International Union of Basic and Clinical Pharmacology. XCVIII. Histamine Receptors

Panula, Pertti; Chazot, Paul L.; Cowart, Marlon; Gutzmer, Ralf; Leurs, Rob; Liu, Wai L. S.; Stark, Holger; Thurmond, Robin L.; Haas, Helmut L.

doi:10.1124/pr.114.010249

Cited by 490 publications

(655 citation statements)

References 641 publications

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“…The coupling of H 2 R to Gs proteins was demonstrated by agonist-induced photoaffinity-labeling studies with GPCR-Gas fusion proteins, guanosine 59-O-(3-[ 35 S]thio)triphosphate binding, as well as steady-state GTP hydrolysis (Leopoldt et al, 1997;Kelley et al, 2001;WenzelSeifert et al, 2001). H 2 R displayed lower affinity for histamine than the H 3 and H 4 subtypes and had high constitutive activity toward cAMP production (Panula et al, 2015).…”

Section: Introductionmentioning

confidence: 99%

“…To date, four different types of histamine receptors have been described: H 1 R, H 2 R, H 3 R, and H 4 R (Panula et al, 2015).…”

Section: Introductionmentioning

confidence: 99%

“…The pharmacology of histamine receptors was comprehensively reviewed in numerous excellent articles published recently (Panula et al, 2015;Haas and Panula, 2016). However, based on the enormous costs for developing new drugs, this review aims to discuss the different aspects of histamine receptor function that have been characterized more recently and can be considered for repositioning histaminergic ligands for new therapeutic uses or for optimizing the usage of these existing ligands (Nosengo, 2016).…”

Section: Introductionmentioning

confidence: 99%

“…In most tissues where H 2 R is expressed, H 2 R couples to Gs protein and its activation stimulates AC-mediated cAMP production (Alewijnse et al, 1998;Monczor et al, 2003;Panula et al, 2015). The coupling of H 2 R to Gs proteins was demonstrated by agonist-induced photoaffinity-labeling studies with GPCR-Gas fusion proteins, guanosine 59-O-(3-[ 35 S]thio)triphosphate binding, as well as steady-state GTP hydrolysis (Leopoldt et al, 1997;Kelley et al, 2001;WenzelSeifert et al, 2001).…”

Section: Introductionmentioning

confidence: 99%

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Current Knowledge and Perspectives on Histamine H₁and H₂Receptor Pharmacology: Functional Selectivity, Receptor Crosstalk, and Repositioning of Classic Histaminergic Ligands

Monczor

Fernández

2016

Mol Pharmacol

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H 1 and H 2 histamine receptor antagonists, although developed many decades ago, are still effective for the treatment of allergic and gastric acid-related conditions. This article focuses on novel aspects of the pharmacology and molecular mechanisms of histamine receptors that should be contemplated for optimizing current therapies, repositioning histaminergic ligands for new therapeutic uses, or even including agonists of the histaminergic system in the treatment of different pathologies such as leukemia or neurodegenerative disorders. In recent years, new signaling phenomena related to H 1 and H 2 receptors have been described that make them suitable for novel therapeutic approaches. Crosstalk between histamine receptors and other membrane or nuclear receptors can be envisaged as a way to modulate other signaling pathways and to potentiate the efficacy of drugs acting on different receptors. Likewise, biased signaling at histamine receptors seems to be a pharmacological feature that can be exploited to investigate nontraditional therapeutic uses for H 1 and H 2 biased agonists in malignancies such as acute myeloid leukemia and to avoid undesired side effects when used in standard treatments. It is hoped that the molecular mechanisms discussed in this review contribute to a better understanding of the different aspects involved in histamine receptor pharmacology, which in turn will contribute to increased drug efficacy, avoidance of adverse effects, or repositioning of histaminergic ligands.

