艾普拉唑钠

概述药理作用生物活性靶点体外研究体内研究艾普拉唑钠试剂级价格

艾普拉唑钠

CAS号:172152-50-0
英文名:Ilaprazole sodium
中文名:艾普拉唑钠
CBNumber:CB12748578
分子式:C19H19N4NaO2S
分子量:390.44
MOL File:172152-50-0.mol

艾普拉唑钠化学性质

储存条件 :4°C, protect from light
CAS 数据库 :172152-50-0

艾普拉唑钠性质、用途与生产工艺

概述艾普拉唑是丽珠集团2007年全球首家上市的新型强效质子泵抑制肠溶片，适用于十二指肠溃疡和反流性食管炎。其抑酸活性是奥美拉唑的4倍以上，奥美拉唑肠溶制剂的日服量为40mg，艾普拉唑则只需5～10mg；半衰期长，体内作用时间长，不经过CYP2C19代谢，也很少通过CYP3A4酶代谢，对不同基因型患者无个体差异；不良反应更少。为适应消化道出血的患者，发挥艾普拉唑抑酸作用强的特点，使胃内pH迅速达到6以上，止血因子快速起效。
药理作用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。在小鼠、大鼠、豚鼠和比格犬上进行了艾普拉唑的药理实验，发现艾普拉唑对动物的心血管系统、自主神经系统和平滑肌功能没有影响，给予1～3mg/kg时，艾普拉唑抑酸效果显著，且呈剂量依赖性。
生物活性 Ilaprazole (IY-81149) sodium，一种具有口服活性质子泵抑制剂，以剂量依赖性方式不可逆地抑制H+/K+-ATPase，在兔壁细胞制剂中的 IC50 为 6 μM。Ilaprazole sodium 用于胃溃疡的研究。Ilaprazole sodium 也是一种有效的T细胞起源蛋白激酶 (TOPK) 抑制剂。
靶点
Target Value
Proton pump
()
H(+)/K(+)-ATPase
(in rabbit parietal cell preparation) 6 μM
体外研究

On cumulation of 14C-aminopyrine in histamine stimulated parietal cells, the IC ₅₀ of Ilaprazole (IY-81149) sodium is 9 nM.

体内研究

Ilaprazole sodium (3-30 mg/kg; i.d.) dose-dependently inhibits gastric acid secretion.
In anesthetized rats, Ilaprazole sodium dose-dependently increases gastric pH which is lowered by histamine infusion. In the case of i.v. injection, the ED ₅₀ of Ilaprazole sodium and Omeprazole is 1.2 and 1.4 mg/kg and in the case of i.d. administration, the ED ₅₀ of Ilaprazole sodium and omeprazole is 3.9 and 4.1 mg/kg, respectively. Ilaprazole sodium also significantly inhibits pentagastrin-stimulated gastric secretion. Its ED ₅₀ is 2.1 mg/kg and that of Omeprazole was 3.5 mg/kg with i.d. administration. In the case of i.v. injection, Ilaprazole sodium is equipotent to Omeprazole. Ilaprazole sodium also inhibits gastric acid secretion strongly in fistular rats. The ED ₅₀ of Ilaprazole sodium 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.