286930-02-7
286930-02-7 结构式
基本信息
中文别名
弗斯特罗定富马酸弗斯特罗定杂质
英文别名
PF-00695838Fesoterodine
Unii-621G617227
(R) Fesoterodine
2-Methylpropionic acid 2-[3-(N,N-diisopropylamino)-1(R)-phen...
(R)-2-(3-(diisopropylamino)-1-phenylpropyl)-4-(hydroxymethyl)phenyl isobutyrate
2-Methylpropanoic acid 2-[(1R)-3-[bis(1-methylethyl)amino]-1-phenylpropyl]-4-(hydroxymethyl)phenyl ester
Propanoic Acid 2-Methyl- 2-[(1R)-3-[bis(1-methylethyl)amino]-1-phenylpropyl]-4-(hydroxymethyl)phenyl Ester
Desfesoterodine,Fesoterodine,OAB,muscarinic,overactive,Inhibitor,SPM7605,mAChR,orally,5-HMT,antimuscarinic,bladder,Muscarinic acetylcholine receptor,inhibit,receptor
物理化学性质
密度1.043
储存条件Store at -20°C,unstable in solution, ready to use.
溶解度Ethanol: 100 mg/mL (242.97 mM)
形态Viscous Liquid
颜色Colorless to light yellow
常见问题列表
概述
弗斯特罗定(fesoterodine，商品名ToviazTM)是一种新型M受体阻滞剂，在体内迅速代谢成活性代谢产物而发挥作用。用途
弗斯特罗定于2008年10月31日获得美国FDA批准上市，用于治疗膀胱过度活动症(overactivebladder，OAB)。生物活性
Fesoterodine 是一种口服有效，非亚型选择性的，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。Fesoterodine 用于膀胱过度活动症 (OAB)。靶点
pKi: 8.0 (M1), 7.7 (M2), 7.4 (M3), 7.3 (M4) and 7.5 (M5)
体外研究
Fesoterodine decreases micturition frequency, urgency severity and urgency incontinence episodes and increases the volume voided with each micturition.
After oral administration, Fesoterodine is rapidly and extensively hydrolysed in plasma by nonspecific esterases to Desfesoterodine (5-hydroxymethyl tolterodine; SPM 7605; HY-76569; an active metabolite of Fesoterodine).
体内研究
Fesoterodine (0.01-1 mg/kg; IV) reduces the micturition pressure and increases bladder capacity and ICIs (intercontraction intervas) at the lowest dose tested of 0.01 mg/kg.
| Animal Model: | Bladders from female Sprague-Dawley rats (225-275 g) |
| Dosage: | 0.01, 0.1 and 1 mg/kg |
| Administration: | IV |
| Result: | Reduced the micturition pressure and increased bladder capacity and ICIs at the lowest dose tested of 0.01 mg/kg. |