弗斯特罗定
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- CAS号:
- 286930-02-7
- 英文名:
- (R) Fesoterodine
- 英文别名:
- PF-00695838;Fesoterodine;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
- 中文名:
- 弗斯特罗定
- 中文别名:
- 弗斯特罗定;富马酸弗斯特罗定杂质
- CBNumber:
- CB61175365
- 分子式:
- C26H37NO3
- 分子量:
- 411.58
- MOL File:
- 286930-02-7.mol
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弗斯特罗定化学性质
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密度:
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1.043
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储存条件:
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Store at -20°C,unstable in solution, ready to use.
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溶解度:
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Ethanol: 100 mg/mL (242.97 mM)
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弗斯特罗定性质、用途与生产工艺
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。
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)。
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)。
pKi: 8.0 (M1), 7.7 (M2), 7.4 (M3), 7.3 (M4) and 7.5 (M5)
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).
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.
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Animal Model:
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Bladders from female Sprague-Dawley rats (225-275 g)
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Dosage:
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0.01, 0.1 and 1 mg/kg
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Administration:
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IV
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Result:
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Reduced the micturition pressure and increased bladder capacity and ICIs at the lowest dose tested of 0.01 mg/kg.
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弗斯特罗定
上下游产品信息
上游原料
下游产品
286930-02-7, 弗斯特罗定 相关搜索:
- 266930-03-8
- 富马酸弗斯特罗定杂质
- 弗斯特罗定
- 286930-02-7
- Desfesoterodine,Fesoterodine,OAB,muscarinic,overactive,Inhibitor,SPM7605,mAChR,orally,5-HMT,antimuscarinic,bladder,Muscarinic acetylcholine receptor,inhibit,receptor
- 2-Methylpropionic acid 2-[3-(N,N-diisopropylamino)-1(R)-phen...
- PF-00695838
- (R)-2-(3-(diisopropylamino)-1-phenylpropyl)-4-(hydroxymethyl)phenyl isobutyrate
- Unii-621G617227
- Fesoterodine
- 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
- (R) Fesoterodine