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 antihistaminic compound belonging to the class of ethylenediamine derivatives, widely recognized for its potent H1-receptor antagonist properties. Exhibiting a unique molecular architecture, Antazoline Sulfate is characterized by high water solubility and stability, making it suitable for diverse experimental and formulation purposes. Its rapid onset of action and ability to block histamine-induced responses have positioned it as a valuable tool in various biochemical, pharmacological, and analytical research settings. The compound's compatibility with multiple delivery systems further expands its utility, allowing for seamless integration into complex investigative protocols and product development pipelines.
Pharmacological Research: In pharmacological research, Antazoline Sulfate serves as a robust reference compound for studying histamine-mediated pathways and receptor pharmacodynamics. Researchers frequently utilize it to delineate the mechanisms underlying allergic reactions and to characterize the efficacy of novel antihistaminic agents. By selectively inhibiting H1 receptors, Antazoline Sulfate facilitates the elucidation of histamine's role in smooth muscle contraction, vascular permeability, and neurotransmission, thereby contributing to a deeper understanding of allergic and inflammatory processes at the cellular and systemic levels.
Allergy Model Development: For the development of allergy models, this compound is instrumental in simulating and modulating hypersensitivity responses in vitro and in vivo. Scientists employ Antazoline Sulfate to induce or attenuate allergic reactions within controlled environments, enabling the assessment of immunological parameters such as mast cell degranulation, cytokine release, and leukocyte migration. These studies are critical for screening anti-allergic compounds, optimizing dosing regimens, and investigating the pathophysiology of allergic diseases.
Analytical Method Validation: Analytical laboratories leverage Antazoline Sulfate as a standard or internal control in the validation of chromatographic and spectrophotometric methods. Its well-defined physicochemical properties allow for precise calibration and quantification in complex matrices, supporting the accurate measurement of antihistaminic agents in pharmaceutical formulations and biological samples. The use of this compound enhances the reliability and reproducibility of analytical protocols, which is essential for quality control and regulatory compliance in research and development environments.
Formulation Science: In the field of formulation science, Antazoline Sulfate is frequently incorporated into experimental delivery systems to evaluate solubility, stability, and release kinetics. Its compatibility with various excipients and carriers makes it an ideal candidate for pre-formulation studies, where researchers assess the impact of formulation variables on drug performance. Insights gained from these studies inform the design of optimized dosage forms and contribute to the advancement of innovative drug delivery technologies.
Receptor Binding Assays: Receptor binding assays benefit from the use of Antazoline Sulfate as a competitive ligand in radioligand binding and displacement studies. By occupying H1 receptor sites, it enables the quantification of binding affinities and the investigation of receptor-ligand interactions with high specificity. These assays are fundamental for the characterization of histaminergic signaling pathways and the identification of novel therapeutic targets in allergy and inflammation research.
Biomedical Research: In broader biomedical research, Antazoline Sulfate is applied to probe cellular responses to histamine and to dissect the molecular mechanisms driving immune modulation. Its use in cell-based assays, tissue preparations, and organ bath experiments allows scientists to monitor functional changes in response to histaminergic stimulation or inhibition. Through these multifaceted applications, Antazoline Sulfate continues to advance scientific knowledge and foster innovation across pharmacology, analytical chemistry, and biomedical research disciplines.
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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