Histamine H3 receptors: Potential novel target for analgesia

The central histaminergic system has gained increasing significance over the last decade, with the topographical definition of histaminergic neuronal pathways and the identification of four histamine receptor subtypes in the human central nervous system. The focus of this review lies in the H3 receptor (H3R) subtype which has grown in importance as a therapeutic target in a wide array of clinical indications, the most intensely studied being analgesia. The recent development of selective probes and availability of knockout mice has permitted the initial dissection of the anatomical basis for H3R mediated analgesia. The initial clinical data with a H3R agonist prodrug BP 29-4 and the potential use of targeting the H3R for gastroinflammatory disease and migraine is discussed.