New concepts of histamine receptors and actions

Repka-Ramirez, María Susana

doi:10.1007/s11882-003-0044-3

Cited by 49 publications

(26 citation statements)

References 37 publications

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“…The studies were conducted in: (i) normal rats treated with NaCl (vehicle) or RAMH (10 mg/kg body weight/day) 23,24 for 1 week; and (ii) BDL rats that, immediately after BDL, 27 were treated for 1 week with daily I.P. injections of NaCl, RAMH (10 mg/kg body weight/day), 28 thioperamide maleate (5 mg/kg body weight) 25,26 or histamine (0.5 mg/kg body weight) 15,29 in the absence or presence of thioperamide maleate for 1 week. The doses of RAMH, thioperamide maleate and histamine used in the present studies were similar to those used in other studies in rodents.…”

Section: Animal Modelmentioning

confidence: 99%

“…The doses of RAMH, thioperamide maleate and histamine used in the present studies were similar to those used in other studies in rodents. 15,25,26,28,29 Liver blocks, serum and cholangiocytes were obtained at the end of the selected treatments. We evaluated body and liver weight from the selected groups of animals.…”

Section: Animal Modelmentioning

confidence: 99%

“…14,15 Thus, we performed a series of experiments to pinpoint the role of the H3R in histamine modulation of cholangiocyte proliferative response to cholestasis. We observed that the in vivo administration of RAMH to BDL rats decreased cholangiocyte growth to a higher extent compared to histamine.…”

Section: Histamine Regulation Of Cholangiocyte Growthmentioning

confidence: 99%

“…[11][12][13] Four G-protein coupled histamine receptors (HRs) (H1R, H2R, H3R and H4R) exist. 14,15 Although H1R act via Ga q mobilizing [Ca 2 þ ] i, 16 the activation of H2R is modulated by Ga s proteins, coupled to adenylyl cyclase. 17 H3R were first noted as presynaptic autoreceptors on brain histamine neurons, although they were also found in other cells.…”

mentioning

confidence: 99%

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H3 histamine receptor agonist inhibits biliary growth of BDL rats by downregulation of the cAMP-dependent PKA/ERK1/2/ELK-1 pathway

Francis

Franchitto

Ueno

et al. 2007

Laboratory Investigation

152

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Histamine regulates many functions by binding to four histamine G-coupled receptor proteins (H1R, H2R, H3R and H4R). As H3R exerts their effects by coupling to Ga i/o proteins reducing adenosine 3 0 , 5 0 -monophosphate (cAMP) levels (a key player in the modulation of cholangiocyte hyperplasia/damage), we evaluated the role of H3R in the regulation of biliary growth. We posed the following questions: (1) Do cholangiocytes express H3R? (2) Does in vivo administration of (R)-(a)-(À)-methylhistamine dihydrobromide (RAMH) (H3R agonist), thioperamide maleate (H3R antagonist) or histamine, in the absence/presence of thioperamide maleate, to bile duct ligated (BDL) rats regulate cholangiocyte proliferation? and (3) Does RAMH inhibit cholangiocyte proliferation by downregulation of cAMP-dependent phosphorylation of protein kinase A (PKA)/extracellular signal-regulated kinase 1/2 (ERK1/2)/ets-like gene-1 (Elk-1)? The expression of H3R was evaluated in liver sections by immunohistochemistry and immunofluorescence, and by real-time PCR in cholangiocyte RNA from normal and BDL rats. BDL rats (immediately after BDL) were treated daily with RAMH, thioperamide maleate or histamine in the absence/presence of thioperamide maleate for 1 week. Following in vivo treatment of BDL rats with RAMH for 1 week, and in vitro stimulation of BDL cholangiocytes with RAMH, we evaluated cholangiocyte proliferation, cAMP levels and PKA, ERK1/2 and Elk-1 phosphorylation. Cholangiocytes from normal and BDL rats express H3R. The expression of H3R mRNA increased in BDL compared to normal cholangiocytes. Histamine decreased cholangiocyte growth of BDL rats to a lower extent than that observed in BDL RAMH-treated rats; histamine-induced inhibition of cholangiocyte growth was partly blocked by thioperamide maleate. In BDL rats treated with thioperamide maleate, cholangiocyte hyperplasia was slightly higher than that of BDL rats. In vitro, RAMH inhibited the proliferation of BDL cholangiocytes. RAMH inhibition of cholangiocyte growth was associated with decreased cAMP levels and PKA/ERK1/2/Elk-1 phosphorylation. Downregulation of cAMP-dependent PKA/ERK1/2/Elk-1 phosphorylation (by activation of H3R) is important in the inhibition of cholangiocyte growth in liver diseases.

