Roxatidine Acetate HCl

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Chemical Structure| 93793-83-0 同义名 : HOE 760;Roxatidine Acetate (hydrochloride);TZU-0460;Roxatidine Acetate Hydrochloride
CAS号 : 93793-83-0
货号 : A584050
分子式 : C19H29ClN2O4
纯度 : 98%
分子量 : 384.898
MDL号 : MFCD00941429
存储条件：

Pure form Inert atmosphere,2-8°C

In solvent -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 50 mg/mL(129.9 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO

H2O: 50 mg/mL(129.9 mM)
动物实验配方：
生物活性
靶点

  • H2 receptor

    Histamine H2 receptor, IC50:3.2 μM
描述 Roxatidine Acetate Hydrochloride is a specific and competitive H2-receptor antagonist. Roxatidine acetate and its main metabolite roxatidine inhibit histamine-induced gastric acid secretion in vitro with a potency greater than that of cimetidine, and in the range of that produced by ranitidine. In rats single or repeated dosing with roxatidine acetate did not influence drug metabolising enzymes in the liver nor did the drug show antiandrogenic activity in long term animal studies[3]. Human pharmacology studies and short-term and long-term clinical trials have all shown that roxatidine acetate is an exceptionally well tolerated compound, without the antiandrogenic activity and interference with hepatic drug metabolism which have characterized cimetidine treatment[4]. The pharmacodynamic and clinical data indicate that the efficacy of roxatidine acetate 75 mg twice-daily (b.i.d.) does not differ significantly from ranitidine 150 mg b.i.d. Roxatidine acetate is equally effective in the treatment of peptic disease including gastric ulcer, duodenal ulcer, and reflux esophagitis[5].
临床研究
NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT02555852 - Completed - Canada, Quebec ... 展开 >> Lady Davis Institute for Medical Research, Jewish General Hospital Montreal, Quebec, Canada, H3T1E2 收起 <<
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.60mL

0.52mL

0.26mL

12.99mL

2.60mL

1.30mL

25.98mL

5.20mL

2.60mL
参考文献

[1]Pali-Scholl I, Jensen-Jarolim E. Anti-acid medication as a risk factor for food allergy. Allergy. 2011 Apr;66(4):469-77.

[2]Murdoch D, McTavish D. Roxatidine acetate. A review of its pharmacodynamic and pharmacokinetic properties, and its therapeutic potential in peptic ulcer disease and related disorders. Drugs. 1991 Aug;42(2):240-60.

[3]Scholtholt J, Bickel M, Herling AW. A review of the animal pharmacology of roxatidine acetate. Drugs. 1988;35 Suppl 3:30-40

[4]Dammann HG, de Looze SM, Bender W, Labs R. Clinical characteristics of roxatidine acetate: a review. Scand J Gastroenterol Suppl. 1988;146:121-34

[5]Merki HS, Bender W, Labs R. Safety and efficacy of roxatidine acetate. Evidence from pharmacodynamic and clinical trials. J Clin Gastroenterol. 1989;11 Suppl 1:S20-3; discussion S24