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9-氨基-1,2,3,4-四氢吖啶(THA)是一种用于治疗阿尔茨海默病的候选药物,对其与红细胞膜相互作用的自旋标记研究。

Spin-labelling studies of the interaction of 9-amino-1,2,3,4-tetrahydroacridine (THA), a proposed drug for the treatment of Alzheimer's disease, with erythrocyte membranes.

作者信息

Butterfield D A, Palmieri D A

机构信息

Department of Chemistry, University of Kentucky, Lexington 40506-0055.

出版信息

Free Radic Res Commun. 1990;9(3-6):361-6. doi: 10.3109/10715769009145695.

DOI:10.3109/10715769009145695
PMID:2167274
Abstract

ESR spin labels specific for skeletal proteins or cell-surface sialic acid have been used to monitor the interaction of 9-amino-1,2,3,4-tetrahydroacridine (THA) and its structural analogs with human erythrocyte membranes. The results suggest that THA significantly increases skeletal protein-protein interactions and may secondarily alter the physical state of the opposite side of the membrane. The fully aromatic analog of THA, 9-aminoacridine, showed even more pronounced effects on skeletal proteins than did THA. These results are discussed in relation to possible interaction sites of THA in erythrocyte ghosts and to potential mechanisms by which THA reportedly increases mental function of victims of Alzheimer's disease.

摘要

针对骨骼蛋白或细胞表面唾液酸的电子自旋共振(ESR)自旋标记已被用于监测9-氨基-1,2,3,4-四氢吖啶(THA)及其结构类似物与人红细胞膜的相互作用。结果表明,THA显著增加了骨骼蛋白-蛋白相互作用,并可能继而改变膜另一侧的物理状态。THA的全芳香族类似物9-氨基吖啶对骨骼蛋白的影响比THA更为显著。本文结合THA在红细胞血影中的可能相互作用位点以及据报道THA增强阿尔茨海默病患者心理功能的潜在机制对这些结果进行了讨论。

相似文献

1
Spin-labelling studies of the interaction of 9-amino-1,2,3,4-tetrahydroacridine (THA), a proposed drug for the treatment of Alzheimer's disease, with erythrocyte membranes.9-氨基-1,2,3,4-四氢吖啶(THA)是一种用于治疗阿尔茨海默病的候选药物,对其与红细胞膜相互作用的自旋标记研究。
Free Radic Res Commun. 1990;9(3-6):361-6. doi: 10.3109/10715769009145695.
2
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.
3
Structure-activity investigation of the alteration of the physical state of the skeletal network of proteins in human erythrocyte membranes induced by 9-amino-1,2,3,4-tetrahydroacridine.9-氨基-1,2,3,4-四氢吖啶诱导人红细胞膜中蛋白质骨架网络物理状态改变的构效关系研究
Biochim Biophys Acta. 1990 May 24;1024(2):285-8. doi: 10.1016/0005-2736(90)90356-s.
4
Membrane-altering effects of velnacrine and N-methylacridinium: relevance to tacrine and Alzheimer's disease.维那克林和N-甲基吖啶鎓的膜改变作用:与他克林及阿尔茨海默病的相关性
Biochem Biophys Res Commun. 1992 Jun 15;185(2):596-603. doi: 10.1016/0006-291x(92)91666-e.
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Morphological alterations in erythrocyte membranes induced by 9-amino-1,2,3,4-tetrahydroacridine and 9-aminoacridine.9-氨基-1,2,3,4-四氢吖啶和9-氨基吖啶诱导的红细胞膜形态学改变
Biochem Biophys Res Commun. 1989 Sep 29;163(3):1351-5. doi: 10.1016/0006-291x(89)91127-3.
6
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.
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Electron spin resonance and biochemical studies of the interaction of the polyamine, spermine, with the skeletal network of proteins in human erythrocyte membranes.多胺精胺与人红细胞膜中蛋白质骨架网络相互作用的电子自旋共振及生化研究。
Biochim Biophys Acta. 1988 Jun 22;941(2):141-9. doi: 10.1016/0005-2736(88)90174-5.
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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.
9
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.
10
ESR studies of the erythrocyte membrane skeletal protein network: influence of the state of aggregation of spectrin on the physical state of membrane proteins, bilayer lipids, and cell surface carbohydrates.红细胞膜骨架蛋白网络的电子自旋共振研究:血影蛋白聚集状态对膜蛋白、双层脂质及细胞表面碳水化合物物理状态的影响。
Biochim Biophys Acta. 1985 Dec 19;821(3):420-30. doi: 10.1016/0005-2736(85)90046-x.

引用本文的文献

1
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.