1206695-46-6
中文名稱
(R)-2-(3-(二異丙基氨基)-1-苯基丙基)-4-(羥基甲基)苯基異丁酸酯(S)-2-羥基-2
英文名稱
Fesoterodine ((S)-2-hydroxy-2-phenylacetic acid)
CAS
1206695-46-6
分子式
C34H45NO6
分子量
563.724
MOL 文件
1206695-46-6.mol
1206695-46-6 結構式
基本信息
中文別名
弗斯特羅定扁桃酸鹽FESOTERODINE L-MANDELATE
(R)-2-(3-(二異丙基氨基)-1-苯基丙基)-4-(羥基甲基)苯基異丁酸酯(S)-2-羥基-2
(R)-2-(3-(二異丙基氨基)-1-苯基丙基)-4-(羥基甲基)苯基異丁酸酯(S)-2-羥基-2-苯基乙酸酯
英文別名
Fesoterodine L-mandelateFesoterodine ((S)-2-hydroxy-2-phenylacetic acid)
2-[(1R)-3-[bis(1-methylethyl)amino]-1-phenylpropyl]-4-hydroxy-methylphenyl isobutyrate mandelate
常見問題列表
生物活性
Fesoterodine L-mandelate 是一種口服有效，非亞型選擇性的，競爭性毒蕈堿受體 (mAChR) 拮抗劑，對 M1，M2，M3，M4，M5 受體的 pKi 值分別為 8.0，7.7，7.4，7.3，7.5。Fesoterodine L-mandelate 用于膀胱過度活動癥 (OAB)。靶點
pKi: 8.0 (M1), 7.7 (M2), 7.4 (M3), 7.3 (M4) and 7.5 (M5)
體外研究
Fesoterodine L-mandelate decreases micturition frequency, urgency severity and urgency incontinence episodes and increases the volume voided with each micturition.
After oral administration, Fesoterodine L-mandelate is rapidly and extensively hydrolysed in plasma by nonspecific esterases to Desfesoterodine (5-hydroxymethyl tolterodine; SPM 7605; HY-76569; an active metabolite of Fesoterodine).
體內研究
Fesoterodine L-mandelate (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. |