Acetylcholinesterase inhibitor ENA-713 protects against ischemia-induced decrease in pre- and postsynaptic cholinergic indices in the gerbil brain following transient ischemia
Acetylcholinesterase inhibitor ENA-713 protects against ischemia-induced decrease in pre- and postsynaptic cholinergic indices in the gerbil brain following transient ischemia
复制标题
乙酰胆碱酯酶抑制剂 ENA-713 可防止短暂性缺血后沙鼠大脑中缺血引起的突触前和突触后胆碱能指数下降
作者：
K. Tanaka;N. Ogawa;K. Mizukawa;M. Asanuma;Y. Kondo;S. Nishibayashi;A. Mori
本实验观察了沙土鼠脑缺血再灌注后4天和14天给予乙酰胆碱酯酶（AChE）抑制剂ENA-713预处理对脑突触前和突触后胆碱能指数变化的影响。在缺血组中，海马乙酰胆碱（ACh）水平在缺血后4天显著降低（至假手术对照组的23%），但ENA-713治疗完全阻止了这种降低。胆碱乙酰转移酶（ChAT）和胆碱酯酶（ChE）活性在缺血后4和14天无明显变化。虽然在缺血后14天，海马中毒蕈碱型ACh受体（mACh-R）结合的最大数量（Bmax）降低（至44%）而亲和力没有任何变化，但这种降低也被ENA-713治疗抑制。此外，组织学实验表明，ENA-713抑制缺血诱导的海马CA 1区锥体细胞丢失。因此，这些发现表明ENA-713对脑缺血引起的脑血管型痴呆具有保护、神经营养和治疗作用。
The effects of pre-treatment with ENA-713, an acetylcholinesterase (AChE) inhibitor, on changes in pre- and postsynaptic cholinergic indices in gerbil brain following transient ischemia were studied at 4 and 14 days after recirculation. In the ischemic group, hippocampal acetylcholine (ACh) level was significantly reduced (to 23% of sham-operated controls) at 4 days post-ischemia, but this reduction was completely prevented by ENA-713 treatment. Choline acetyltransferase (ChAT) and cholinesterase (ChE) activities were not significantly changed at 4 and 14 days post-ischemia. Although the maximum number (Bmax) of muscarinic ACh receptor (mACh-R) binding in the hippocampus was decreased (to 44%) without any change in affinity at 14 days post-ischemia, this decrease was also inhibited by ENA-713 treatment. In addition, histological experiment indicated that ENA-713 inhibited ischemia-induced pyramidal cell loss in the hippocampal CA1 regions. Thus, these findings suggest that ENA-713 has protective, neurotrophic and therapeutic effects on cerebrovascular type dementia due to cerebral ischemia.
DOI：
10.1176/ajp.139.11.1421
发表时间：
1982-11
期刊：
The American journal of psychiatry
影响因子：
--
作者：
K. Davis;R. Mohs
通讯作者：
K. Davis;R. Mohs
影响因子：
5.9
作者：
PULSINELLI, WA;LEVY, DE;PLUM, F
通讯作者：
PLUM, F