H. Stark, J. Arrang, X. Ligneau
2001
Citations
0
Influential Citations
48
Citations
Journal
Progress in medicinal chemistry
Abstract
Publisher Summary This chapter explores that the detection of the histamine H3 receptor was first performed with burimamide, an H2/H3-receptor antagonist formerly used for the first differentiation between histamine H1 and H2 receptors. The existence of H3 receptors is proven with selective agonists and antagonists using classical pharmacological analysis. The recent cloning of human and rodent histamine H3 receptors and the identification of two splice variants has brought fresh impetus into research field. It reviews that many pharmacological auto and heteroreceptor functions have been demonstrated in characterizing the H3 receptor in the central nervous system and in peripheral tissues with a number of structurally different ligands. Unlike H1 and H2-receptor antagonists, however, which are widely used for the therapy of allergic and acid-related diseases, no selective ligands for H3 receptors so far, have been introduced for therapeutic use, although, some promising candidates have reached clinical phases and are currently under further development.