Biochemical and Biophysical Research Communications
Regular ArticleGenomic Cloning, Heterologous Expression and Pharmacological Characterization of a Human Histamine H1 Receptor
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Histamine H3 receptor antagonists – Roles in neurological and endocrine diseases and diabetes mellitus
2022, Biomedicine and PharmacotherapyCitation Excerpt :Second generation antihistamines were introduced in 1981 [16], and cardiac toxicity of the H1 antihistamines was reported in 1986 [17]. Human H2 receptor was cloned in 1991 [18] and H1 receptor was cloned in 1993 [19]. Human H3 receptor was cloned in 1999 [20] and human H4 receptor was cloned in 2000 [21].
New insights on the arylpiperazinylalkyl pyridazinone ET1 as potent antinociceptive and anti-inflammatory agent
2020, European Journal of PharmacologyCitation Excerpt :The histamine H1 receptor binding assay was performed on recombinant CHO cells expressing human receptor membrane extracts, using 1.2 nM [3H]Pyrilamine as radioligand. Non-specific binding was measured in the presence of 1 μM of Pyrilamine, in incubation buffer containing 50 mM Tris-HCl, pH 7.4, 2 mM MgCl, 100 mM NaCl, 250 mM Sucrose (De Backer et al., 1993). The sigma non-opioid intracellular receptor 1 (σ1) binding assay was performed on human Jurkat cells membrane extracts, using 8 nM [3H]Haloperidol as radioligand.
Structural and clinical impact of anti-allergy agents: An overview
2020, Bioorganic ChemistryCitation Excerpt :A.1 Mechanism of action Zafirlukast is an antagonist of cysteinyl leukotriene receptor-1 (CysLT1), a receptor found throughout the smooth muscle of the lungs, within interstitial lung macrophages (white blood cells that operate in the interstitial space of the lungs), and rarely in epithelial cells [120–122]. CystLT1 is a receptor for a specific class of leukotrienes that contain the amino acid cysteine.
Molecular and cellular analysis of human histamine receptor subtypes
2013, Trends in Pharmacological SciencesCitation Excerpt :Based on the limitations of hHxR analysis in native human cells, recombinant systems are essential for comprehensive hHxR characterization. hHxRs have been expressed in classic mammalian expression systems, including HEK293 cells, CHO cells, NIH-3T3 cells, and COS-7 cells (Table 2) [57–61]. hH3R and hH4R have also been expressed in SK-N-MC cells (Table 2) [55].
Synthesis, biological evaluation and SAR studies of benzimidazole derivatives as H <inf>1</inf>-antihistamine agents
2012, Chinese Chemical LettersCitation Excerpt :Compounds 17e and 17f with CH2 between benzimidazole and piperidine were 2–5-fold more active than 17a and 17b in which benzimidazole directly linked to piperidine, whereas 3–10-fold improvement was observed for 17c and 17d with a carbon–carbon double bond between benzimidazole and piperidine. The further receptor binding assay [14] indicated that all tested compounds displaced the radioligand (3H-mepyramine) from H1 receptor with an IC50 ranging from 0.8 to 717 nmol/L (Table 1). In this respect, compounds 17d are more active than astermizole and desloratadine, while compounds (17c, 17e, 17f) showed the same order of magnitude of an affinity for the receptor as the controls.