Effects of 3-benzidino-6-phenylpyridazine, as an acetylcholinesterase inhibitor, on outward potassium current in acutely isolated rat hippocampal pyramidal neurons.
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.
Du
Huizhi
H
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.
Li
Miaoyu
M
Yang
Pin
P
D000818:Animals; D002800:Cholinesterase Inhibitors / Q000494:pharmacology*; D051668:Delayed Rectifier Potassium Channels / Q000187:drug effects / Q000502:physiology; D004305:Dose-Response Relationship, Drug; D004593:Electrophorus; D018408:Patch-Clamp Techniques; D015221:Potassium Channels / Q000187:drug effects* / Q000502:physiology; D017966:Pyramidal Cells / Q000187:drug effects* / Q000378:metabolism; D011724:Pyridazines / Q000494:pharmacology*; D051381:Rats; D017208:Rats, Wistar
C533063:3-benzidino-6-phenylpyridazine; D002800:Cholinesterase Inhibitors; D051668:Delayed Rectifier Potassium Channels; D015221:Potassium Channels; D011724:Pyridazines