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 organic compound classified as an antihistaminic agent, notable for its imidazoline structure and phosphate salt form. As a member of the first-generation H1-receptor antagonists, it is primarily recognized for its ability to modulate histaminergic signaling pathways. The phosphate salt enhances its aqueous solubility, making it suitable for a variety of biochemical and analytical applications. Its unique chemical properties and well-characterized mechanism of action have established its relevance in histamine research, receptor binding studies, and drug screening protocols within the life sciences sector.
Pharmacological research: Antazoline Phosphate serves as a valuable tool in the investigation of histamine H1-receptor interactions and the broader pharmacodynamics of antihistaminic compounds. Researchers utilize it in in vitro and ex vivo systems to elucidate the molecular mechanisms underlying histamine-mediated responses, such as smooth muscle contraction, vascular permeability, and neurotransmitter release. By selectively inhibiting H1-receptor activity, the compound enables detailed dissection of histaminergic pathways, contributing to a deeper understanding of allergic and inflammatory processes at the cellular and tissue levels.
Receptor binding assays: The compound is frequently employed in competitive binding experiments to quantify the affinity and specificity of candidate molecules targeting histamine H1-receptors. Radioligand displacement studies and fluorescence-based assays benefit from the well-defined binding characteristics of Antazoline Phosphate, allowing for accurate assessment of receptor-ligand interactions. Such applications are essential for the characterization of novel antihistaminic agents, structure-activity relationship (SAR) analyses, and the optimization of lead compounds in pharmaceutical research.
Analytical standard: Due to its chemical stability and well-documented analytical profile, Antazoline Phosphate functions as a reference standard in chromatographic and spectrophotometric methods. Laboratories incorporate it into quality control protocols to validate the performance of analytical instruments, ensure the accuracy of quantitative assays, and support the identification of related substances in complex matrices. Its use as a calibration standard enhances the reliability and reproducibility of analytical results across diverse research and industrial settings.
Metabolic studies: The compound is utilized in studies of xenobiotic metabolism to investigate its biotransformation, enzymatic pathways, and potential metabolite profiles. By tracing its metabolic fate in microsomal preparations, liver homogenates, or cell-based systems, scientists gain insights into the enzymatic processes governing imidazoline derivatives. These investigations inform risk assessment, support toxicological evaluations, and contribute to the broader field of drug metabolism and pharmacokinetics.
Chemical synthesis and method development: Antazoline Phosphate is also relevant as a model imidazoline derivative in synthetic organic chemistry. Its structural features facilitate the exploration of novel synthetic methodologies, phosphate salt formation, and the development of analogs with tailored physicochemical or pharmacological properties. Synthetic chemists may use it as a benchmark compound when designing new synthetic routes or optimizing purification protocols for related molecules, thereby advancing compound library development and chemical process innovation.
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.
1. Adipose tissue is a key organ for the beneficial effects of GLP-2 metabolic function
3. Store-operated Ca2+ entry sustains the fertilization Ca2+ signal in pig eggs
4. Emerging applications of nanotechnology for diagnosis and therapy of disease: a review
If you have any peptide synthesis requirement in mind, please do not hesitate to contact us at . We will endeavor to provide highly satisfying products and services.
Creative Peptides is a trusted CDMO partner specializing in high-quality peptide synthesis, conjugation, and manufacturing under strict cGMP compliance. With advanced technology platforms and a team of experienced scientists, we deliver tailored peptide solutions to support drug discovery, clinical development, and cosmetic innovation worldwide.
From custom peptide synthesis to complex peptide-drug conjugates, we provide flexible, end-to-end services designed to accelerate timelines and ensure regulatory excellence. Our commitment to quality, reliability, and innovation has made us a preferred partner across the pharmaceutical, biotechnology, and personal care industries.
Read More