化学性质
| Physical Appearance | A crystalline solid |
| Storage | Store at -20°C |
| M.Wt | 330.3 |
| Cas No. | 118909-22-1 |
| Formula | C13H14N2O·C4H4O4 |
| Synonyms | HP 029,1-Hydroxytacrine,P 83-6029A,Velnacrine |
| Solubility | ≤30mg/ml in DMSO;2mg/ml in dimethyl formamide |
| Chemical Name | 9-amino-1,2,3,4-tetrahydro-1-acridinol, 2Z-butenedioate |
| Canonical SMILES | NC1=C2C(CCCC2O)=NC3=CC=CC=C31.OC(/C=C\C(O)=O)=O |
| 运输条件 | 蓝冰运输或根据您的需求运输。 |
| 一般建议 | 为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异，仅做参考。若实验所需浓度过大至产品溶解极限，请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存，请尽快用完。 |
资料参考
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.
