93793-83-0
中文名称
盐酸罗沙替丁醋酸酯
英文名称
Roxatidine acetate hydrochloride
CAS
93793-83-0
分子式
C19H29ClN2O4
分子量
384.9
MOL 文件
93793-83-0.mol
更新日期
2024/04/22 18:17:52
93793-83-0 结构式
基本信息
中文别名
罗沙盐酸醋酸罗沙替丁
醋酸罗沙替丁盐酸
盐酸罗沙替丁盐酸盐
盐酸罗沙替丁醋酸酯
盐酸罗沙替丁醋酸脂
罗沙替丁醋酸氢氯化物
罗沙替丁醋酸酯盐酸盐
盐酸罗沙替丁醋酸酯盐酸盐
罗沙替丁杂质2(盐酸醋酸罗沙替丁)
英文别名
AltatRoxit
Xarcin
Neo H2
tzu0460
tzu-0460
93793-83-0
PIFEATIDINE
Roxatidine acetate h
ROXATIDINE ACETATE HCL
所属类别
生物化工：Histamine Receptor 拮抗剂物理化学性质
熔点145-146°
储存条件Inert atmosphere,2-8°C
溶解度DMSO: 78 mg/ml; Ethanol: 12 mg/ml; Water: 77 mg/ml
形态粉末晶体
颜色白色到近乎白色
Merck14,8274
常见问题列表
概述
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。生物活性
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。靶点
| Target | Value |
| Histamine H2 receptor | 3.2 μM |
体外研究
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.
体内研究
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.
| Animal Model: | ICR male mice (6 weeks old) |
| Dosage: | 20 mg/kg |
| Administration: | Oral gavage; 20 mg/kg; single dose |
| Result: | Suppressed compound 48/80-induced allergic inflammation in anaphylactic animal model. |