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Tegaserod 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。
Tegaserod maleate图片
CAS NO:189188-57-6
包装与价格:
包装价格(元)
10mg电议
50mg电议

产品介绍
Tegaserod maleate 是一种选择性 5-HT4 受体部分激动剂和 5-HT2B 受体拮抗剂。
Cas No.189188-57-6
别名马来酸替加色罗; SDZ-HTF-919; HTF-919
化学名(E)-2-((Z)-(5-methoxy-3H-indol-3-ylidene)methyl)-N'-pentylhydrazinecarboximidamide maleate
Canonical SMILESN/C(NN/C=C1C2=CC(OC)=CC=C2N=C/1)=N\CCCCC.OC(/C=C\C(O)=O)=O
分子式C16H23N5O.C4H4O4
分子量417.46
溶解度DMF: 25 mg/ml,DMF:PBS (pH 7.2)(1:3): 0.03 mg/ml,DMSO: 20 mg/ml
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

Tegaserod maleate is a partial agonist of the 5-HT4 receptor; stimulates the peristaltic reflex and accelerates gastrointestinal transit.IC50 value:Target: 5-HT4 agonistIn an in vivo model for peripheral nerve regeneration, mice receiving tegaserod at the site of injury showed enhanced recovery compared to control mice receiving vehicle control as evidenced by functional measurements and histology [1]. Treatment with fluoxetine (10 mg · kg(-1) · day(-1), days 36-42), tegaserod (1 mg · kg(-1) · day(-1), day 43), or the combination of both, reduced visceral hypersensitivity and plasma 5-HT levels [2]. Intravenous or intraduodenal tegaserod (0.3-1.0 mg.kg(-1)) had no inhibitory effect on mesenteric and colonic blood flow. Peroral treatment of rats with alosetron or tegaserod for 7 days did not modify mesenteric haemodynamics at baseline and after blockade of nitric oxide synthesis [3].

References:
[1]. Bushman J, et al. Tegaserod mimics the neurostimulatory glycan polysialic acid and promotes nervous system repair. Neuropharmacology. 2014 Apr;79:456-66.
[2]. Yan C, et al. Effect of the 5-HT4 receptor and serotonin transporter on visceral hypersensitivity in rats. Braz J Med Biol Res. 2012 Oct;45(10):948-54.
[3]. Painsipp E, et al. Alosetron, cilansetron and tegaserod modify mesenteric but not colonic blood flow in rats. Br J Pharmacol. 2009 Nov;158(5):1210-26.