Histamine H2 receptor antagonist-1

Antiulcer Agent 3 is a orally active histamine H₂-receptor competitive antagonist (pA₂ = 6.7). Antiulcer Agent 3 reduces gastric acid secretion. Antiulcer Agent 3 reduces gastric lesions in water-immersion stress-induced ulcer rat models. Antiulcer Agent 3 protects against HCl-ethanol-induced gastric lesions in rats. Antiulcer Agent 3 can be used for the research of peptic ulcer disease^[1]. In Vitro: Antiulcer Agent 3 (compound 8) acts as a competitive histamine H₂ receptor antagonist in isolated guinea pig right atria, with a pA₂ value of 6.7^[1]. In Vivo: Antiulcer Agent 3 (Compound 8) (30 mg/kg; intradermal injection; single administration) inhibits gastric acid secretion in conscious rats with gastric fistula. At the dose of 30 mg/kg, its inhibition rate reaches 79.5%, with an ED₅₀ of 12.9 mg/kg^[1].
Antiulcer Agent 3 (administered orally; single dose; 5 minutes before stress) inhibits water-immersion stress-induced gastric ulcers in rats, with an oral ED₅₀ of 13.3 mg/kg^[1].
Antiulcer Agent 3 (oral administration; single dose) exhibits cytoprotective activity against hydrochloric acid-ethanol-induced gastric ulcers in rats, with an oral ED₅₀ of 43.7 mg/kg^[1].
Antiulcer Agent 3 (0.25-1.0 mg/kg; intravenous injection; single administration) inhibits Histamine (HY-B1204)-induced gastric acid secretion in conscious dogs with Heidenhain pouches, and exhibits significant long-acting activity at the dose of 1.0 mg/kg, with an ED₅₀ of 0.38 mg/kg^[1].