Thioperamide is a highly potent and selective ligand for histamine H3-receptors.
ChEBI: Thioperamide is a primary aliphatic amine.
Potent histamine H 3 and H 4 antagonist/inverse agonist. K i values are 25 and 27 nM for human recombinant H 3 and H 4 receptors respectively. Blocks eosinophil shape change (IC 50 = 1.4 μ M) and chemotaxis (IC 50 = 519 nM) induced by histamine. Freely crosses the blood-brain barrier. Also available as part of the Histamine H 3 Receptor Tocriset™ .
