59 products were found matching "K04150"!

Histamine is a ubiquitous messenger molecule released from mast cells, enterochromaffin-like cells, and neurons. Its various actions are mediated by histamine receptors H1, H2, H3, and H4. Specifically, the histamine receptor H2 belongs to the rhodopsin-like family of G protein-coupled receptors. As an integral...

Cimetidine is a histamine H2 receptor antagonist (Ki = 0.6 µM). 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). In vivo, it...

Ranitidine is a histamine H2 receptor antagonist. It reverses histamine-induced relaxation of isolated rat uterine horn (pA2 = 6.9) as well as histamine-induced increases in contraction frequency in isolated guinea pig right atrium (pA2 = 7.2). Ranitidine (0.03-3 mg/kg, i.v.) inhibits histamine-and...

Histamine is a biogenic amine. It is produced from histidine in basophils, mast cells, gastric enterochromaffin-like (ECL) cells, and histaminergic neurons by histidine decarboxylase (HDC). Histamine activates the G protein-coupled histamine H1-4 receptors to regulate allergic and inflammatory responses, gastric...

Roxatidine acetate is a competitive histamine H2 receptor antagonist that upon oral absorption is rapidly converted to its active metabolite roxatidine. By inhibiting the binding of histamine to H2 receptors, roxatidine reduces both intracellular cAMP concentrations and gastric acid secretion by parietal...

Famotidine is a histamine H2 receptor antagonist with a Ki value of 12 nM in fractionated guinea pig cerebral cortex membranes. It is selective for H2 over H1 and muscarinic receptors (Kis = 4 and 28 µM, respectively, in bovine cerebral cortex). Famotidine inhibits histamine-induced acid secretion in isolated canine...

Dimaprit is a histamine H2 receptor agonist with a Ki value of 44 µM in guinea pig right atrium. It is selective for histamine H2 over H1 and H3 receptors with relative potencies of 71, A. suum extract, which is not affected by pretreatment with mepyramine (Cay-20978), an H1 receptor inverse agonist, or cimetidine...

Roxatidine is a histamine H2 receptor antagonist and major active metabolite of roxatidine acetate (Cay-21248). Roxatidine reduces histamine-induced adenylate cyclase production in guinea pig parietal cells (IC50 = 0.8 µM). It inhibits histamine-induced hydrogen ion accumulation in the same cells (pA2 = 7.03)....

Protein function: The H2 subclass of histamine receptors mediates gastric acid secretion. Also appears to regulate gastrointestinal motility and intestinal secretion. Possible role in regulating cell growth and differentiation. The activity of this receptor is mediated by G proteins which activate adenylyl cyclase...

A H2-receptor antagonist, found to be a potent inhibitor of gastric acid secretion.

Histamine H2 receptors mediate gastric acid secretion by coupling to Galphas proteins and increasing cAMP formation. Nizatidine is a histamine H2 receptor antagonist that decreases gastric acid secretion (ED50 = 0.9 µM in isolated gastric mucosa of bullfrog and ED50s = 1.383 and 0.08 µmol/kg in rats and dogs,...

A histamine H2-receptor antagonist used in ulcer treatment. It is found to inhibit platelet function in vitro.