The influence of H1-, H2- and H3-receptors on the spontaneous and ConA induced histamine release from human adenoidal mast cells

Bent, S A S van der; Fehling, U.; Braam, U.; Schunack, Walter; Schmutzler, W.

doi:10.1007/bf01993129

Cited by 15 publications

(4 citation statements)

References 7 publications

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“…Its spontaneous histaminereleasing effect was thought to indicate the presence of the H 3 receptor, but the differing effects on stimulated and unstimulated cells suggested that H 3 -independent mechanisms may be involved. The existence of the H 3 receptor on the human basophil has also been investigated, 18 but no modulation of IgE-mediated histamine release was observed after incubation with RAMHA and thioperamide. In addition, IgE-independent basophil mediator release was studied in atopic dermatitis patients by Bull et al and neither RAMHA nor thioperamide modulated histamine release.…”

Section: Discussionmentioning

confidence: 99%

The intradermal effects of the H₃ receptor agonist R α methylhistamine in human skin

Kavanagh

Sabroe

Greaves

et al. 1998

British Journal of Dermatology

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We have investigated the possible existence of the H3 histamine receptor in human skin with the highly selective ligands R alpha methylhistamine (RAMHA) (H3 agonist) and thioperamide (H3 antagonist). We compared the intradermal effects of RAMHA with histamine, and studied their potential modulation by the H1 antagonist terfenadine, and H2 antagonist cimetidine. The effects of RAMHA and thioperamide on codeine phosphate-, substance P- and histamine-induced weal and flare responses were also studied. RAMHA produced dose-related weal and flare responses that were approximately 10- and fivefold less, respectively, than responses to histamine. Flare responses to RAMHA were significantly inhibited by oral terfenadine (P < 0.05). Weal and flare responses to histamine after oral cimetidine showed much intersubject variation, and cimetidine did not significantly alter either RAMHA- or histamine-induced weal and flare responses. Codeine phosphate-, substance P- and histamine-induced responses were not significantly affected by concurrent administration of RAMHA. Thioperamide was not found to influence codeine phosphate-, substance P-, RAMHA- or histamine-induced effects. RAMHA induces vascular (weal and flare) responses in human skin, and these responses are partially inhibited by terfenadine. There is a trend for RAMHA to have an additive effect to the weal induced by substance P and histamine, although our results largely do not reach statistical significance. Thioperamide does not affect the vascular responses to RAMHA, codeine phosphate, histamine or substance P. We cannot conclude that the effects of RAMHA are induced by H3 receptors on cutaneous endothelial or mast cells.

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Section: Discussionmentioning

confidence: 99%

The intradermal effects of the H₃ receptor agonist R α methylhistamine in human skin

Kavanagh

Sabroe

Greaves

et al. 1998

British Journal of Dermatology

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“…H3 receptors were initially found on rat peritoneal and cutaneous (Ohkubo et al, 1994;Bissonnette, 1996) as well as on human adenoidal mast cells. (Bent et al, 1991) However, according to more recent data, they seem to be restricted to the central nervous system (Rozniecki et al, 1999). Expression of the H4 receptor has so far been described at the mRNA level with commercially available probes from cultured bone marrow-derived mast cells (Morse et al, 2001), and very recently also indirectly in receptor-deficient mice (Hofstra et al, 2003).…”

mentioning

confidence: 92%

Human Skin Mast Cells Express H2 and H4, but not H3 Receptors

Lippert¹,

Artuc

Grützkau

et al. 2004

Journal of Investigative Dermatology

135

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Mast cells generate and release histamine during anaphylactic reactions, and there is pharmacological evidence that histamine regulates this process via specific receptors. Therefore, we examined human leukemic (HMC-1) and normal skin mast cells for the expression of all four currently known histamine receptors. Both cell types expressed H2 and H4 receptors at mRNA and protein levels, whereas H3 receptor specific mRNA and receptor protein was undetectable. Similarly, immunohistochemistry of cutaneous tissue showed an absence of H3 receptor in these cells. Despite transcription of mRNA, H1 receptor protein was only moderately expressed in HMC-1 cells and was virtually absent in skin mast cells. Furthermore, only H1, H2, and H4 receptors were detectable by Western blot analysis of HMC-1 cells. Radiolabeled histamine binding was strongly inhibited only by H2 (ranitidine)- and H3/H4 (FUB 108)-specific antagonists. Histamine-induced increase of cAMP was inhibited by the H2 receptor antagonist famotidine, whereas induction of IP3 was not observed, making signaling via the H1 receptor unlikely. These data show that human mast cells constitutively express primarily H2 and H4 receptors and that H2 receptors are functionally linked to cellular processes. They provide new insights into the mechanisms that govern auto- and paracrine histamine-induced mast cell functions.

