Current Knowledge and Perspectives on Histamine H1 and H2 Receptor Pharmacology: Functional Selectivity, Receptor Crosstalk, and Repositioning of Classic Histaminergic Ligands

作者: Federico Monczor , Natalia Fernandez

DOI: 10.1124/MOL.116.105981

关键词: HistaminergicHistamineHistamine H2 receptorHistamine receptorBiologyFunctional selectivityPharmacologyReceptorReceptor Cross-TalkSignal transduction

摘要: H1 and H2 histamine receptor antagonists, although developed many decades ago, are still effective for the treatment of allergic gastric acid-related conditions. This article focuses on novel aspects pharmacology molecular mechanisms receptors that should be contemplated optimizing current therapies, repositioning histaminergic ligands new therapeutic uses, or even including agonists system in different pathologies such as leukemia neurodegenerative disorders. In recent years, signaling phenomena related to have been described make them suitable approaches. Crosstalk between other membrane nuclear can envisaged a way modulate pathways potentiate efficacy drugs acting receptors. Likewise, biased at seems pharmacological feature exploited investigate nontraditional uses malignancies acute myeloid avoid undesired side effects when used standard treatments. It is hoped discussed this review contribute better understanding involved pharmacology, which turn will increased drug efficacy, avoidance adverse effects, ligands.

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