101526-83-4
101526-83-4 結(jié)構(gòu)式
基本信息
中文別名
司馬替利司美利特
英文別名
RU-752Sematilide
N-(DIETHYLAMINOETHYL)-4-METHYLSULFOAMINOBENZAMIDE
N-(2-(DiethylaMino)ethyl)-4-(MethylsulfonaMido)benzaMide
N-(2-Diethylaminoethyl)-4-(methylsulfonylamino)benzamide
N-[2-(DIETHYLAMINO)ETHYL]-4-(METHANESULFONAMIDO)BENZAMIDE
Benzamide,N-[2-(diethylamino)ethyl]-4-[(methylsulfonyl)amino]-
常見問題列表
生物活性
Sematilide (CK-1752) 是一種選擇性的 IKr 通道阻滯劑。Sematilide 抑制延遲整流鉀通道 (K+ current)，IC50 為 25 μM，這種作用存在濃度依賴性。Sematilide 是一種 III 類抗心律不齊劑。靶點
IC50: 25 μM (K + current)
體外研究
Application of 10, 30, 100 and 300 μM Sematilide causes a concentration-dependent inhibition of the delayed rectifier K + current (IC 50 =25 μM).
體內(nèi)研究
Sematilide (0.3-1.0 mg/kg, intravenously i.v.) is effective in a canine model of arrhythmia.
| Animal Model: | Mongrel dogs of either sex (10-18 kg body weight) |
| Dosage: | 0.3, 1, 3, and 10 mg/kg |
| Administration: | I.v. infusions |
| Result: | Demonstrated antiarrhythmic effects at 0.3 and 3.0 mg/kg. |