弗斯特羅定
| 中文名稱 | 弗斯特羅定 |
|---|---|
| 中文同義詞 | 弗斯特羅定;富馬酸弗斯特羅定雜質(zhì) |
| 英文名稱 | (R) Fesoterodine |
| 英文同義詞 | (R) Fesoterodine;Propanoic Acid 2-Methyl- 2-[(1R)-3-[bis(1-methylethyl)amino]-1-phenylpropyl]-4-(hydroxymethyl)phenyl Ester;2-Methylpropanoic acid 2-[(1R)-3-[bis(1-methylethyl)amino]-1-phenylpropyl]-4-(hydroxymethyl)phenyl ester;Fesoterodine;Unii-621G617227;(R)-2-(3-(diisopropylamino)-1-phenylpropyl)-4-(hydroxymethyl)phenyl isobutyrate;PF-00695838;2-Methylpropionic acid 2-[3-(N,N-diisopropylamino)-1(R)-phen... |
| CAS號(hào) | 286930-02-7 |
| 分子式 | C26H37NO3 |
| 分子量 | 411.58 |
| EINECS號(hào) | |
| 相關(guān)類別 | |
| Mol文件 | 286930-02-7.mol |
| 結(jié)構(gòu)式 |  |
弗斯特羅定 性質(zhì)
| 密度 | 1.043 |
|---|---|
| 儲(chǔ)存條件 | Store at -20°C,unstable in solution, ready to use. |
| 溶解度 | 乙醇：100 mg/ml（242.97 mM） |
| 形態(tài) | 粘稠液體 |
| 顏色 | 無(wú)色至淺黃 |
弗斯特羅定(fesoterodine，商品名ToviazTM)是一種新型M受體阻滯劑，在體內(nèi)迅速代謝成活性代謝產(chǎn)物而發(fā)揮作用。弗斯特羅定于2008年10月31日獲得美國(guó)FDA批準(zhǔn)上市，用于治療膀胱過度活動(dòng)癥(overactivebladder，OAB)。Fesoterodine 是一種口服有效，非亞型選擇性的，競(jìng)爭(zhēng)性毒蕈堿受體 (mAChR) 拮抗劑，對(duì) M1，M2，M3，M4，M5 受體的 pKi 值分別為 8.0，7.7，7.4，7.3，7.5。Fesoterodine 用于膀胱過度活動(dòng)癥 (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.
| 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. |