Biochemical and Biophysical Research Communications
Regular ArticleLysine200 Located in the Fifth Transmembrane Domain of the Histamine H1 Receptor Interacts with Histamine but Not with All H1 Agonists
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Evolutionary history of histamine receptors: Early vertebrate origin and expansion of the H<inf>3</inf>-H<inf>4</inf> subtypes
2021, Molecular Phylogenetics and EvolutionRoles of Lys191 and Lys179 in regulating thermodynamic binding forces of ligands to determine their binding affinity for human histamine H<inf>1</inf> receptors
2020, Biochemical PharmacologyCitation Excerpt :Since the mutation of Lys1915.39 reduced the binding affinity for histamine but not the non-imidazole agonist 2-(2-pyridyl)ethylamine, which was due to decreases in the enthalpy-dependent electrostatic binding forces of histamine, electrostatic interactions between Lys1915.39 and the imidazole group of histamine appeared to be important in determining the affinity for histamine. These results are consistent with a previous report stating that Lys2005.39 of the guinea-pig H1 receptor, which corresponds to Lys1915.39 of the human H1 receptor, interacts with the Nπ-nitrogen of histamine [25]. Interestingly, although the mutation of Lys179ECL2 to alanine decreased the enthalpy-dependent electrostatic binding forces of histamine as well as 2-(2-pyridyl)ethylamine, their affinity for the H1 receptors increased due to concomitant increases in their entropy-dependent hydrophobic binding forces.
HMF causes anaphylactic symptoms by acting as a H<inf>1</inf> receptor agonist
2020, Biochemical PharmacologyCitation Excerpt :Histamine is known to bring several complex physiologic changes, including neurotransmission, inflammation, smooth muscle contraction, dilatation of capillaries, chemotaxis, cytokine production, and gastric acid secretion. Activation of the H1 receptor by histamine and other agonists cause endothelial cells to contract, leading to increased vascular permeability and release of a variety of bioactive substances, including nitric oxide [14–16]. Therefore, we suspected that the hind-paw swelling and extravasation caused by HMF were the results of H1 activation.
Molecular and cellular analysis of human histamine receptor subtypes
2013, Trends in Pharmacological SciencesRegulation of the immune response and inflammation by histamine and histamine receptors
2011, Journal of Allergy and Clinical ImmunologyCitation Excerpt :H1R is encoded by an intronless gene, which is located on chromosome 3p25 and contains 487 amino acids. The 56-kd H1R is expressed by a broad range of cell types, including neurons, airway and vascular smooth muscle cells, hepatocytes, chondrocytes, endothelial cells, DCs, monocytes, neutrophils, and T and B cells.26-29 H1R gene expression can be upregulated by IL-3, IL-4, and histamine.30
Binding mode analysis and enrichment studies on homology models of the human histamine H4 receptor
2008, European Journal of Medicinal ChemistryCitation Excerpt :Site-directed mutagenesis studies revealed that the protonated ethylamine function of histamine forms H-bond to the conserved Asp (3.32) in both cases. In the case of H1R, the imidazole N(3)–H and N(1) interact with Asn198 (5.46) [60] and Lys191 (5.39) [61], respectively, while in H2R, the imidazole N(3)–H and N(1) form interactions with Asp186 (5.42) and Thr190 (5.46), respectively [62]. H4R has a similarly low level of homology for H1R and H2R as for any other GPCR [9].