we have shown that the drug accelerates the conversion of the nicotinic acetylcholine receptor from a state of low affinity to a state of high affinity for carbamyalcholine, a phenomenon correlated with receptor desensitization. The drug did not induce such a shift by itself. The present data and those by Earnest et al. (Biochemistry22, 5523-5535, 1984) show that the nicotinic acetylcholine receptor reconstituted into liposomes is a good model for studying the effects of noncompetitive blockers of nicotinic acetylcholine receptor function.
抗病毒药物金刚烷胺也是一种有效的神经肌肉阻滞剂。当将来自电鳐科物种的烟碱型受体重构到大豆脂质体中时，尽管氨甲酰胆碱诱导的放射性阳离子内流被阻断，但α-银环蛇毒素的结合并未改变。通过研究预先用金刚烷胺孵育的膜中的阳离子通量，这些膜先前在不同时间段暴露于不同浓度的氨甲酰胆碱，我们已经表明该药物加速了烟碱型乙酰胆碱受体从对氨甲酰胆碱低亲和力状态转变为高亲和力状态，这一现象与受体脱敏相关。该药物本身不会诱导这种转变。目前的数据以及欧内斯特等人（《生物化学》22卷，5523 - 5535页，1984年）的数据表明，重构到脂质体中的烟碱型乙酰胆碱受体是研究烟碱型乙酰胆碱受体功能非竞争性阻滞剂作用的良好模型。
