Du Huizhi, Li Miaoyu, Yang Pin
Institute of Molecular Science, Key Laboratory of Chemical Biology and Molecular Engineering of Ministry of Education, Shanxi University, Wucheng Road 92, Taiyuan 030006, PR China.
Toxicol Lett. 2008 Sep 26;181(2):104-11. doi: 10.1016/j.toxlet.2008.07.004. Epub 2008 Jul 15.
As an acetylcholinesterase (AChE) inhibitor, the effects of 3-benzidino-6-phenylpyridazine (BPP) on outward potassium current including delayed rectifier potassium current (I(K(DR))) and transient outward potassium current (I(K(A))) in acutely isolated rat hippocampal pyramidal neurons were studied, using the whole cell patch-clamp technique. BPP reversibly inhibited electric eel AChE as an inhibitor, with IC(50) of 1.43 microM. BPP (0.10-100 microM) decreased I(K(DR)) and I(K(A)) in a concentration-dependent, voltage-independent and partial reversible manner, with IC(50) of 0.47 and 0.31 microM, respectively. 10 microM BPP did not affect steady-state activation of I(K(DR)) and I(K(A)). In addition, 10 microM BPP shifted the voltage dependence of steady-state inactivation of I(K(A)) towards negative potential. In conclusion, BPP potently inhibits I(K(DR)) and I(K(A)) in rat hippocampal pyramidal neurons, which may contribute to BPP's restoring the damaged central nervous system.
作为一种乙酰胆碱酯酶（AChE）抑制剂，采用全细胞膜片钳技术研究了3-联苯胺基-6-苯基哒嗪（BPP）对急性分离的大鼠海马锥体神经元外向钾电流，包括延迟整流钾电流（I(K(DR))）和瞬时外向钾电流（I(K(A))）的影响。BPP作为抑制剂可可逆性抑制电鳗AChE，IC(50)为1.43微摩尔。BPP（0.10 - 100微摩尔）以浓度依赖性、电压非依赖性和部分可逆的方式降低I(K(DR))和I(K(A))，IC(50)分别为0.47和0.31微摩尔。10微摩尔BPP不影响I(K(DR))和I(K(A))的稳态激活。此外，10微摩尔BPP使I(K(A))稳态失活的电压依赖性向负电位方向移动。总之，BPP可有效抑制大鼠海马锥体神经元中的I(K(DR))和I(K(A))，这可能有助于BPP修复受损的中枢神经系统。
