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

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Abstract

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].

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Leurs, R., Vollinga, R.C., Timmerman, H. (1995). The medicinal chemistry and therapeutic potentials of ligands of the histamine H3 receptor. In: Jucker, E. (eds) Progress in Drug Research / Fortschritte der Arzneimittelforschung / Progrès des Recherches Pharmaceutiques. Progress in Drug Research / Fortschritte der Arzneimittelforschung / Progrès des recherches pharmaceutiques, vol 45. Birkhäuser Basel. https://doi.org/10.1007/978-3-0348-7164-8_4

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