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CAS号:93793-83-0
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英文名称:Roxatidine acetate hydrochloride, a specific and competitive histamin H2 receptor antagonist
分子式
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EINECS号
MDL
Smiles
InChIKey
乙二醇化学百科
基本信息
物化性质
安全信息
生产及用途
盐酸罗沙替丁醋酸酯在机体内通过醋解作用脱乙酰基转化为代谢物罗沙替丁。盐酸罗沙替丁醋酸酯和罗沙替丁都具有药效活性,可以有效抑制动物的基础胃酸分泌和刺激引起的胃酸分泌。Roxatidine Acetate HCl是特异性的,竞争性的组胺H2受体拮抗剂,IC50为3.2 μM,抑制胃酸分泌和溃疡形成。
Roxatidine Acetate Hydrochloride (6.25 μM, 12.5 μM, and 25 μM; pre-treatment for 30 min) suppresses the PMACI-induced activation of p38 MAPK, but does not affect the phosphorylation of ERK or JNK. The total ERK 1/2, JNK, and p38 MAPK levels are unaffected by roxatidine in human mast-cells-1 (HMC-1) cells.
Roxatidine Acetate Hydrochloride (oral gavage; 20 mg/kg; single dose) inhibits Compound 48/80-increased TNF-α, IL-6, and IL-1β production and mRNA expression. Additionally, Roxatidine decreases the compound 48/80-induced degradation of procaspase-1 and appearance of the corresponding cleaved bands in mice.
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