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172152-50-0

中文名稱 艾普拉唑鈉
英文名稱 Ilaprazole sodium
CAS 172152-50-0
分子式 C19H19N4NaO2S
分子量 390.44
MOL 文件 172152-50-0.mol
更新日期 2024/12/17 16:14:26
172152-50-0 結(jié)構(gòu)式 172152-50-0 結(jié)構(gòu)式

基本信息

中文別名
艾普拉唑鈉
英文別名
IY-81149 sodium
Ilaprazole sodium
Sodium ilaprazole
Ilaprazole sodium USP/EP/BP
所屬類別
原料藥:胃腸動(dòng)力藥

物理化學(xué)性質(zhì)

儲(chǔ)存條件4°C, protect from light
形態(tài)Solid
顏色White to off-white
CAS 數(shù)據(jù)庫172152-50-0

常見問題列表

概述
艾普拉唑是麗珠集團(tuán)2007年全球首家上市的新型強(qiáng)效質(zhì)子泵抑制腸溶片,適用于十二指腸潰瘍和反流性食管炎。其抑酸活性是奧美拉唑的4倍以上,奧美拉唑腸溶制劑的日服量為40mg,艾普拉唑則只需5~10mg;半衰期長,體內(nèi)作用時(shí)間長,不經(jīng)過CYP2C19代謝,也很少通過CYP3A4酶代謝,對(duì)不同基因型患者無個(gè)體差異;不良反應(yīng)更少。為適應(yīng)消化道出血的患者,發(fā)揮艾普拉唑抑酸作用強(qiáng)的特點(diǎn),使胃內(nèi)pH迅速達(dá)到6以上,止血因子快速起效。
藥理作用
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。在小鼠、大鼠、豚鼠和比格犬上進(jìn)行了艾普拉唑的藥理實(shí)驗(yàn),發(fā)現(xiàn)艾普拉唑?qū)?dòng)物的心血管系統(tǒng)、自主神經(jīng)系統(tǒng)和平滑肌功能沒有影響,給予1~3mg/kg時(shí),艾普拉唑抑酸效果顯著,且呈劑量依賴性。
生物活性
Ilaprazole (IY-81149) sodium,一種具有口服活性質(zhì)子泵抑制劑,以劑量依賴性方式不可逆地抑制H+/K+-ATPase,在兔壁細(xì)胞制劑中的 IC50 為 6 μM。Ilaprazole sodium 用于胃潰瘍的研究。Ilaprazole sodium 也是一種有效的T細(xì)胞起源蛋白激酶 (TOPK) 抑制劑。
靶點(diǎn)
TargetValue
Proton pump
()
H(+)/K(+)-ATPase
(in rabbit parietal cell preparation)
6 μM
體外研究

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

體內(nèi)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.
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