IMR Press / FBS / Volume 4 / Issue 2 / DOI: 10.2741/s279

Frontiers in Bioscience-Scholar (FBS) is published by IMR Press from Volume 13 Issue 1 (2021). Previous articles were published by another publisher on a subscription basis, and they are hosted by IMR Press on as a courtesy and upon agreement with Frontiers in Bioscience.


Histamine receptor subtypes: a century of rational drug design

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1 Johann Wolfgang Goethe University, Institute of Pharmaceutical Chemistry, Biocenter, ZAFES/LiFF/CMP/ICNF, Max-vonLaue-Str. 9, 60438 Frankfurt, Germany

*Author to whom correspondence should be addressed.

Academic Editor:Ekaterini Tiligada

Front. Biosci. (Schol Ed) 2012, 4(2), 461–488;
Published: 1 January 2012
(This article belongs to the Special Issue Histamine revisited: the H4 receptor in health and disease)

Histamine plays an important role as neurotransmitter and chemical mediator in multiple physiological and pathophysiological processes in central and peripheral tissues. In the last century the extensive study of its actions in the human body, resulted in the identification of four G protein-coupled receptor (GPCR) subtypes (H1R-H4R), mediating numerous effects. The successful application of H1R and H2R antagonists/inverse agonists in the treatment of allergic conditions and gastric ulcer proved that these two receptors are excellent drug targets. Ligands for H3R are currently in advanced stages of clinical development for a broad spectrum of mainly central diseases (e.g. narcolepsy, Alzheimer’s disease, epilepsy and schizophrenia). Meanwhile, preclinical research in the H4R field, focused on inflammatory and immunological processes, led to the evaluation of the first H4R-targeting clinical candidates. Drug development for each histamine receptor subtype will be discussed with a special focus on H3R and H4R ligands.

Drug Design
Medicinal Chemistry
Drug Development
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