Roxatidine acetate

Roxatidine acetate is a potent, selective, competitive and orally active histamine _H2-receptor antagonist. Roxatidine acetate has antisecretory potency against gastric acid secretion. Roxatidine acetate can also suppress inflammatory responses and can be used for gastric and duodenal ulcers research. Roxatidine acetate has antitumor activity^[1][2][3]. In Vitro: Roxatidine acetate (0-120 μM, 1 h) suppresses inflammatory responses via inhibition of NF-κB and p38 MAPK activation in LPS-induced RAW 264.7 macrophages^[2].
Roxatidine acetate (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^[4]. In Vivo: Roxatidine acetate (0-300 mg/kg; p.o.; 26 days) suppressed growth of Colon 38 tumor implants in mice^[3].
Roxatidine acetate (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^[4].