Molecular mechanism of antihistamines recognition and …
2024年1月2日 · Histamine receptors are a group of G protein-coupled receptors (GPCRs) that play important roles in various physiological and pathophysiological conditions. Antihistamines that target the...
Histamine, histamine receptors, and anti-histamines in the …
2019年4月24日 · Simultaneous activation of H 1 and H 2 receptors via histamine can lead to clinical symptoms of anaphylaxis such as hypotension, tachycardia, flushing, and headache. With its diverse distribution and various effector activities, the H 1 receptor is involved in allergic rhinitis, asthma, atopic dermatitis, conjunctivitis, and urticaria development.
Molecular Determinants of the Kinetic Binding Properties of ...
Kinetic analyses of the rate constants of association and dissociation (k on and k off, respectively) of antihistamines have suggested that second-generation antihistamines have a long duration of action owing to the long residence time (1/k off) at the H 1 receptors. In this study, we examined the relationship between the kinetic and ...
Pharmacology of Antihistamines - PMC - PubMed Central (PMC)
This article reviews the molecular biology of the interaction of histamine with its H 1-receptor and describes the concept that H 1-antihistamines are not receptor antagonists but are inverse agonists i.e. they produce the opposite effect on the receptor to histamine.
Pharmacology of Antihistamines - World Allergy Organization …
This article reviews the molecular biology of the interaction of histamine with its H 1 -receptor and describes the concept that H 1 -antihistamines are not receptor antagonists but are inverse agonists i.e. they produce the opposite effect on the receptor to histamine.
Novel Insights on the Biology and Immunological Effects of Histamine…
5 天之前 · Histamine (C 5 H 9 N 3, molecular weight 111.15 g/mol) is a well-studied endogenous biogenic amine composed of an imidazole ring attached to an ethylamine side chain.It has a limited half-life of a few minutes within tissues and in circulation. Several cell types including mast cells (MCs), basophils, platelets, histaminergic neurons, and enterochromaffin cells produce varying amounts of ...
Structural basis of ligand recognition and design of antihistamines ...
2024年3月20日 · Histamine, a biogenic amine chemical messenger, plays pivotal roles in various physiological and pathophysiological processes through binding and activating histamine receptors (H 1 R-H 4 R),...
Structural basis for recognition of antihistamine drug by human ...
2022年10月15日 · Here we report the crystal structure of human histamine receptor H 3 R bound to an antagonist PF-03654746 at 2.6 Å resolution. Combined with the computational and functional assays, our...
Histamine and antihistamines - ScienceDirect
2024年10月1日 · Clinically used antihistamines demonstrate inverse agonism to the histamine receptor and drugs are available with activity at H1, H2 and H3 receptors. H1 antihistamines are used in the treatment of allergy, and are classified as either first or second generation.
Antihistamines - StatPearls - NCBI Bookshelf
2023年7月10日 · There are two main classes of histamine receptors: H-1 receptors and H-2 receptors. Antihistamine drugs that bind to H-1 receptors are generally used to treat allergies and allergic rhinitis. Drugs that bind to H-2 receptors can treat upper gastrointestinal conditions that are caused by excessive stomach acid.