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“…The novel histamine H receptors were identified as inhibitory presynaptic autoreceptors on histamine-containing nerve terminals in the rat brain cortex but have since been shown to inhibit the release of various neurotransmitters both in the central and peripheral nervous systems. 2 Recent articles provide strong evidence for the presence of histamine H receptors at the different sites, including the rabbit middle cerebral artery endo-3,4 5 6 thelium,' guinea-pig aorta, mesenteric artery, rabbit saphenous artery, 7 guinea-pig myo- 8 9 cardium, guinea-pig ileum, guinea-pig lung and 10 11 I2 bronchiole, guinea-pig intestine, porcine small intestine, rabbit gastric glands, 14 human 15 adenoidal mast cells, human and rhesus monkey brain. 6 .The purpose of the present study was to determine whether histamine H receptors are localized on rat aorta endothelium and to assess their possible role in endothelium-dependent responses.…”

Section: Introductionmentioning

confidence: 99%

The evidence for histamine H₃ receptor‐mediated endothelium‐dependent relaxation in isolated rat aorta

Djuric

Andjelković

1995

Mediators of Inflammation

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The presence of histamine H3 receptors was evaluated on the rat aorta endothelium. In the presence of pyrilamine (1 nM, 7 nM, 10 nM) or thioperamide (1 nM, 10 nM, 30 nM) the concentration–response curve for histamine-induced (0.1 nM − 0.01 mM) endothelium-dependent rat aorta relaxation was shifted to the right without significant change of the Emax indicating competitive antagonism by pyrilamine (pA2 = 9.33 ± 0.34, slope = 1.09 ± 0.36) or thioperamide (pA2 =9.31 ± 0.16, slope=0.94 ± 0.10). Cimetidine (1 μM) did not influence histamine-induced endothelium-dependent rat aorta relaxation. In the presence of thioperamide (1 nM, 10 nM, 30 nM) the concentration–response curve for (R)α-MeHA-induced (0.1 nM − 0.01 mM) endothelium-dependent relaxation was shifted to the right without significant change of Emax indicated competitive antagonism by thioperamide (pA2 = 9.21 ± 0.4, slope = 1.03 ± 0.35). Pyrilamine (100 nM) or cimetidine (1 μM) did not influence (R)α-MeHA-induced endothelium-dependent rat aorta relaxation. These results suggest the presence of a heterogenous population of histamine receptors, H1 and H3, on rat aorta endothelium.

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The influence of H1-, H2- and H3-receptors on the spontaneous and ConA induced histamine release from human adenoidal mast cells

Cited by 15 publications

References 7 publications

The intradermal effects of the H₃ receptor agonist R α methylhistamine in human skin

The intradermal effects of the H₃ receptor agonist R α methylhistamine in human skin

Human Skin Mast Cells Express H2 and H4, but not H3 Receptors

The evidence for histamine H₃ receptor‐mediated endothelium‐dependent relaxation in isolated rat aorta

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The influence of H1-, H2- and H3-receptors on the spontaneous and ConA induced histamine release from human adenoidal mast cells

Cited by 15 publications

References 7 publications

The intradermal effects of the H3 receptor agonist R α methylhistamine in human skin

The intradermal effects of the H3 receptor agonist R α methylhistamine in human skin

Human Skin Mast Cells Express H2 and H4, but not H3 Receptors

The evidence for histamine H3 receptor‐mediated endothelium‐dependent relaxation in isolated rat aorta

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Product

Resources

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The intradermal effects of the H₃ receptor agonist R α methylhistamine in human skin

The intradermal effects of the H₃ receptor agonist R α methylhistamine in human skin

The evidence for histamine H₃ receptor‐mediated endothelium‐dependent relaxation in isolated rat aorta