效果的口服zanapezil (tak - 147) 21天在腹侧海马乙酰胆碱和类层次的自由移动的老鼠。
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Hatip-Al-Khatib我Iwasaki K, Arai Yoshimitsu Y, T, Egashira N, K三岛,Ikeda T,藤原M
效果的口服zanapezil (tak - 147) 21天在腹侧海马乙酰胆碱和类层次的自由移动的老鼠。
Br J杂志。2005年8月,145 (8):1035 - 44。
- PubMed ID
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15951830 (在PubMed]
- 文摘
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Zanapezil (tak - 147 (3 - [1 benzylpiperdin-4-yl] 1 - (2、3、4, 5-tetrahydro-1 H-1-benzazepin-8-yl) propan-1-one延胡索酸酯))是一种选择性乙酰胆碱酯酶抑制剂(ACh)在调查中作为阿尔茨海默病(AD)的药物治疗。在这项研究中,tak - 147 2毫克公斤的影响(1)21天,卖方与多奈哌齐(E2020)相比,乙酰胆碱的水平,catecolamines和吲哚胺调查在腹侧海马(VH) microdialysis-high-performance液相色谱的自由移动的老鼠。结果显示,VH包含92.05 + / - -21.97 fmol 20 microl (1) ACh和下面的类级别(pg 30 microl(1))、去甲肾上腺素(NE) 1.92 + / - -0.39,肾上腺素(Epi) 1.91 + / - -0.183, 3-methoxy-4-hydroxyphenylglycol (MHPG) 11.53 + / - -3.22, normetanephrine 3.26 + / - -0.61,多巴胺(DA) 0.77 + / - -0.23, 3, 4-dihydroxyphenylacetic酸(DOPAC) 3.37 + / - -1.01,高香草酸(4-hydroxy-3-methoxyphenylacetic酸;HVA) 4.04 + / - -0.93, 3-methoxytyramine 0.64 + / - -0.13, 5 -羟色胺(5 -)0.73 + / - -0.16和5-hydroxyindoleacetic酸(5-HIAA) 313.15 + / - -18.42。21天前最后一次剂量,tak - 147增加,Epi, DA和5,而E2020 MHPG增加,Epi哒。最后剂量后,tak - 147不增加,而E2020增加NE,疼或者5 -除了之前最后一个剂量的影响。tak - 147减少HVA:达比,但略微减少DOPAC: DA和5-HIAA: 5 -比率。另一方面,E2020 HVA的下降比率:哒,DOPAC: DA(前最后一次剂量),和5-HIAA: 5 -(90 - 180分钟后最后剂量)。这两种药物减少MHPG:不只是在180分钟后最后剂量。结果还表明,tak - 147增加Epi:东北比之前和120分钟后过去的剂量,而只E2020增加了比之前最后的剂量。 The present results show that TAK-147 at a subthreshold dose could differentially increase ACh and 5-HT, compared to MHPG increased by E2020. The last dose of each drug could extend their effects to other monoamines. The increase of the monoamines levels, in addition to that on the ACh, and decrease of their oxidation could be of value in the treatment of the AD, other dementic diseases and the cohort neurological disorders depending on the type of the monoamine underlying the disorder.