172152-36-2
172152-36-2 结构式
基本信息
奥普拉唑
艾普拉唑
伊拉普拉唑
艾普拉唑/奥普拉唑
艾普拉唑[干冰运输]
Ilaprazole(IY 81149)
Ilaprazole USP/EP/BP
IY81149
IY-81149
IY 81149
2-[(4-methoxy-3-methylpyridin-2-yl)methylsulfinyl]-6-pyrrol-1-yl-1H-benzimidazole
2-[(4-methoxy-3-methyl-pyridin-2-yl)methylsulfinyl]-5-pyrrol-1-yl-3H-benzoimidazole
2-[[(4-Methoxy-3-methyl-2-pyridinyl)methyl]sulfinyl]5-(1H-pyrrol-1-yl) 1H benzimidazole
2-[[(4-Methoxy-3-methyl-2-pyridinyl)methyl]sulfinyl]-6-(1H-pyrrol-1-yl)-1H-benzimidazole
1H-BenziMidazole,2-[[(4-Methoxy-3-Methyl-2-pyridinyl)Methyl]sulfinyl]-6-(1H-pyrrol-1-yl)-
2-[(4-methoxy-3-methyl-pyridin-2-yl)methylsulfinyl]-5-pyrrol-1-yl-3H-benzoimidazole USP/EP/BP
物理化学性质
常见问题列表
艾普拉唑属不可逆型质子泵抑制剂，其结构属于苯并咪唑类。艾普拉唑经口服后 选择性地进入胃壁细胞，转化为次磺酰胺活性代谢物，与H + /K+ -ATP酶上的巯基作 用，形成二硫键的共价结合，不可逆抑制H + /K+ -ATP酶，产生抑制胃酸分泌的作用。
艾普拉唑的普遍副作用有（发病率超过1%、低于10%）有腹泻（2.41%）、头晕目眩（2.41%）、血细胞转氨酶（ALT/AST）上升（1.81%）；罕见副作用（发病率超过0.1%、低于1%）有皮疹、荨麻疹、腰痛、腹胀、口干口苦口臭、胸闷气短、心悸、月经时间增加、肾功能异常（蛋白尿、BUN上升）、心电图异常（室性期前收缩、I度房室传导阻滞）、白细胞减少等。所述副作用常以轻、轻中度，可自主修复。
| Target | Value |
|
Proton pump
() | |
|
H+/K+-ATPase
(Cell-free assay) | 6 μM |
|
TOPK
() | 111 μM(Kd) |
On cumulation of 14C-aminopyrine in histamine stimulated parietal cells, the IC 50 of Ilaprazole (IY-81149) sodium is 9 nM.
Ilaprazole (3-30 mg/kg; i.d.) dose-dependently inhibits gastric acid secretion.
In anesthetized rats, Ilaprazole dose-dependently increased gastric pH which was lowered by histamine infusion. In the case of i.v. injection, the ED
50
of Ilaprazole and omeprazole is 1.2 and 1.4 mg/kg and in the case of i.d. administration, the ED
50
of Ilaprazole and omeprazole is 3.9 and 4.1 mg/kg, respectively. Ilaprazole also significantly inhibits pentagastrin-stimulated gastric secretion. Its ED
50
is 2.1 mg/kg and that of Omeprazole is 3.5 mg/kg with i.d. administration. In the case of i.v. injection, Ilaprazole is equipotent to Omeprazole. Ilaprazole also inhibits gastric acid secretion strongly in fistular rats. The ED
50
of Ilaprazole administered intraduodenally is 0.43 mg/kg and that of Omeprazole is 0.68 mg/kg.
| Animal Model: | Male SD rat (after pylorus ligation) |
| Dosage: | 3, 10, 30 mg/kg |
| Administration: | Intraduodenally |
| Result: | The acid output and volume significantly inhibited by about 60 % and 46 % at 3 mg/kg were s, respectively. At 30 mg/kg, it showed 93 % and 73 % inhibition on acid output and volume, respectively. |