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Ciproxifan 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。
Ciproxifan maleate图片
CAS NO:184025-19-2
包装与价格：
包装价格(元)
5mg电议
25mg电议

产品介绍
Ciproxifan maleate (FUB 359 maleate) 是一种有效的、选择性的、具有口服生物利用度和竞争性的组胺 H3 受体拮抗剂，IC50 为 9.2 nM。
Cas No.184025-19-2
别名环丙基[4-[3-(1H-咪唑-4-基)丙氧基]苯基]甲酮马来酸盐,FUB 359 maleate
化学名(Z)-but-2-enedioic acid;cyclopropyl-[4-[3-(1H-imidazol-5-yl)propoxy]phenyl]methanone
Canonical SMILESC1CC1C(=O)C2=CC=C(C=C2)OCCCC3=CN=CN3.C(=CC(=O)O)C(=O)O
分子式C20H22N2O6
分子量386.4
溶解度Soluble in DMSO
储存条件Store at -20°C
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

Ciproxifan maleate(FUB-359 maleate) is a highly potent and selective histamin H3-receptor antagonist with IC50 of 9.2 nM, with low apparent affinity at other receptor subtypes.IC50 value: Target: H3 receptorIn vitro, Ciproxifan behaved as a competitive antagonist at the H3 autoreceptor controlling 3H histamine release from synaptosomes and displayed similar Ki values (0.5-1.9 nM) at the H3 receptor controlling the electrically-induced contraction of guinea pig ileum or at the brain H3 receptor labeled with 125I-iodoproxyfan. This appears to be an orally bioavailable, extremely selective and potent H3-receptor antagonist whose vigilance- and attention-promoting effects are promising for therapeutic applications in aging disorders.

References:
[1]. Motawaj M, Arrang JM.Ciproxifan, a histamine H -receptor antagonist / inverse agonist, modulates methamphetamine-induced sensitization in mice.Eur J Neurosci. 2011 Apr;33(7):1197-204. doi: 10.1111/j.1460-9568.2011.07618.x.
[2]. Bardgett ME, Davis NN, Schultheis PJ, Griffith MS. Ciproxifan, an H3 receptor antagonist, alleviates hyperactivity and cognitive deficits in the APP Tg2576 mouse model of Alzheimer's disease. Neurobiol Learn Mem. 2011 Jan;95(1):64-72.
[3]. Bardgett ME, Points M, Kleier J, Blankenship M, Griffith MS. The H3 antagonist, ciproxifan, alleviates the memory impairment but enhances the motor effects of MK-801 (dizocilpine) in rats. Neuropharmacology. 2010 Nov;59(6):492-502.
[4]. Day M, et al . Differential effects of ciproxifan and nicotine on impulsivity and attention measures in the 5-choice serial reaction time test. Biochem Pharmacol. 2007 Apr 15;73(8):1123-34.
[5]. Pillot C, Héron A, Schwartz JC, Arrang JM. Ciproxifan, a histamine H3-receptor antagonist/inverse agonist, modulates the effects of methamphetamine on neuropeptide mRNA expression in rat striatum. Eur J Neurosci. 2003 Jan;17(2):307-14.