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Cimetidine is a histamine H2 receptor antagonist (Ki = 0.6 μM).1 It also acts as an inverse agonist, inhibiting basal cAMP production in CHO cells expressing recombinant H2 receptors (IC50 = 1.2 μM). Cimetidine inhibits histamine-induced acid secretion from isolated bullfrog gastric mucosa (IC50 = 16 μM).2 In vivo, it inhibits histamine-induced gastric acid secretion in gastric fistulae and Heidenhain pouches in dogs (ED50 = 1.88 μmol/kg, p.o.). Cimetidine (20 mg/kg per day) also reduces tumor growth and neovascularization in a CMT93 colon cancer mouse syngeneic model.3
WARNING This product is not for human or veterinary use.
1. Inverse agonism of histamine H2 antagonist accounts for upregulation of spontaneously active histamine H2 receptors. Proc. Natl. Acad. Sci. USA 93(13), 6802-6807 (1996).
2. Actions of nizatidine, a selective histamine H2-
3. Cimetidine inhibits angiogenesis and suppresses tumor growth. Biomed. Pharmacother. 59(1-2), 56-60 (2005).