172152-36-2
172152-36-2 結(jié)構(gòu)式
基本信息
奧普拉唑
艾普拉唑
伊拉普拉唑
艾普拉唑/奧普拉唑
艾普拉唑[干冰運(yùn)輸]
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
物理化學(xué)性質(zhì)
常見問題列表
艾普拉唑?qū)俨豢赡嫘唾|(zhì)子泵抑制劑，其結(jié)構(gòu)屬于苯并咪唑類。艾普拉唑經(jīng)口服后 選擇性地進(jìn)入胃壁細(xì)胞，轉(zhuǎn)化為次磺酰胺活性代謝物，與H + /K+ -ATP酶上的巰基作 用，形成二硫鍵的共價(jià)結(jié)合，不可逆抑制H + /K+ -ATP酶，產(chǎn)生抑制胃酸分泌的作用。
艾普拉唑的普遍副作用有（發(fā)病率超過1%、低于10%）有腹瀉（2.41%）、頭暈?zāi)垦＃?.41%）、血細(xì)胞轉(zhuǎn)氨酶（ALT/AST）上升（1.81%）；罕見副作用（發(fā)病率超過0.1%、低于1%）有皮疹、蕁麻疹、腰痛、腹脹、口干口苦口臭、胸悶氣短、心悸、月經(jīng)時(shí)間增加、腎功能異常（蛋白尿、BUN上升）、心電圖異常（室性期前收縮、I度房室傳導(dǎo)阻滯）、白細(xì)胞減少等。所述副作用常以輕、輕中度，可自主修復(fù)。
| 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. |