Histamine receptors: subclasses and specific ligands

Haaksma, Eric E. J.; Leurs, Rob; Timmerman, H.

doi:10.1016/0163-7258(90)90046-5

Cited by 75 publications

(30 citation statements)

References 148 publications

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“…H1R, a Gq-coupled receptor, associates with phospholipase C; and stimulation of the receptor leads to the formation of two second messengers, inositol 1,4,5-trisphosphate (IP 3 ) and 1,2-diacylglycerol (17,18). IP 3 induces the release of Ca 2+ from intracellular stores, and Ca 2+ and 1,2-diacylglycerol activate PKC.…”

Section: Introductionmentioning

confidence: 99%

β2-Adrenergic Receptor-Mediated Histamine H1 Receptor Down-Regulation: Another Possible Advantage of β2 Agonists in Asthmatic Therapy

et al. 2004

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Abstract. To clarify heterologous regulation of a receptor is important in considering medication. Histamine constricts the airway smooth muscle through the action to the H 1 receptor (H1R), which contributes to asthma. b 2 -Adrenergic receptor (b2R) agonists are widely used in asthmatic therapy for their bronchodilating effects. In this study, we investigated the effect of b2R activation on the H1R function using Chinese hamster ovary cells stably co-expressing human histamine H1R and b2R (CHO-H1/ b2 cell). The stimulation of b2R resulted in the decrease of H1R in the membrane. Heterologous H1R down-regulation was significantly reversed in the presence of the cyclic AMP-dependent protein kinase (PKA) inhibitor KT5720. Since phosphorylation of G protein-coupled receptor (GPCR) by second messenger-dependent kinases, is proposed to be a key step initiating heterologous receptor desensitization, we examined whether heterologous H1R down-regulation was accompanied by H1R phosphorylation. H1R was phosphorylated by b2R stimulation; however, a PKA inhibitor did not inhibit heterologous H1R phosphorylation. Our results suggest that H1R was heterologously regulated by b2R. Not only a direct action of b2R agonist to b2R causing bronchodilation but also indirect action that reduces the number of H1R responsible for bronchoconstriction might contribute to a decrease in the bronchial resistance, which proposes another possible advantage of b2R agonists for asthmatic medication.

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Section: Introductionmentioning

confidence: 99%

β2-Adrenergic Receptor-Mediated Histamine H1 Receptor Down-Regulation: Another Possible Advantage of β2 Agonists in Asthmatic Therapy

et al. 2004

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“…The histamine H 1 receptor (H1R), one of the G protein-coupled receptors (GPCRs), predominantly couples with Gq / 11 protein and phospholipase C-b and mediates type I allergy in peripheral tissues and histaminergic neurotransmission in the central nervous system (1,2). Desensitization of various GPCRs including H1R has been documented and is thought to be a protection mechanism of receptor-bearing cells against excess stimulation.…”

Section: Introductionmentioning

confidence: 99%

Histamine H1 Receptor Down-Regulation Mediated by M3 Muscarinic Acetylcholine Receptor Subtype

et al. 2004

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Abstract. Heterologous down-regulation of histamine H 1 receptor (H1R) mediated by muscarinic acetylcholine receptor subtype was investigated using five kinds of Chinese hamster ovary (CHO) cells stably co-expressing the human H1R and one of the five (M 1 -M 5 ) muscarinic acetylcholine receptors, CHO-H1/ M1, CHO-H1/ M2, CHO-H1/ M3, CHO-H1/ M4, and CHO-H1/ M5 cells. Among the CHO-H1/ M1, CHO-H1/ M3, and CHO-H1/ M5 cells, carbachol treatment of the CHO-H1/ M3 cells time-dependently led to remarkable down-regulation of the H1R to 60% of the control level. In contrast, stimulation of CHO-H1/ M1 cells by carbachol induced negligible effect on the down-regulation. Stimulation of CHO-H1/ M5 cells by carbachol induced significant but only small H1R down-regulation. M 2 and M 4 muscarinic receptors showed negligible effect on the down-regulation. H1R-mediated accumulation of inositol phosphates in CHO-H1/ M3 cells with long-term expose to carbachol was decreased to 60% compared with non-treated cells. Heterologous phosphorylation of H1R was induced by the stimulation of each muscarinic receptor. H1R was phosphorylated by about twofold from the basal level through five subtypes of muscarinic receptor. The M 3 muscarinic receptor-mediated phosphorylation of H1R was reversed by the inhibition of protein kinase C. In the present study we demonstrated that the M 3 muscarinic acetylcholine receptor mediated remarkable down-regulation of the H1R with decreased receptor signaling.

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“…Pharmacological studies, and more recently gene cloning, have established that multiple receptor types (HI, H, and H,) exist for histamine (Haaksma et al, 1990;Parsons, 1991). While all the histamine receptors are recognized by histamine, they are nevertheless pharmacologically distinct and are encoded by separate genes.…”

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confidence: 99%

Stable Expression of Human H₁‐histamine‐receptor cDNA in Chinese Hamster Ovary Cells

Moguilevsky

Varsalona

Noyer

et al. 1994

European Journal of Biochemistry

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A cDNA clone for the histamine HI receptor was isolated from a human lung cDNA library; it encoded a protein of 487 amino acids which showed characteristic features of G-protein-coupled receptors. The percentages of identity of the deduced amino acid sequence with bovine, rat and guinea pig H, histamine receptors were 82.6%, 79.4% and 73.3%, respectively, whereas these percentages decreased to 74.6%, 66% and 56.7% for the amino acid sequence of the third intracellular loop. The human H,-receptor cDNA was transfected into Chinese hamster ovary cells (CHO) via an eukaryotic expression vector ; the receptor protein present on cell membranes specifically bound [3H]mepyramine with a Kd of 3.7 nM. The binding was displaced by H,-histamine-receptor antagonists and histamine. Northern blot analysis indicated the presence of two histamine HI receptor mRNAs of 3.5 kb and 4

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Histamine receptors: subclasses and specific ligands

Cited by 75 publications

References 148 publications

β2-Adrenergic Receptor-Mediated Histamine H1 Receptor Down-Regulation: Another Possible Advantage of β2 Agonists in Asthmatic Therapy

β2-Adrenergic Receptor-Mediated Histamine H1 Receptor Down-Regulation: Another Possible Advantage of β2 Agonists in Asthmatic Therapy

Histamine H1 Receptor Down-Regulation Mediated by M3 Muscarinic Acetylcholine Receptor Subtype

Stable Expression of Human H₁‐histamine‐receptor cDNA in Chinese Hamster Ovary Cells

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Histamine receptors: subclasses and specific ligands

Cited by 75 publications

References 148 publications

β2-Adrenergic Receptor-Mediated Histamine H1 Receptor Down-Regulation: Another Possible Advantage of β2 Agonists in Asthmatic Therapy

β2-Adrenergic Receptor-Mediated Histamine H1 Receptor Down-Regulation: Another Possible Advantage of β2 Agonists in Asthmatic Therapy

Histamine H1 Receptor Down-Regulation Mediated by M3 Muscarinic Acetylcholine Receptor Subtype

Stable Expression of Human H1‐histamine‐receptor cDNA in Chinese Hamster Ovary Cells

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Stable Expression of Human H₁‐histamine‐receptor cDNA in Chinese Hamster Ovary Cells