New Histamine Receptor Antagonists

Cat.No. Product Name Information
S4353 Terfenadine Terfenadine is an antihistamine, generally completely metabolizes to the active form fexofenadine in the liver by the enzyme cytochrome P450 CYP3A4 isoform. Terfenadine ((±)-Terfenadine) is a potent open-channel blocker of hERG with an IC50 of 204 nM. Terfenadine, an H1 histamine receptor antagonist, acts as a potent apoptosis inducer in melanoma cells through modulation of Ca2+ homeostasis. Terfenadine induces ROS-dependent apoptosis, simultaneously activates Caspase-4, -2, -9.
S4382 Pyrilamine Maleate Pyrilamine is a histamine H1 receptor inverse agonist, it binds to a G protein-coupled form of the receptor and promotes a G protein-coupled inactive state of the H1 receptor that interferes with the Gq/11-mediated signaling.
S6612 Betazole Dihydrochloride Betazole Dihydrochloride is a histamine H2 agonist used clinically to test gastric secretory function.
S6569 VUF10460 VUF10460 is a histamine H4 receptor agonist.
S6435 Mequitazine Mequitazine is a histamine H1 antagonist which competes with histamine for the normal H1-receptor sites on effector cells of the gastrointestinal tract, blood vessels and respiratory tract.
All Histamine Receptor Antagonists