Abbreviations: A1R: Adenosine A1 Receptor; A2AR: Adenosine A2A Receptor; A2BR: Adenosine A2B Receptor; A3R: Adenosine A3 Receptor; Cpd: Compound; D2R: Dopamine D2 Receptor; Emax: Efficacy; gp: Guinea-pig; GPCR: G-Protein Coupled Receptor; h: Human; H1R: Histamine H1 Receptor; H3R: Histamine H3 Receptor; r: rat; 5-HT1AR: Serotonine 5-HT1A Receptor; βR: β-Adrenergic Receptors; β2R: Adrenergic β2 ...

The diverse functions of histamine are mediated by four specific histamine receptor subtypes, which belong to the family of G-protein-coupled receptors. Here, we summarize data obtained with histamine-deficient L-histidine decarboxylase knockout and histamine receptor subtype knockout mice in inflammation models. Advantages and disadvantages of the knockout approaches compared with pharmacologi...

Study was made of the developmental mechanism of histamine induced ulcers and inhibitory effects of receptor antagonists from the view point of gastric acidity and microvasculature of the gastric mucosa, and the following results were obtained. 1. In histamine induced ulcers, hypersecretion of gastric acid caused by histamine is not the primary developmental mechanism of the lesion. The main ca...

One of the common side effects of antihistamine medicines is xerostomia (dry mouth). The current consensus is that antihistamine-induced xerostomia comes from an antimuscarinic effect. Although the effect of antihistamines on salivary secretion is both obvious and significant, the cellular mechanism whereby this happens is still unclear because of the lack of knowledge of histamine signaling in...

Histamine mediates its physiological function through binding to four known histamine receptors. Here, we describe the first selective antagonist of the histamine H4 receptor, the newest member of the histamine receptor family, and provide evidence that such antagonists have anti-inflammatory activity in vivo. 1-[(5-chloro-1H-indol-2-yl)carbonyl]-4-methylpiperazine (JNJ 7777120) has a K(i) of 4...

Antihistamines, more formally termed H1 receptor antagonists, are well known to exert sedative effects in humans, yet their locus and mechanism of action in the human brain remains unknown. To better understand this phenomenon, the effects of histamine upon human cortical neurons were studied using intracellular recordings in brain slices maintained in vitro. Bath application of 50 microM hista...

The diverse functions of histamine are mediated by four specific histamine receptor subtypes, which belong to the family of Gprotein-coupled receptors. Here, we summarize data obtained with histamine-deficient L-histidine decarboxylase knockout and histamine receptor subtype knockout mice in inflammation models. Advantages and disadvantages of the knockout approaches compared with pharmacologic...

In gastric parietal cells the histamine H2 receptor is involved in gastric acid secretion. Molecular cloning of the cDNA for the histamine H2 receptor has revealed that the receptor is a member of the G-protein coupled receptor family. We expressed histamine H2 receptors in CHO cells, COS7 cells, and Sf9 cells to analyze N-glycosylation, palmitoylation, and desensitization of the H2 receptor, w...

background: previous investigations have revealed, cimetidine, a histamine h2-receptor antagonist, show radioprotective effects against gamma- and neutron-induced micronuclei in bone marrow erythrocytes. in this study, the anticlastogenic effects of famotidine and ranitidine, which act similar to cimetidine as histamine h2-receptor antagonists, was investigated. materials and methods : balb/c m...

Diamine oxidase (DAO) is abundantly expressed in mammalian small intestine catalyzing the oxidative breakdown of polyamines and histamine. The aim of this study was to determine the relationship between stimulation of intestinal diamine oxidase secretion with intestinal fat absorption and histamine release. Conscious intestinal lymph fistula rats were used. The mesenteric lymph ducts were cannu...