Cloning and pharmacological characterization of the dog histamine H4 receptor

Jiang, Wen; Lim, Herman D.; Desai, Pragnya J.; Dai, Heng; Colling, Patricia M.; Leurs, Rob; Thurmond, Robin L.

doi:10.1016/j.ejphar.2008.06.095

Cited by 35 publications

(64 citation statements)

References 21 publications

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“…Interestingly, although expression differences were observed among species [14,15,17,18,34], the similar tissue distribution in different mammals indicates conserved and comparable physiological roles of the H 4 receptor across species. Therefore, we could speculate similar roles in humans.…”

Section: Renal H 4 Receptor Expression In Diabetic Ratsmentioning

confidence: 99%

“…A very low level of H 4 receptor mRNA has been reported in the kidney of dog, monkey, rat, mouse, guinea pig and pig [14][15][16][17][18]. Despite the demonstration of an increasing histamine release in diabetic kidney, there is no evidence for the involvement of H 4 receptor expression in the diabetes-related kidney disease.…”

mentioning

confidence: 90%

“…Later, the constitutive, but very low H 4 receptor gene expression, was confirmed in different species [14][15][16][17][18]36];…”

Section: Renal H 4 Receptor Expression In Diabetic Ratsmentioning

confidence: 99%

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Overexpression of histamine H4 receptors in the kidney of diabetic rat

Rosa

Grange²,

Pini

et al. 2012

Inflamm. Res.

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Objective and design: The renal expression of H 1 and H 2 receptors was previously demonstrated, while that of the H 4 receptor has been poorly investigated, thus the aim of this research was to investigate the expression of the H 4 receptor in the kidney of diabetic rats.Material or subjects: 24 8-week-old male Wistar rats Treatment: Diabetes was induced in 12 rats by a single i.v. injection of streptozotocin, and animals were sacrificed 6 weeks later.Methods: Kidneys were collected and processed for quantitative PCR or immunohistochemical analyses. To ascertain the renal topology of the H 4 receptor, colocalization experiments were performed with a series of markers.Results: H 4 receptor is expressed in healthy rats, although at a very low level, and is profoundly upregulated in diabetic animals. Immunohistochemical analysis revealed the highest immune-positivity in the medulla. Colocalization experiments revealed a close overlap in expression topology of the H 4 receptor and both Tamm-Horsfall glycoprotein and aquaporin 1 was observed.Conclusions: The results demonstrate, for the first time, that the H 4 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.

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Section: Renal H 4 Receptor Expression In Diabetic Ratsmentioning

confidence: 99%

mentioning

confidence: 90%

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Overexpression of histamine H4 receptors in the kidney of diabetic rat

Rosa

Grange²,

Pini

et al. 2012

Inflamm. Res.

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“…Recently, a possible role for H 4 R has been suggested by our research group [14]. While a very low mRNA level of the latest discovered histamine receptor has been reported in the kidney of dog, monkey, rat, mouse, guinea pig and pig [15][16][17][18][19][20], in 2013 we demonstrated the presence of H 4 R in resident renal cells of the loop of Henlé!and its profound upregulation in the kidney of diabetic rats [14]. Notably, these data provide the first basis to hypothesize a possible involvement of H 4 R in the onset/progression of diabetes-associated renal disease.…”

Section: Introductionmentioning

confidence: 99%

Histamine receptor expression in human renal tubules: a comparative pharmacological evaluation

et al. 2015

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Objective and design The aim of this study is to evaluate the expression of the histamine receptors, particularly focusing on the H 4 R in human renal tubules. MaterialThe 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.Treatment Cells were pretreated for 10 min with chlorfeniramine maleate 10 µM (H 1 R antagonist), ranitidine 10 µM (H 2 R antagonist), GSK189254 1 µM (H 3 R antagonist) or JNJ7777120 10 µM (H 4 R antagonist), and then exposed to histamine (3 pM -10 nM) for 30 min. MethodsThe 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.Results 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 IP 3 production, shifted to the right by chlorpheniramine maleate, and elicited a double bell-shaped curve for cAMP production, partially suppressed by the selective H 2 R, H 3 R and H 4 R antagonists when each added alone, and completely ablated when combined together.Conclusions Herein, we report the identification of all four histamine receptors in human renal tubules.

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“…For several GPCRs, including the H 3 R, significant species differences are known and have seriously hampered drug discovery efforts (Oksenberg et al, 1992;Maconi et al, 2002;Reinhart et al, 2004;Hancock, 2006). Various species orthologs of H 4 R were promptly cloned based on their homology to the human H 4 R sequence (Oda et al, 2000), including those of mouse, rat, guinea pig, pig, monkey (Macaca fascilularis), and dog (Liu et al, 2001b;Oda et al, 2002Oda et al, , 2005Jiang et al, 2008). The H 4 R species variants show relatively low homology to the human H 4 R (65-71%), except for the monkey H 4 R, which shows an overall amino acid homology of 93% (Fig.…”

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confidence: 99%

Molecular Determinants of Ligand Binding to H₄R Species Variants

Lim¹,

Graaf²,

Jiang³

et al. 2010

Mol Pharmacol

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The histamine H 4 receptor (H 4 R) is the latest identified histamine receptor to emerge as a potential drug target for inflammatory diseases. Animal models are employed to validate this potential drug target. Concomitantly, various H 4 R orthologs have been cloned, including the human, mouse, rat, guinea pig, monkey, pig, and dog H 4 Rs. In this article, we expressed all these H 4 R orthologs in human embryonic kidney 293T cells and compared their interactions with currently used standard H 4 R ligands, including the H 4 R agonists histamine, 4-methylhistamine, guanidinylethyl isothiourea (VUF 8430), the H 4 R antagonists 1-[(5-chloro-1H-indol-2-yl)carbonyl]-4-methylpiperazine (JNJ 7777120) and [(5-chloro-1H-benzimidazol-2-yl)carbonyl]-4-methylpiperazine (VUF 6002), and the inverse H 4 R agonist thioperamide. Most of the evaluated ligands display significantly different affinities at the different H 4 R orthologs. These "natural mutants" of H 4 R were used to study ligand-receptor interactions by using chimeric human-pig-human and pig-human-pig H 4 R proteins and site-directed mutagenesis. Our results are a useful reference for ligand selection for studies in animal models of diseases and offer new insights in the understanding of H 4 R-ligand receptor interactions.

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Cloning and pharmacological characterization of the dog histamine H4 receptor

Cited by 35 publications

References 21 publications

Overexpression of histamine H4 receptors in the kidney of diabetic rat

Overexpression of histamine H4 receptors in the kidney of diabetic rat

Histamine receptor expression in human renal tubules: a comparative pharmacological evaluation

Molecular Determinants of Ligand Binding to H₄R Species Variants

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Cloning and pharmacological characterization of the dog histamine H4 receptor

Cited by 35 publications

References 21 publications

Overexpression of histamine H4 receptors in the kidney of diabetic rat

Overexpression of histamine H4 receptors in the kidney of diabetic rat

Histamine receptor expression in human renal tubules: a comparative pharmacological evaluation

Molecular Determinants of Ligand Binding to H4R Species Variants

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Molecular Determinants of Ligand Binding to H₄R Species Variants