Histamine H3 receptors: an overview

Abstract

Histamine H3 receptors represent a new class of prejunctional receptors, which, first described as modulators of histamine synthesis and release in the central nervous system, were subsequently found to occur also in peripheral tissues. They may behave both as autoreceptors located in histaminergic neurons and as heteroreceptors localized in adrenergic, cholinergic, serotoninergic and NANC nerve endings. As far as the gastrointestinal tract is concerned, H3 receptors seem to negatively control gastric acid secretion induced by endogenous cholinergic stimuli as well as gastrointestinal motility, as observed in different isolated preparations electrically stimulated. So far experimental evidence suggests that these receptors are absent in the effector organs. The most selective agonist and antagonist of H3 receptors are (R) alpha-methylhistamine and thioperamide, respectively; however, a lot of similar compounds are being synthesized in a few laboratories. It is easy to foresee that in the near future the availability of such substances will help the investigators in enlarging our knowledge in this interesting field.