34970-69-9

Burimamide is a blocker of histamine H2-receptor. Burimamide inhibits gastric acid secretion evoked by Pentagastrin (HY-A0261) or Gastrin. Burimamide also has alpha-adrenoceptor blocking activity. Burimamide in combination with the H1-receptor antagonist Mepyramine (HY-B1281) shows anti-inflammatory activity in a rat paw edema model induced by Compound 48/80 (HY-115768)[1][2].

ChEBI: Burimamide is a member of imidazoles.

Histamine H 3 /H 2 receptor antagonist (K i values are 0.07, 7.8 and 290 μ M for H 3 , H 2 and H 1 receptors respectively). Displays partial agonist activity in SK-N-MC cells. Produces antinociceptive effects following intraventricular administration (ED 50 = 183 nmol/mouse in hot-plate test).

[1] Brimblecombe RW, et al. The pharmacology of burimamide and metiamide, two histamine H2-receptor antagonists. Fed Proc. 1976 Jun;35(8):1931-4. PMID:5313
[2] Gupta SC, et al. Azadirone, a limonoid tetranortriterpene, induces death receptors and sensitizes human cancer cells to tumor necrosis factor-related apoptosis-inducing ligand (TRAIL) through a p53 protein-independent mechanism: evidence for the role of the ROS-ERK-CHOP-death receptor pathway. J Biol Chem. 2013 Nov 8;288(45):32343-32356. DOI:10.1074/jbc.M113.455188