新型抗胆碱药物盐酸戊乙奎醚及其4种光学异构体对N受体离子通道的作用

在非洲爪蟾培养的胚胎神经元和骨骼肌细胞上, 本文采用细胞膜片钳技术, 研究新型抗胆碱能药物盐酸戊乙奎醚(PHC)及其4种光学异构体对骨骼肌细胞N受体离子通道的作用. 结果表明PHC可阻断神经肌肉接头乙酰胆碱传递; 其4种光学异构体与之相比在对抗强度上无明显差别. PHC优先阻断开放时间长、电流强度大的N受体通道. 此外, PHC及其4种光学异构体对钠和钾离子通道也具有一定强度的阻断作用.

Effects of the novel cholinolytics penehyclidine hydrochloride and its four optical isomers on nicotinic receptor ion channels

The effects of the novel cholinolytics penehyclidine hydrochloride(PHC) and its four optical isomers on nicotinic receptor ion channels were studied in co-cultured neurons and myocytes using patch clamp techniques. The acetylcholine transmission in neuromuscular junctions was blocked by PHC, and there were no differences in antagonistic potency of PHC and its four optical isomers. PHC has preference to blocking the nicotinic receptor ion channels which have long open time, and high current amplitude. In addition, PHC and the four isomers have potent effects against sodium and potassium ion channels.