奥美拉唑钠

奥美拉唑钠用途

Omeprazole (H 16868) 是一种质子泵 (proton pump) 抑制剂 (PPI),有潜力用于胃肠道疾病的研究。Omeprazole 竞争性抑制 CYP2C19 活性,Ki 为 2 到 6 μM。Omeprazole 还抑制革兰氏阳性菌和革兰氏阴性菌生长。Omeprazole 是中性鞘磷脂酶 (N-SMase) 的抑制剂(外泌体抑制剂)。

奥美拉唑钠名称

[ CAS 号 ]:
95510-70-6

[ 中文名 ]:
奥美拉唑钠

[ 英文名 ]:
Omeprazole sodium monohydrate

[中文别名 ]:

[英文别名 ]:

Omeprazole powder/pellets/sodium
MFCD01939422
Omeprazole sodium hydrate
Omeprazole,sodium salt

奥美拉唑钠生物活性

[ 描述 ]:

[ 相关类别 ]:

研究领域 >> 癌症

研究领域 >> 感染

信号通路 >> 代谢酶/蛋白酶 >> 磷脂

信号通路 >> 自噬 >> 自噬

研究领域 >> 代谢疾病

信号通路 >> 跨膜转运 >> 质子泵

信号通路 >> 抗感染 >> 细菌

[体外研究]

奥美拉唑(h16868)是一种质子泵抑制剂,用于治疗消化不良、消化性溃疡病、胃食管反流病、咽喉反流和Zollinger-Ellison综合征。奥美拉唑(H 16868)几乎消除了所有患者的胃内酸度：24小时胃内pH值中位数从1.4上升到5.3,平均小时氢离子活性从38.50降至1.95 mmol(mEq)/1(p<0.001)。这种对24小时胃内酸性的抑制作用比以前报道的每天服用1克西咪替丁或每天服用300毫克雷尼替丁更为深刻[1]。研究了一组健康男性受试者单次和多次口服30和60毫克奥美拉唑的药代动力学。奥美拉唑(H 16868)从其肠溶制剂中的吸收是不可预测的。反复给药后,血浆浓度-时间曲线(AUC)下面积显著增加。奥美拉唑(H 16868)在反复给药后增加自身的相对可用性。这可能是由于奥美拉唑(一种不耐酸的化合物)抑制胃酸分泌所致[2]。奥美拉唑钠是一种有效的脑渗透剂中性鞘磷脂酶(N-SMase)抑制剂(外显体抑制剂)[3]。

[参考文献]

[1]. Li XQ, et al. Comparison of inhibitory effects of the proton pump-inhibiting drugs omeprazole, esomeprazole, lansoprazole, pantoprazole, and rabeprazole on human cytochrome P450 activities. Drug Metab Dispos. 2004 Aug;32(8):821-7.

[2]. Jonkers D, et al. Omeprazole inhibits growth of gram-positive and gram-negative bacteria including Helicobacter pylori in vitro. J Antimicrob Chemother. 1996 Jan;37(1):145-50.

[3]. Huarui Zhang, et al. Advances in the discovery of exosome inhibitors in cancer. J Enzyme Inhib Med Chem. 2020 Dec;35(1):1322-1330.

奥美拉唑钠物理化学性质

[ 密度 ]:
1.37g/cm3

[ 沸点 ]:
600ºC at 760mmHg

[ 熔点 ]:
220°C

[ 分子式 ]:
C₁₇H₂₀N₃NaO₄S

[ 分子量 ]:
385.413

[ 闪点 ]:
316.7ºC

[ 精确质量 ]:
385.107208

[ PSA ]:
94.68000

[ LogP ]:
3.48690

[ 外观性状 ]:
在水中透明

[ 储存条件 ]:
室温

奥美拉唑钠毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: DD9088500

CHEMICAL NAME :: 1H-Benzimidazole, 5-methoxy-2-(((4-methoxy-3,5-dimethyl-2-pyridinyl)met hyl)sulfinyl)-, sodium salt, hydrate

CAS REGISTRY NUMBER :: 95510-70-6

LAST UPDATED :: 199512

DATA ITEMS CITED :: 6

MOLECULAR FORMULA :: C17-H18-N3-O3-S.Na.H2-O

MOLECULAR WEIGHT :: 385.45

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 278 mg/kg

TOXIC EFFECTS :: Behavioral - somnolence (general depressed activity) Behavioral - convulsions or effect on seizure threshold Lungs, Thorax, or Respiration - dyspnea

REFERENCE :: OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180, Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 49,479,1995

TYPE OF TEST :: LDLo - Lowest published lethal dose

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Mammal - dog

DOSE/DURATION :: 400 mg/kg

TOXIC EFFECTS :: Behavioral - somnolence (general depressed activity) Behavioral - convulsions or effect on seizure threshold Gastrointestinal - changes in structure or function of salivary glands

REFERENCE :: OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180, Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 49,497,1995 ** OTHER MULTIPLE DOSE TOXICITY DATA **

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 4550 mg/kg/13W-I

TOXIC EFFECTS :: Gastrointestinal - other changes Skin and Appendages - dermatitis, other (after systemic exposure)

REFERENCE :: OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180, Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 49,479,1995

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Mammal - dog

DOSE/DURATION :: 328 mg/kg/13W-I

TOXIC EFFECTS :: Kidney, Ureter, Bladder - changes in bladder weight

REFERENCE :: OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180, Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 49,497,1995 ** REPRODUCTIVE DATA **

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Intravenous

DOSE :: 8400 mg/kg

SEX/DURATION :: male 9 week(s) pre-mating female 2 week(s) pre-mating - 7 day(s) after conception

TOXIC EFFECTS :: Reproductive - Paternal Effects - testes, epididymis, sperm duct Reproductive - Fertility - pre-implantation mortality (e.g. reduction in number of implants per female; total number of implants per corpora lutea) Reproductive - Fertility - post-implantation mortality (e.g. dead and/or resorbed implants per total number of implants)

REFERENCE :: OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180, Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 49,573,1995

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Intravenous

DOSE :: 83200 ug/kg

SEX/DURATION :: female 17-21 day(s) after conception lactating female 21 day(s) post-birth

TOXIC EFFECTS :: Reproductive - Effects on Newborn - growth statistics (e.g.%, reduced weight gain)

REFERENCE :: OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180, Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 49,573,1995

奥美拉唑钠安全信息

[ 海关编码 ]:
2933990090

奥美拉唑钠海关

[ 海关编码 ]: 2933990090

[ 中文概述 ]:
2933990090. 其他仅含氮杂原子的杂环化合物. 增值税率:17.0%. 退税率:13.0%. 监管条件:无. 最惠国关税:6.5%. 普通关税:20.0%

[ 申报要素 ]: 品名, 成分含量, 用途, 乌洛托品请注明外观, 6－己内酰胺请注明外观, 签约日期

[ Summary ]:
2933990090. heterocyclic compounds with nitrogen hetero-atom(s) only. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0%