Antazoline Phosphate, as phosphate salt of antazoline, is the histamine H1 receptor antagonist. It acts as an antihistamine. Generally by combinating with a decongestant, antazoline phosphate is applied topically to relieve the symptoms of allergic conjunctivitis.
CAT No: 10-101-109
CAS No:91-75-8 (net), 154-68-7 (phosphate)
Synonyms/Alias:2-(N-Phenyl-N-benzyl-aminomethyl)imidazoline . phosphate; 2-[(N-Benzylanilino)methyl]-2-imidazoline . phosphate; 4,5-Dihydro-N-phenyl-N-(phenylmethyl)-1H-imidazole-2-methanamine . phosphate
Chemical Name:N-benzyl-N-(4,5-dihydro-1H-imidazol-2-ylmethyl)aniline;phosphoric acid
Antazoline Phosphate is a synthetic antihistaminic compound belonging to the ethylenediamine class, recognized for its unique molecular structure that enables selective interaction with histamine receptors. As a water-soluble salt form, it demonstrates enhanced stability and compatibility for a wide range of laboratory and research applications. Its chemical properties make it an ideal candidate for studies requiring precise modulation of histaminergic pathways, and its versatility has led to its adoption in various scientific investigations. Researchers value Antazoline Phosphate for its ability to serve as a reliable tool in dissecting complex biological responses associated with allergic and inflammatory processes, as well as for its role in elucidating signal transduction mechanisms at the cellular level.
Allergy Research: Antazoline Phosphate is extensively utilized in allergy research to investigate the mechanisms underlying histamine-mediated responses. By acting as a competitive antagonist at histamine H1 receptors, it allows scientists to effectively block histaminic activity in experimental models. This facilitates the study of allergic reactions, including vascular permeability, smooth muscle contraction, and sensory nerve stimulation, thereby contributing to the development of new therapeutic strategies for hypersensitivity disorders. Its application in in vitro and in vivo systems provides valuable insights into the modulation of immune responses and the identification of novel targets for anti-allergic agents.
Inflammatory Pathway Analysis: In the context of inflammation research, Antazoline Phosphate serves as a critical probe for delineating the role of histamine in the initiation and propagation of inflammatory cascades. By inhibiting histamine-induced signaling, researchers can assess the contribution of this biogenic amine to cytokine release, leukocyte recruitment, and tissue edema. The compound's utility extends to the evaluation of anti-inflammatory drug candidates, where it is employed to establish baseline responses and to differentiate between histamine-dependent and independent mechanisms. This approach aids in the comprehensive understanding of inflammatory pathophysiology and the refinement of pharmacological intervention strategies.
Neuropharmacological Investigations: Antazoline Phosphate is also applied in neuropharmacological studies aimed at exploring the influence of histaminergic modulation on neuronal activity. Its ability to traverse biological membranes and interact with central and peripheral H1 receptors makes it a valuable agent for examining the effects of histamine antagonism on neurotransmission, synaptic plasticity, and behavioral outcomes. Researchers utilize it to dissect the interplay between histamine and other neurotransmitter systems, such as acetylcholine and dopamine, which is crucial for advancing knowledge in neurobiology and for the identification of potential neuroprotective compounds.
Cellular Signaling Studies: The phosphate salt of antazoline is frequently employed in cellular signaling research to probe the downstream effects of histamine receptor engagement. By selectively blocking H1 receptor activation, it enables the characterization of secondary messenger systems, such as cyclic AMP and calcium mobilization, in various cell types. This application is instrumental in mapping the intricate networks that govern cellular responses to external stimuli, facilitating the discovery of signaling modulators and the development of targeted molecular interventions.
Biochemical Assays: In biochemical assay development, Antazoline Phosphate is used as a reference antagonist to validate the specificity and sensitivity of histamine detection methods. Its well-defined pharmacological profile allows for the standardization of assay conditions and the benchmarking of novel analytical techniques. Researchers leverage its properties to optimize assay performance, ensuring accurate quantification of histamine and related metabolites in complex biological matrices. This supports advancements in diagnostic research and the monitoring of histamine dynamics in physiological and pathological states.
Pharmacodynamic Modeling: For pharmacological modeling, Antazoline Phosphate is incorporated into experimental protocols to simulate histamine blockade and to analyze the pharmacodynamic interactions between multiple receptor systems. Its predictable antagonistic activity provides a foundation for constructing dose-response relationships and for evaluating the efficacy of combination therapies in preclinical models. By integrating it into these studies, scientists can refine their understanding of receptor pharmacology, optimize dosing regimens, and contribute to the rational design of multi-target agents for research use.
A controlled, double-blind comparison of naphalzoline hydrochloride 0.05%, antazoline phosphate 0.5%, a combination of both components and a placebo was performed on 51 ragweed sensitive patients presenting allergic conjunctivitis. Evaluation of response at various times after instillation of medication for lacrimation, conjunctival inflammation, pruritus, photophobia and pain showed naphazoline hydrochloride, antazoline phosphate and the combination product superior to placebo. The combination product was statistically significantly superior for conjunctival inflammation and photophobia. The need for post-challenge treatment with epinephrine hydrochloride was significantly less in those eyes treated with the combination product. demonstrating prophylactic efficacy.
Miller J, Wolf E H. Antazoline phosphate and naphazoline hydrochloride, singly and in combination for the treatment of allergic conjunctivitis-a controlled, double-blind clinical trial[J]. Annals of allergy, 1975, 35(2): 81-86.
A method for the determination of 2-[(N-phenyl)benzylaminomethyl]-2-imidazoline X H3PO4 (antazoline phosphate) and 2-(1,2,3,4-tetrahydro-1-naphthyl)-2-imidazoline X HCl (tetrahydrozoline hydrochloride) in ophthalmic solution is described. The pharmaceutical preparation is analysed directly by reversed-phase ion-pair high-performance liquid chromatography and the method is very rapid, selective and simple.
Puglisi G, Sciuto S, Chillemi R, et al. Simultaneous high-performance liquid chromatographic determination of antazoline phosphate and tetrahydrozoline hydrochloride in ophthalmic solution[J]. Journal of Chromatography A, 1986, 369: 165-170.
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