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Section: Animal Modelmentioning

confidence: 99%

Section: Animal Modelmentioning

confidence: 99%

Section: Histamine Regulation Of Cholangiocyte Growthmentioning

confidence: 99%

mentioning

confidence: 99%

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H3 histamine receptor agonist inhibits biliary growth of BDL rats by downregulation of the cAMP-dependent PKA/ERK1/2/ELK-1 pathway

Francis

Franchitto

Ueno

et al. 2007

Laboratory Investigation

152

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“…As a proinflammatory mediator, histamine is selectively located in the granules of human mast cells and basophils and released from these cells upon degranulation. To date, a total of four histamine receptors H 1 , H 2 , H 3 and H 4 have been discovered [98] and the first three of them have been located in human gut [99,100] , proving that there are some specific targets on which histamine can work in intestinal tract. Histamine was found to cause a transient concentration-dependent increase in short-circuit current, a measure of total ion transport across the epithelial tissue in gut [101] .…”

Section: Involvement Of Histamine In Pathogenesis Of Ibdmentioning

confidence: 99%

Key role of mast cells and their major secretory products in inflammatory bowel disease

He¹

2004

WJG

225

173

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Historically, mast cells were known as a key cell type involved in type I hypersensitivity. Until last two decades, this cell type was recognized to be widely involved in a number of non-allergic diseases including inflammatory bowel disease (IBD). Markedly increased numbers of mast cells were observed in the mucosa of the ileum and colon of patients with IBD, which was accompanied by great changes of the content in mast cells such as dramatically increased expression of TNFα, IL-16 and substance P. The evidence of mast cell degranulation was found in the wall of intestine from patients with IBD with immunohistochemistry technique. The highly elevated histamine and tryptase levels were detected in mucosa of patients with IBD, strongly suggesting that mast cell degranulation is involved in the pathogenesis of IBD. However, little is known of the actions of histamine, tryptase, chymase and carboxypeptidase in IBD. Over the last decade, heparin has been used to treat IBD in clinical practice. The low molecular weight heparin (LMWH) was effective as adjuvant therapy, and the patients showed good clinical and laboratory response with no serious adverse effects. The roles of PGD2, LTC4, PAF and mast cell cytokines in IBD were also discussed. Recently, a series of experiments with dispersed colon mast cells suggested there should be at least two pathways in man for mast cells to amplify their own activationdegranulation signals in an autocrine or paracrine manner. The hypothesis is that mast cell secretogogues induce mast cell degranulation, release histamine, then stimulate the adjacent mast cells or positively feedback to further stimulate its host mast cells through H 1 receptor. Whereas released tryptase acts similarly to histamine, but activates mast cells through its receptor PAR-2. The connections between current anti-IBD therapies or potential therapies for IBD with mast cells were discussed, implicating further that mast cell is a key cell type that is involved in the pathogenesis of IBD. In conclusion, while pathogenesis of IBD remains unclear, the key role of mast cells in this group of diseases demonstrated in the current review implicates strongly that IBD is a mast cell associated disease. Therefore, close attentions should be paid to the role of mast cells in IBD.He SH. Key role of mast cells and their major secretory products in inflammatory bowel disease.

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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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New concepts of histamine receptors and actions

Cited by 49 publications

References 37 publications

H3 histamine receptor agonist inhibits biliary growth of BDL rats by downregulation of the cAMP-dependent PKA/ERK1/2/ELK-1 pathway

H3 histamine receptor agonist inhibits biliary growth of BDL rats by downregulation of the cAMP-dependent PKA/ERK1/2/ELK-1 pathway

Key role of mast cells and their major secretory products in inflammatory bowel disease

Histamine and Histamine Receptor Ligands

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