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 SMILES | N/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 tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
| Shipping Condition | Evaluation 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. |
