Cimetidine-d3

Cimetidine-d3 is intended for use as an internal standard for the quantification of cimetidine by GC- or LC-MS. 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

|1. Smit, M.J., Leurs, R., Alewijnse, A.E., et al. 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. Lin, T.M., Evans, D.C., Warrick, M.W., et al. Actions of nizatidine, a selective histamine H2-receptor antagonist, on gastric acid secretion in dogs, rats and frogs. J. Pharmacol. Exp. Ther. 239(2), 406-410 (1986).|3. Natori, T., Sata, M., Nagai, R., et al. Cimetidine inhibits angiogenesis and suppresses tumor growth. Biomed. Pharmacother. 59(1-2), 56-60 (2005).