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The medicinal chemistry and therapeutic potentials of ligands of the histamine H3 receptor

1995; Linguagem: Inglês

10.1007/978-3-0348-7164-8_4

Rob Leurs, Roeland C. Vollinga, H. Timmerman,

Polyamine Metabolism and Applications

The monoamine histamine is one of the several chemical messengers involved in the concerted regulation of (patho)physiological processes. In rat brain, histamine can be found in a restricted population of neurons originating from the tuberomammillary nucleus of the hypothalamus [1, 2]. These histaminergic neurons project diffusely to several brain areas and are involved in the regulation of physiological functions (e.g. sleep/wakefullness, feeding, cardiovascular control, neuroendocrine control) [1, 2]. In the periphery histamine is mainly found in mast cells, basophils and enterochrommafin cells. Mast cell degranulation after IgG-allergen interactions results in a massive release of histamine, which is responsible for many of the well-known symptoms of allergic conditions [3, 4]. In gastric mucosa histamine is especially stored in enterochromaffin cells, from which it can be release upon stimulation with gastrin or acetylcholine [5]. In turn, histamine stimulates the parietal cell, resulting in gastric acid secretion [5].