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首页> 外文期刊>Pharmacology, Biochemistry and Behavior >Comparative studies of huperzine A, E2020, and tacrine on behavior and cholinesterase activities.
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Comparative studies of huperzine A, E2020, and tacrine on behavior and cholinesterase activities.

机译：石杉碱甲，E2020和他克林对行为和胆碱酯酶活性的比较研究。

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Comparative effects of cholinesterase inhibitors (ChEI) huperzine A with E2020 and tacrine on the radial maze performance in ethylcholine mustard aziridinium ion (AF64A)-treated rat and inhibition of cholinesterase activity were studied. The intracerebroventricular (i.c.v.) injection of AF64A (3 nmol/side) caused significant impairment in the rat's ability to fulfill the partially baited maze paradigm. Oral huperzine A (0.5-0.8 mg/kg), E2020 (1.0-2.0 mg/kg), and tacrine (8.0 mg/kg) effectively reversed AF64A-induced working memory deficit. The doses that improved AF64A-induced memory deficit were correlated to about 25-30% (huperzine A) and less than 10% (E2020, tacrine) inhibition of acetylcholinesterase (AChE) activity in the cortex and hippocampus. Huperzine A, E2020 and tacrine all produced dose-dependent inhibition of brain AChE following i.c.v. and oral administration. Oral huperzine A exhibited higher efficacy on the inhibition of AChE in the cortex and hippocampus than those of E2020 and tacrine. Tacrine was more effective in inhibiting plasma butyrylcholinesterase (BuChE) than it was brain AChE. Conversely, the BuChE activity was less affected by huperzine A and E2020. The results showed that huperzine A had high bioavailability and more selective inhibition on AChE activity in cortex and hippocampus. Huperzine A fits more closely with the established criteria for an ideal AChE inhibitor to be used in clinical studies.
机译：研究了胆碱酯酶抑制剂（ChEI）石杉碱甲与E2020和他克林对乙胆碱芥子叠氮鎓离子（AF64A）处理的大鼠the迷宫性能和抑制胆碱酯酶活性的比较作用。脑室内（i.c.v.）AF64A（3 nmol /侧）注射导致大鼠满足部分诱饵迷宫范式的能力受到重大损害。口服石杉碱甲（0.5-0.8 mg / kg），E2020（1.0-2.0 mg / kg）和他克林（8.0 mg / kg）有效逆转了AF64A诱导的工作记忆缺陷。改善AF64A诱导的记忆缺陷的剂量与皮质和海马中乙酰胆碱酯酶（AChE）活性的抑制约25-30％（石杉碱甲）和少于10％（E2020，他克林）有关。石杉碱甲，E2020和他克林在i.c.v.后均产生剂量依赖性的脑AChE抑制作用。和口服。与E2020和他克林相比，口服石杉碱甲在皮质和海马中对AChE的抑制作用更高。他克林比血浆AChE更有效地抑制血浆丁酰胆碱酯酶（BuChE）。相反，石杉碱甲和E2020对BuChE活性的影响较小。结果表明石杉碱甲具有较高的生物利用度，并且对皮质和海马中的AChE活性具有更高的选择性抑制作用。石杉碱甲更符合临床研究中理想的AChE抑制剂的既定标准。

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