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Hydroxytacrine(maleate)
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Hydroxytacrine(maleate)图片
CAS NO:118909-22-1
包装与价格:
包装价格(元)
100mg电议
250mg电议
1g电议

产品介绍
anticholinesterase activity
Cas No.118909-22-1
别名马来酸维吖啶,HP 029,1-Hydroxytacrine,P 83-6029A,Velnacrine
化学名9-amino-1,2,3,4-tetrahydro-1-acridinol, 2Z-butenedioate
Canonical SMILESNC1=C2C(CCCC2O)=NC3=CC=CC=C31.OC(/C=C\C(O)=O)=O
分子式C13H14N2O o C4H4O4
分子量330.3
溶解度≤30mg/ml in DMSO;2mg/ml in dimethyl formamide
储存条件Store at -20℃
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

Hydroxytacrine maleate, a bioactive monohydroxylated metabolite of cholinesterase inhibitor, is a potential Alzheimer's therapeutic of low toxicity [1]. Hydroxytacrine maleate exhibited biochemical and pharmacological profile similar to tacrine (THA) except that the far less liver toxicity in humans. The prolonged use of tacrine has been associated with liver toxicity[1, 2].

Hydroxytacrine maleate is a parasympathomimetic and a centrally acting cholinesterase inhibitor (anticholinesterase). As the first cholinesterase inhibitor approved for the treatment of AD, tacrine was marketed under the trade name Cognex [3]. Through hydroxylation of benzylic carbon by CYP450 in the liver, tacrine has been metabolized into metabolite 1-hydroxy-tacrine (velnacrine) [4]. It has also been shown that maleate is an inhibitor of AChE [5].

References:
[1].  D. Muoz-Torrero. Acetylcholinesterase inhibitors as disease-modifying therapies for Alzheimer’s disease. Curr. Med. Chem. 15, 2433-2455 (2008).
[2].  E. Giacobini. Cholinesterase inhibitors for Alzheimer’s disease therapy: From tacrine to future applications. Neurochemistry International 32, 413-419(1998).
[3].  Birks J S. Cholinesterase inhibitors for Alzheimer's disease[J]. The Cochrane Library, 2006.
[4].  Peng J Z, Remmel R P, Sawchuk R J. Inhibition of murine cytochrome P4501A by tacrine: in vitro studies[J]. Drug metabolism and disposition, 2004, 32(8): 805-812.
[5].  Acetylcholine and choline effects on erythrocyte nitrite and nitrate levels.