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Section: Introductionmentioning

confidence: 99%

“…To date, four different types of histamine receptors have been described: H 1 R, H 2 R, H 3 R, and H 4 R (Panula et al, 2015).…”

Section: Introductionmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

See 2 more Smart Citations

Current Knowledge and Perspectives on Histamine H₁and H₂Receptor Pharmacology: Functional Selectivity, Receptor Crosstalk, and Repositioning of Classic Histaminergic Ligands

Monczor

Fernández

2016

Mol Pharmacol

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“…Histamine is a pleiotropic mediator which exerts its biological effects through the activation of four different G-protein-coupled receptor subtypes (H 1 -4 R) [14]. The H 1 R is involved in allergic and immune responses, the H 2 R regulates gastric acid secretion, the H 3 R, a presynaptic receptor mainly present in the Central Nervous System, controls neurotransmitter release [15], and the H 4 R, expressed in hematopoietic cells, activates mast cells, eosinophil and neutrophil migration [16,17]. Moreover, Kohyama and coworkers [18] demonstrated that the H 4 R mediates in vitro the profibrotic effects of histamine on human foetal lung fibroblasts.…”

Section: Introductionmentioning

confidence: 99%

Role of histamine H 4 receptor ligands in bleomycin-induced pulmonary fibrosis

Lucarini

Pini

Rosa

et al. 2016

Pharmacological Research

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Use policyThe full-text may be used and/or reproduced, and given to third parties in any format or medium, without prior permission or charge, for personal research or study, educational, or not-for-prot purposes provided that:• a full bibliographic reference is made to the original source • a link is made to the metadata record in DRO • the full-text is not changed in any way The full-text must not be sold in any format or medium without the formal permission of the copyright holders.Please consult the full DRO policy for further details. This is a PDF file of an unedited manuscript that has been accepted for publication. As a service to our customers we are providing this early version of the manuscript. The manuscript will undergo copyediting, typesetting, and review of the resulting proof before it is published in its final form. Please note that during the production process errors may be discovered which could affect the content, and all legal disclaimers that apply to the journal pertain. The results here reported clearly demonstrated that H 4 R ligands have a beneficial effect in a model of lung fibrosis in the mouse, thus indicating that H 4 R antagonists or inverse agonists could be a novel therapeutic strategy for lung inflammatory diseases.4

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Histamine and Histamine Receptor Ligands

Ghamari

Stark

Hamzeh‐Mivehroud

2023

Kirk-Othmer Encyclopedia of Chemical Technology

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Histamine belongs to the group of biogenic amines and exerts its biological properties mainly mediated by four different G‐protein‐coupled receptor class A subtypes, named H 1 –H 4 receptors. While selective agonists are mainly used for pharmacological experiments, antagonists are widely used in different therapeutic fields. Different generations of H 1 receptor antagonists are mainly used for the treatment of allergic diseases and sleep disturbances, whereas H 2 receptor antagonists became blockbuster drugs in the treatment of stomach ulcers. With the detection of the H 3 receptor, the neurotransmitter properties of histamine have been proven. Despite several approaches, so far only one H 3 receptor antagonist (Pitolisant) got market approval for the orphan disease narcolepsy and for obstructive sleep apnea. The immunomodulatory and anti‐inflammatory properties of H 4 receptor antagonists have raised hopes for new therapeutic approaches in the near future.

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International Union of Basic and Clinical Pharmacology. XCVIII. Histamine Receptors

Cited by 490 publications

References 641 publications

Current Knowledge and Perspectives on Histamine H₁and H₂Receptor Pharmacology: Functional Selectivity, Receptor Crosstalk, and Repositioning of Classic Histaminergic Ligands

Current Knowledge and Perspectives on Histamine H₁and H₂Receptor Pharmacology: Functional Selectivity, Receptor Crosstalk, and Repositioning of Classic Histaminergic Ligands

Role of histamine H 4 receptor ligands in bleomycin-induced pulmonary fibrosis

Histamine and Histamine Receptor Ligands

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International Union of Basic and Clinical Pharmacology. XCVIII. Histamine Receptors

Cited by 490 publications

References 641 publications

Current Knowledge and Perspectives on Histamine H1and H2Receptor Pharmacology: Functional Selectivity, Receptor Crosstalk, and Repositioning of Classic Histaminergic Ligands

Current Knowledge and Perspectives on Histamine H1and H2Receptor Pharmacology: Functional Selectivity, Receptor Crosstalk, and Repositioning of Classic Histaminergic Ligands

Role of histamine H 4 receptor ligands in bleomycin-induced pulmonary fibrosis

Histamine and Histamine Receptor Ligands

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Product

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Current Knowledge and Perspectives on Histamine H₁and H₂Receptor Pharmacology: Functional Selectivity, Receptor Crosstalk, and Repositioning of Classic Histaminergic Ligands

Current Knowledge and Perspectives on Histamine H₁and H₂Receptor Pharmacology: Functional Selectivity, Receptor Crosstalk, and Repositioning of Classic Histaminergic Ligands