Biochemical and Biophysical Research Communications
Molecular cloning of the human histamine H2 receptor
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Expression and localization of histamine H<inf>1</inf>, H<inf>2</inf>, and H<inf>3</inf> receptors in rat olfactory epithelium
2017, International Journal of Pediatric OtorhinolaryngologyCherry-picked ligands at histamine receptor subtypes
2016, NeuropharmacologyCitation Excerpt :The H2R was recognized in 1972 following the discovery that numerous physiological effects of histamine, including the stimulation of gastric acid secretion, increase of heart rate, and inhibition of rat uterus contraction were not blocked by the H1R antagonist mepyramine (Black et al., 1972). Moreover, cloning of the H2R allowed studies which indicated strong expression in the stomach and brain (Gantz et al., 1991). Clinically, H2R antagonists shaped the treatment regimen of dyspepsia, oesophageal and gastric ulcers, a trend that sustained until these drugs were mostly substituted by proton pump inhibitors (Panula et al., 2015).
Molecular and cellular analysis of human histamine receptor subtypes
2013, Trends in Pharmacological SciencesEvidence for ligand-specific conformations of the histamine H <inf>2</inf>-receptor in human eosinophils and neutrophils
2012, Biochemical PharmacologyCitation Excerpt :The longer isoform 1 was identified by the Mammalian Gene Collection Program of the National Institutes of Health [56] and encodes 397 amino acids. The isoform 2, which was cloned from human gastric mucosa [57] has a truncated C-terminus compared to the isoform 1 and encodes a protein of 359 amino acids. No PCR product was obtained upon use of primers specific for isoform 1 (Fig. 5B, lane 3) expected PCR product length 1197 bp), whereas the expected 1085 bp long PCR product could be detected with an isoform 2 specific primer pair (Fig. 5B, lane 5).
Discovery of potent and selective histamine H<inf>3</inf> receptor inverse agonists based on the 3,4-dihydro-2H-pyrazino[1,2-a]indol-1-one scaffold
2010, Bioorganic and Medicinal Chemistry LettersScombroid poisoning: A review
2010, ToxiconCitation Excerpt :This assay is actually responding to H1-agonist activity and this approach could be updated and extended by developing cell lines rich in the relevant histaminergic receptors. Transvected cells could be used for this purpose since the H1 receptor has been cloned (Fujimoto et al., 1993) as have the H2 (Gantz et al., 1991), H3 (Lovenberg et al., 1999) and H4 (Liu et al., 2001) receptors. The viability of cell assays in the study of other seafood toxins in samples from outbreak-implicated sample extracts has been demonstrated (Manger et al., 1995) and proved especially powerful when combined with analysis of individual LC-MS fractions (Dickey et al., 1999; Dickey, 2008); combined activity and structure information were easily obtained, even for toxins and toxin metabolites for which no purified standards were available.
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Present address: Department of Internal Medicine, Universität Kiel, Germany.