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Pl Chazot

Bio: Pl Chazot is an academic researcher from Durham University. The author has contributed to research in topics: Histamine H1 receptor & Histamine. The author has an hindex of 1, co-authored 1 publications receiving 20 citations.

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Journal ArticleDOI
TL;DR: It is demonstrated, for the first time, that the H4 receptor is expressed in the kidney mainly by resident renal cells of the loop of Henlé and that this receptor is significantly overexpressed in diabetic animals, thus suggesting a possible role in the pathogenesis of diabetes-associated renal disease.
Abstract: Objective and design The renal expression of H1 and H2 receptors has previously been demonstrated, while that of the H4 receptor has been poorly investigated, and thus the aim of this research was to investigate the expression of the H4 receptor in the kidney of diabetic rats.

22 citations


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Journal ArticleDOI
TL;DR: The H3R is an autoreceptor and heteroreceptor providing negative feedback on histaminergic and inhibition on other neurons, a block of these actions promotes waking and the development of anti-inflammatory drugs is anticipated.
Abstract: Histamine is a developmentally highly conserved autacoid found in most vertebrate tissues. Its physiological functions are mediated by four 7-transmembrane G protein–coupled receptors (H1R, H2R, H3R, H4R) that are all targets of pharmacological intervention. The receptors display molecular heterogeneity and constitutive activity. H1R antagonists are long known antiallergic and sedating drugs, whereas the H2R was identified in the 1970s and led to the development of H2R-antagonists that revolutionized stomach ulcer treatment. The crystal structure of ligand-bound H1R has rendered it possible to design new ligands with novel properties. The H3R is an autoreceptor and heteroreceptor providing negative feedback on histaminergic and inhibition on other neurons. A block of these actions promotes waking. The H4R occurs on immuncompetent cells and the development of anti-inflammatory drugs is anticipated.

411 citations

Journal ArticleDOI
TL;DR: An interesting upsurge in the field which provides scope for new insights into the role of histamine in diabetes is revealed.

21 citations

Journal ArticleDOI
24 Apr 2020-Life
TL;DR: The histamine H4 receptor, belonging to the family of G-protein coupled receptors, is an increasingly attractive drug target, and numerous H4R ligands are being studied for the treatment of several inflammatory, allergic, and autoimmune disorders.
Abstract: The histamine H4 receptor, belonging to the family of G-protein coupled receptors, is an increasingly attractive drug target. It plays an indispensable role in many cellular pathways, and numerous H4R ligands are being studied for the treatment of several inflammatory, allergic, and autoimmune disorders, including pulmonary fibrosis. Activation of H4R is involved in cytokine production and mediates mast cell activation and eosinophil chemotaxis. The importance of this receptor has also been shown in inflammatory models: peritonitis, respiratory tract inflammation, colitis, osteoarthritis, and rheumatoid arthritis. Recent studies suggest that H4R acts as a modulator in cancer, neuropathic pain, vestibular disorders, and type-2 diabetes, however, its role is still not fully understood.

17 citations

Journal ArticleDOI
TL;DR: All four histamine receptors in human renal tubules are identified, particularly the H4R, which was partially suppressed by the selective H2R, H3R and H 4R antagonists when each added alone, and completely ablated when combined together.
Abstract: The aim of this study is to evaluate the expression of the histamine receptors, particularly focusing on the H4R in human renal tubules. The ex vivo evaluation was carried on specimens from human renal cortex. Primary and immortalized tubular epithelial cells (TECs) and the HK-2 cell line were used as in vitro models. Cells were pretreated for 10 min with chlorpheniramine maleate 10 μM (H1R antagonist), ranitidine 10 µM (H2R antagonist), GSK189254 1 µM (H3R antagonist) or JNJ7777120 10 µM (H4R antagonist), and then exposed to histamine (3 pM–10 nM) for 30 min. The ex vivo evaluation on specimens from human renal cortex was performed by immunohistochemistry. The expression of histamine receptors on primary and immortalized TECs and the HK-2 cell line was evaluated at both gene (RT-PCR) and protein (immunocytofluorescence) levels. The pharmacological analysis was performed by TR-FRET measurements of second messenger (IP3 and cAMP) production induced by histamine with or without the selective antagonists. Our data revealed the presence of all histamine receptors in human tubules; however, only TECs expressed all the receptors. Indeed, histamine elicited a sigmoid dose–response curve for IP3 production, shifted to the right by chlorpheniramine maleate, and elicited a double bell-shaped curve for cAMP production, partially suppressed by the selective H2R, H3R and H4R antagonists when each added alone, and completely ablated when combined together. Herein, we report the identification of all four histamine receptors in human renal tubules.

17 citations

Journal ArticleDOI
TL;DR: The data suggest that the H4R participates in diabetic nephropathy progression through both a direct effect on tubular reabsorption and an indirect action on renal tissue architecture via inflammatory cell recruitment, and H 4R antagonism emerges as a possible new multi‐mechanism therapeutic approach to counteract development of diabetic neephropathy development.

16 citations