Antistine-Privine (Antazoline Sulfate) is a 1st generation antihistamine, with good anticholinergic properties. It is used to relieve nasal congestion and added in eye drops, usually in combination with naphazoline, to relieve the symptoms of allergic conjunctivitis.
CAT No: 10-101-110
CAS No:91-75-8 (net), 24359-81-7 (sulfate)
Synonyms/Alias:2-(N-Phenyl-N-benzyl-aminomethyl)imidazoline · sulfate; 2-[(N-Benzylanilino)methyl]-2-imidazoline · sulfate; 4,5-Dihydro-N-phenyl-N-(phenylmethyl)-1H-imidazole-2-methanamine · sulfate
Chemical Name:N-benzyl-N-(4,5-dihydro-1H-imidazol-2-ylmethyl)aniline;sulfuric acid
Antazoline Sulfate is a synthetic organic compound classified as an antihistaminic agent, structurally characterized by its imidazoline core and commonly supplied in the sulfate salt form for enhanced solubility and stability. As a small-molecule histamine H1 receptor antagonist, it is widely recognized for its ability to modulate histaminergic signaling pathways in vitro and in biochemical assays. Its physicochemical properties and defined mode of action have established it as a valuable reference compound in receptor-binding studies, pharmacological profiling, and cellular signaling research. Due to its well-documented interactions with histamine receptors, antazoline sulfate is frequently employed in experimental designs exploring the molecular basis of allergic responses and the pharmacodynamics of histaminergic modulation.
Receptor Binding Assays: Antazoline sulfate is extensively utilized in receptor binding studies to elucidate the affinity and selectivity of ligands for histamine H1 receptors. Researchers employ it as a standard antagonist in radioligand binding experiments to characterize receptor-ligand interactions, quantify binding kinetics, and benchmark the activity of novel compounds. Its established pharmacological profile enables precise comparison and calibration of assay systems, supporting the development of new histaminergic modulators and facilitating the interpretation of competitive binding data.
Signal Transduction Studies: The compound serves as an effective probe for dissecting histaminergic signal transduction pathways in cell-based assays. By antagonizing H1 receptor-mediated responses, it allows investigators to differentiate between receptor subtypes and to map downstream signaling cascades, such as intracellular calcium mobilization or phospholipase C activation. These applications are critical for understanding the cellular consequences of histamine receptor engagement and for delineating the molecular mechanisms underlying allergic and inflammatory phenomena.
Pharmacological Profiling: In drug discovery and development, antazoline sulfate is routinely incorporated as a reference standard in high-throughput screening and pharmacological profiling platforms. Its consistent antagonist activity provides a benchmark for evaluating the potency, efficacy, and selectivity of investigational compounds targeting the histamine H1 receptor. This role is essential for structure-activity relationship studies, enabling medicinal chemists to optimize candidate molecules and predict their pharmacodynamic properties.
Allergy and Inflammation Research: The compound is a key tool in experimental models designed to investigate the molecular and cellular mechanisms of allergic and inflammatory responses. By selectively inhibiting histamine-induced effects, it assists researchers in isolating the contribution of H1 receptor signaling to processes such as vascular permeability, leukocyte recruitment, and cytokine release. Its use in vitro and in animal studies enhances the resolution of mechanistic insights into hypersensitivity reactions and supports the validation of anti-allergic strategies.
Analytical Method Development: Antazoline sulfate is also employed in the development and validation of analytical methods for quantifying histaminergic agents in complex biological matrices. Its well-defined chemical properties and stability make it suitable as an internal standard or calibration reference in chromatographic and spectrometric assays. These applications are instrumental for pharmacokinetic studies, quality control testing, and the establishment of robust bioanalytical protocols in research and industrial laboratories.
Antazoline seems to be safe agent in termination of AF in patients undergoing pulmonary vein isolation. We also observed satisfying efficacy, which needs to be proved in a randomized clinical trial.
Balsam P, Koźluk E, Peller M, et al. Antazoline for termination of atrial fibrillation during the procedure of pulmonary veins isolation[J]. Advances in medical sciences, 2015, 60(2): 231-235.
Intravenous antazoline was effective and safe in the rapid conversion of non-valvular paroxysmal atrial fibrillation to sinus rhythm in patients without heart failure.
Maciag A, Farkowski M M, Chwyczko T, et al. Efficacy and safety of antazoline in the rapid cardioversion of paroxysmal atrial fibrillation (the AnPAF Study)[J]. EP Europace, 2016: euw384.
Antazoline is an old antihistaminic and new antiarrhythmic agent with unknown mechanisms of action which recently has been shown to effectively terminate atrial fibrillation. The aim of study was to examine the effects of antazoline on hemodynamic and ECG parameters.
Piotrowski R, Giebułtowicz J, Baran J, et al. Antazoline—insights into drug‐induced electrocardiographic and hemodynamic effects: Results of the ELEPHANT II substudy[J]. Annals of Noninvasive Electrocardiology, 2017.
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