Lin J H, Hu G Y, Tang X C
State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, China.
Zhongguo Yao Li Xue Bao. 1997 Jan;18(1):6-10.
To compare the effects of huperzine A (Hup A), tacrine, and E2020 on cholinergic transmission at mouse neuromuscular junction in vitro.
The isolated mouse phrenic nerve-hemidiaphragm preparations were used with the conventional intracellular recording technique. The miniature end-plate potentials (MEPP), the mean quantal content of end-plate potentials (EPP), and the resting membrane potentials of muscle fiber were recorded.
Hup A, tacrine, and E2020 at the concentration of 1.0 mumol.L-1 increased the amplitude, time-to-peak, and half-decay time of MEPP in the potencies of E2020 > Hup A > tacrine. Hup A did not significantly change the frequency of MEPP, the appearance of giant MEPP or slow MEPP, the resting membrane potentials, and the mean quantal content of EPP.
Hup A is a selective and potent cholinesterase inhibitor, by which activity it facilitates the cholinergic transmission at mouse neuromuscular junction, and devoid of pre- and post-synaptic actions.
比较石杉碱甲(Hup A)、他克林和E2020对体外小鼠神经肌肉接头处胆碱能传递的影响。
采用常规细胞内记录技术,使用分离的小鼠膈神经 - 半膈肌标本。记录微小终板电位(MEPP)、终板电位(EPP)的平均量子含量以及肌纤维的静息膜电位。
浓度为1.0 μmol·L-1的Hup A、他克林和E2020均能增加MEPP的幅度、达峰时间和半衰时间,其效能顺序为E2020 > Hup A > 他克林。Hup A对MEPP的频率、巨大MEPP或缓慢MEPP的出现、静息膜电位以及EPP的平均量子含量均无显著影响。
Hup A是一种选择性强效胆碱酯酶抑制剂,通过该活性促进小鼠神经肌肉接头处的胆碱能传递,且无突触前和突触后作用。