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目的:观察二氢—β—刺桐啶碱(dHβE)对大鼠骨骼肌细胞烟碱诱发电流的抑制作用并确定其在烟碱受体上的作用位点。方法:取新生Wistar大鼠骨骼肌细胞体外培养获得肌球,用膜片钳全细胞记录技术观察肌球给予不同浓度dHβE后对烟碱诱发电流的影响。结果:骨骼肌细胞烟碱(浓度40~160μmol.L-1)诱发电流及dHβE(浓度0~40μmol.L-1)对其的抑制作用均具有量效关系;dHβE作用于烟碱识别位点而非烟碱受体离子通道。结论:膜片钳技术使探讨烟碱受体拮抗药的作用位点成为可能。
AIM: To observe the inhibitory effects of dihydro-β-pyralines (dHβE) on nicotine-induced currents in rat skeletal muscle cells and to determine their role in nicotinic receptors. Methods: Skeletal muscle cells of neonatal Wistar rats were cultured in vitro and myoblasts were harvested. The effects of dHβE with different concentrations of dHβE on the induced current were observed by patch-clamp whole cell recording. RESULTS: The inhibitory effect of nicotine (concentration 40 ~ 160μmol.L-1) and its inhibitory effect on dHβE (concentration 0 ~ 40μmol.L-1) in skeletal muscle cells were dose-effect relationship. Rather than nicotinic receptor ion channels. Conclusion: Patch-clamp technique makes it possible to explore the site of action of nicotinic receptor antagonists.