93793-83-0
中文名稱
鹽酸羅沙替丁醋酸酯
英文名稱
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
2024/12/30 11:14:25
93793-83-0 結(jié)構(gòu)式
基本信息
中文別名
羅沙鹽酸醋酸羅沙替丁
醋酸羅沙替丁鹽酸
鹽酸羅沙替丁鹽酸鹽
鹽酸羅沙替丁醋酸酯
鹽酸羅沙替丁醋酸脂
羅沙替丁醋酸氫氯化物
羅沙替丁醋酸酯鹽酸鹽
鹽酸羅沙替丁醋酸酯鹽酸鹽
羅沙替丁雜質(zhì)2(鹽酸醋酸羅沙替丁)
英文別名
AltatRoxit
Xarcin
Neo H2
tzu0460
tzu-0460
93793-83-0
PIFEATIDINE
Roxatidine acetate h
ROXATIDINE ACETATE HCL
所屬類別
生物化工：Histamine Receptor 拮抗劑物理化學(xué)性質(zhì)
熔點145-146°
儲存條件Inert atmosphere,2-8°C
溶解度DMSO: 78 mg/ml; Ethanol: 12 mg/ml; Water: 77 mg/ml
形態(tài)粉末晶體
顏色白色到近乎白色
Merck14,8274
常見問題列表
概述
鹽酸羅沙替丁醋酸酯在機體內(nèi)通過醋解作用脫乙?；D(zhuǎn)化為代謝物羅沙替丁。鹽酸羅沙替丁醋酸酯和羅沙替丁都具有藥效活性，可以有效抑制動物的基礎(chǔ)胃酸分泌和刺激引起的胃酸分泌。生物活性
Roxatidine Acetate HCl是特異性的，競爭性的組胺H2受體拮抗劑，IC50為3.2 μM，抑制胃酸分泌和潰瘍形成。靶點
| Target | Value |
| Histamine H2 receptor | 3.2 μM |
體外研究
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.
體內(nèi)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. |