Fesoterodine Fumarate 是一种口服活性、非亚型选择性、竞争性毒蕈碱受体 (mAChR) 拮抗剂，对 M1、M2、M3、M4、M5 受体的 pKi 值分别为 8.0、7.7、7.4、7.3、7.5。
| Cas No. | 286930-03-8 |
| 别名 | 富马酸非索罗定 |
| 化学名 | (E)-but-2-enedioic acid;[2-[(1R)-3-[di(propan-2-yl)amino]-1-phenylpropyl]-4-(hydroxymethyl)phenyl] 2-methylpropanoate |
| Canonical SMILES | CC(C)C(=O)OC1=C(C=C(C=C1)CO)C(CCN(C(C)C)C(C)C)C2=CC=CC=C2.C(=CC(=O)O)C(=O)O |
| 分子式 | C30H41NO7 |
| 分子量 | 527.65 |
| 溶解度 | Methanol: Slightly Soluble,Water: Slightly Soluble |
| 储存条件 | Store at -20°C |
| 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 | Fesoterodine Fumarate is an antimuscarinic agent and is rapidly de-esterified to its active metabolite 5-hydroxymethyl tolterodine that is a muscarinic receptor antagonist.IC50 value:Target: mAChRFesoterodine has the advantage of allowing more flexible dosage than other muscarinic antagonists. Its tolerability and side effects are similar to other muscarinic antagonists and as a new drug seems unlikely to make great changes in practices of treatment for overactive bladder. References:
[1]. Staskin David; Khullar Vik; Michel Martin C et al. Effects of voluntary dose escalation in a placebo-controlled, flexible-dose trial of fesoterodine in subjects with overactive bladder. Neurourology and urodynamics (2011), 30(8), 1480-5.
[2]. Vella Maria; Cardozo Linda Review of fesoterodine. Expert opinion on drug safety (2011), 10(5), 805-8.
[3]. Malhotra Bimal; Alvey Christine; Gong Jason et al. Effects of fesoterodine on the pharmacokinetics and pharmacodynamics of warfarin in healthy volunteers. British journal of clinical pharmacology (2011), 72(2), 257-62.
[4]. Michel MC. Fesoterodine: a novel muscarinic receptor antagonist for the treatment of overactive bladder syndrome. Expert Opin Pharmacother. 2008 Jul;9(10):1787-96.
[5]. Fesoterodine |
