泮库溴铵对肾上腺嗜铬细胞乙酰胆碱受体的作用

Effects of pancuronium on nicotinic acetylcholine receptors in pheochromocytoma cells

目的 研究泮库溴铵对肾上腺嗜铬细胞(PC12细胞)烟碱型乙酰胆碱受体(nAChR)的作用,探讨其是否与该药的不良反应有关。方法 以DMEM培养液培养PC12细胞。采用全细胞电压钳技术,记录以不同浓度乙酰胆碱(Ach)(10、30、100、300、1000μmol／L)所诱发PC12细胞nAChR的内向电流和不同浓度泮库溴铵(0.01、0.1、1、10、100、1 000 μmol／L)对PC12细胞nAChR的内向电流的抑制率。结果PC12细胞可为不同浓度Ach激动,其电流大小呈浓度依赖性,93.7％的nAChR可被1mmol／LAch激活。泮库溴铵可逆性抑制1 mmol／L Ach所诱发的电流,并呈浓度依赖性。1 mmol／L泮库溴铵能完全抑制1 mmol／L Ach对PC12细胞nAChR的激动作用。结论 泮库溴铵能竞争性抑制PC12的uAChR,阻断儿茶酚胺的分泌。

Objective To investigate the effects of pancuronium on nicotinic acetylcholine receptors (nAChRs) in pheochromocytoma cells (PC12 cells) and to determine if pancuronium has direct effects on PC cells.Methods PC12 cells (purchased from Institute of Cytology, Chinese Academy of Science) were cultured in DMEM containing penicillin and glutamine. nAChR in PC12 cells were stimulated with different concentrations of Ach ( 10, 30, 100, 300, 1 000 μmol·L-1 ). Ach-mediated inward currents were recorded using whole-cell patch clamp technique with holding potential set at - 80 mV. To investigate the effects of pancuronium on nAChR in PC cells, the PC12 cells were perfused with different concentrations of pancuronium (0.01,0.1, 1, 10, 100, 1 000 μmol · L-1 ) before Ach 1 μmol·L-1 was added. Results Inward currents were elicited by stimulation of nAChR with Ach in a concentration-dependent manner. 93.7% of nAChRs could be activated by 1 μmol · L1 Ach. Pancuronium reversibly suppressed the currents in a concentration-dependent manner compared to the control currents elicited by 1 μmol·L-1 Ach. 1 μmol·L-1 pancuronium could almost completely suppressed the currents elicited by 1 μmol · L-1 Ach.Conclusion Pancuronium could inhibit nAChR in PC12 cells and reduce catecholamine release.