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9-氨基-1,2,3,4-四氢吖啶(THA),一种据称可用于治疗阿尔茨海默病的药物,可抑制乙酰胆碱酯酶活性并减慢外向钾电流。

9-Amino-1,2,3,4-tetrahydroacridine (THA), an alleged drug for the treatment of Alzheimer's disease, inhibits acetylcholinesterase activity and slow outward K+ current.

作者信息

Drukarch B, Kits K S, Van der Meer E G, Lodder J C, Stoof J C

机构信息

Department of Neurology, Medical Faculty, Free University, Amsterdam, The Netherlands.

出版信息

Eur J Pharmacol. 1987 Sep 2;141(1):153-7. doi: 10.1016/0014-2999(87)90424-9.

DOI:10.1016/0014-2999(87)90424-9
PMID:2444444
Abstract

The in vitro release of acetylcholine in rat brain tissue was inhibited by 9-amino-1,2,3,4-tetrahydroacridine (THA). Atropine antagonized this effect of THA. As THA does not display an affinity for muscarinic receptors, we conclude that THA inhibits acetylcholinesterase activity. In electrophysiological studies with neurons of Lymnaea stagnalis, THA inhibited the slow outward K+ current and consequently increased the duration of the action potentials. It is discussed that both effects of THA possibly contribute to its reported effect in the treatment of patients with Alzheimer's disease.

摘要

9-氨基-1,2,3,4-四氢吖啶(THA)抑制大鼠脑组织中乙酰胆碱的体外释放。阿托品可拮抗THA的这一作用。由于THA对毒蕈碱受体没有亲和力,我们得出结论,THA抑制乙酰胆碱酯酶活性。在对椎实螺神经元的电生理研究中,THA抑制了缓慢的外向钾电流,从而延长了动作电位的持续时间。讨论了THA的这两种作用可能都有助于其在阿尔茨海默病患者治疗中所报道的效果。

相似文献

1
9-Amino-1,2,3,4-tetrahydroacridine (THA), an alleged drug for the treatment of Alzheimer's disease, inhibits acetylcholinesterase activity and slow outward K+ current.9-氨基-1,2,3,4-四氢吖啶(THA),一种据称可用于治疗阿尔茨海默病的药物,可抑制乙酰胆碱酯酶活性并减慢外向钾电流。
Eur J Pharmacol. 1987 Sep 2;141(1):153-7. doi: 10.1016/0014-2999(87)90424-9.
2
THA increases action potential duration of central histamine neurons in vitro.THA 在体外增加中枢组胺能神经元的动作电位时程。
Eur J Pharmacol. 1988 Oct 18;155(3):265-70. doi: 10.1016/0014-2999(88)90512-2.
3
Further analysis of the neuropharmacological profile of 9-amino-1,2,3,4-tetrahydroacridine (THA), an alleged drug for the treatment of Alzheimer's disease.对9-氨基-1,2,3,4-四氢吖啶(THA)(一种所谓的治疗阿尔茨海默病的药物)神经药理学特征的进一步分析。
Life Sci. 1988;42(9):1011-7. doi: 10.1016/0024-3205(88)90431-6.
4
Anatomy of cholinesterase inhibition in Alzheimer's disease: effect of physostigmine and tetrahydroaminoacridine on plaques and tangles.阿尔茨海默病中胆碱酯酶抑制的剖析:毒扁豆碱和四氢氨基吖啶对斑块和缠结的影响。
Ann Neurol. 1987 Dec;22(6):683-91. doi: 10.1002/ana.410220603.
5
Effect of in vivo microdialysis of 1,2,3,4-tetrahydro-9-aminoacridine (THA) on the extracellular concentration of acetylcholine in the striatum of anesthetized rats.1,2,3,4-四氢-9-氨基吖啶(THA)体内微透析对麻醉大鼠纹状体细胞外乙酰胆碱浓度的影响。
J Pharmacol Exp Ther. 1993 May;265(2):759-64.
6
The cholinergic pharmacology of tetrahydroaminoacridine in vivo and in vitro.四氢氨基吖啶在体内和体外的胆碱能药理学
Br J Pharmacol. 1989 Sep;98(1):79-86. doi: 10.1111/j.1476-5381.1989.tb16865.x.
7
9-Amino-1,2,3,4-tetrahydroacridine (THA) blocks agonist-induced potassium conductance in rat hippocampal neurones.9-氨基-1,2,3,4-四氢吖啶(THA)可阻断激动剂诱导的大鼠海马神经元钾离子电导。
Eur J Pharmacol. 1989 Apr 25;163(2-3):369-72. doi: 10.1016/0014-2999(89)90209-4.
8
Inhibition of rat brain histamine-N-methyltransferase by 9-amino-1,2,3,4-tetrahydroacridine (THA).9-氨基-1,2,3,4-四氢吖啶(THA)对大鼠脑组胺-N-甲基转移酶的抑制作用。
Biochem Pharmacol. 1990 Sep 15;40(6):1345-50. doi: 10.1016/0006-2952(90)90402-7.
9
The mechanism of tetrahydroaminoacridine-evoked release of endogenous 5-hydroxytryptamine and dopamine from rat brain tissue prisms.四氢氨基吖啶诱发大鼠脑组织薄片释放内源性5-羟色胺和多巴胺的机制。
Br J Pharmacol. 1989 Dec;98(4):1127-36. doi: 10.1111/j.1476-5381.1989.tb12656.x.
10
Effects of 9-amino-1,2,3,4-tetrahydroacridine (THA), a potential drug for treatment of Alzheimer's disease, on the physical state of human erythrocyte membranes.9-氨基-1,2,3,4-四氢吖啶(THA)是一种治疗阿尔茨海默病的潜在药物,其对人红细胞膜物理状态的影响。
Prog Clin Biol Res. 1989;292:419-24.

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Nootropic agent vinpocetine blocks delayed rectified potassium currents more strongly than high-threshold calcium currents.
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Neurosci Behav Physiol. 1998 Mar-Apr;28(2):116-20. doi: 10.1007/BF02461956.
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Nicotinic acetylcholine receptor (nACh-R) agonist-induced changes in brain monoamine turnover in mice.烟碱型乙酰胆碱受体(nACh-R)激动剂诱导的小鼠脑单胺代谢变化。
Psychopharmacology (Berl). 1997 Feb;129(3):225-32. doi: 10.1007/s002130050184.
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Interaction of tacrine and velnacrine with neocortical synaptosomal membranes: relevance to Alzheimer's disease.他克林和韦那克林与新皮质突触体膜的相互作用:与阿尔茨海默病的相关性。
Neurochem Res. 1993 Sep;18(9):989-94. doi: 10.1007/BF00966758.
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Tacrine-induced increase in the release of spontaneous high quantal content events in Torpedo electric organ.他克林诱导电鳐电器官中自发高量子含量事件释放增加。
Br J Pharmacol. 1994 May;112(1):19-22. doi: 10.1111/j.1476-5381.1994.tb13022.x.
7
Further analysis of the cognitive effects of tetrahydroaminoacridine (THA) in Alzheimer's disease: assessment of attentional and mnemonic function using CANTAB.四氢氨基吖啶(THA)对阿尔茨海默病认知影响的进一步分析:使用剑桥神经心理测试自动化成套系统评估注意力和记忆功能
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Ethological study of the effects of tetrahydroaminoacridine (THA) on social recognition in rats.四氢氨基吖啶(THA)对大鼠社会识别影响的行为学研究。
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