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 PharmacotherapyNew 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 ChemistryChanges in gene expression induced by histamine, fexofenadine and osthole: Expression of histamine H<inf>1</inf> receptor, COX-2, NF-κB, CCR1, chemokine CCL5/RANTES and interleukin-1β in PBMC allergic and non-allergic patients
2017, ImmunobiologyCitation Excerpt :The biological effects of histamine on H1 receptors include smooth muscle contraction, bronchospasm, increased vascular permeability and stimulation of sensory nerves and cough receptors (Jutel et al., 2001). The clinical consequences are manifested as urticaria, allergic rhino-conjunctivitis, broncho-constriction in asthma and cutaneous reactions to allergens and chemicals (Debacker et al., 1993; Kreutner et al., 2000; Matsubara et al., 2005). Osthole has been used as an herbal drug in traditional medicines for thousands of years (Kermani et al., 2016) with immuno-modulatory (You et al., 2009), anti-inflammatory (Asif, 2015; Chao et al., 2010), anti-tumor (Zhou and Liu, 2005) and anti-allergic effects (Kordulewska et al., 2015).
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 Letters