Antazoline hydrochloride is an antagonist of histamine H1 receptors, with anticholinergic properties. It is used to relieve nasal congestion and in eye drops.
CAT No: 10-101-108
CAS No:91-75-8 (net), 2508-72-7 (hydrochloride)
Synonyms/Alias:2-(N-Phenyl-N-benzyl-aminomethyl)imidazoline . HCl; 2-[(N-Benzylanilino)methyl]-2-imidazoline . HCl; 4,5-Dihydro-N-phenyl-N-(phenylmethyl)-1H-imidazole-2-methanamine . HCl
Chemical Name:N-benzyl-N-(4,5-dihydro-1H-imidazol-2-ylmethyl)aniline;hydrochloride
Antazoline Hydrochloride Ph. Eur., a well-characterized synthetic derivative of ethylenediamine, is widely recognized for its unique physicochemical properties and versatile applications in scientific research and industrial settings. As a member of the first-generation antihistamines, Antazoline Hydrochloride exhibits a stable crystalline structure and high solubility in aqueous environments, making it suitable for diverse formulation and analytical requirements. Its molecular architecture enables selective interactions with histamine receptors, positioning it as a valuable tool in studies involving histaminergic pathways and receptor pharmacology. Researchers and product developers appreciate its compatibility with various excipients and solvents, which facilitates its integration into complex experimental systems and product prototypes. The compound's established safety profile and predictable reactivity further enhance its attractiveness for laboratory investigations and technology development.
Pharmacological Research: In pharmacological research, Antazoline Hydrochloride is extensively utilized to elucidate the mechanisms of histamine-mediated responses and to characterize the binding affinities of histamine receptor antagonists. By serving as a reference compound or positive control, it supports the validation of new molecular entities targeting H1 receptors, enabling comparative studies that inform drug discovery and development. Its well-documented interaction with histaminergic pathways allows for precise modulation of biological systems, making it indispensable in experimental protocols that require the inhibition of histamine-induced effects in vitro or in vivo models.
Allergy Pathway Investigation: Within the context of allergy pathway investigation, Antazoline Hydrochloride plays a pivotal role in dissecting the cellular and molecular processes underlying hypersensitivity reactions. Researchers employ it to block histamine activity in cell cultures or animal models, thereby delineating the contributions of histamine to inflammatory cascades, vascular permeability, and immune cell recruitment. Such studies are critical for advancing the understanding of allergic responses and for identifying novel targets for therapeutic intervention. By providing a reliable means to modulate histamine signaling, the compound accelerates progress in immunological and inflammatory research.
Analytical Method Development: Analytical chemists leverage Antazoline Hydrochloride as a standard or analyte in the development and validation of chromatographic and spectrophotometric methods. Its defined chemical structure and consistent performance enable accurate quantification and detection in complex matrices, supporting the quality control of pharmaceutical formulations and raw materials. The compound's compatibility with various analytical platforms, including HPLC and UV-Vis spectroscopy, ensures robust and reproducible results across different laboratories. This utility is particularly valuable in the context of method transfer and inter-laboratory studies, where consistency and traceability are paramount.
Pharmaceutical Formulation Studies: In the realm of pharmaceutical formulation studies, Antazoline Hydrochloride serves as a model compound for evaluating the performance of novel delivery systems and excipients. Its solubility profile and stability under a range of processing conditions make it suitable for examining the release kinetics, bioavailability, and compatibility of prototype formulations. Researchers use it to assess the impact of formulation variables on drug behavior, thereby informing the optimization of product design and manufacturing processes. The insights gained from such studies contribute to the development of more effective and reliable pharmaceutical products.
Biochemical Assays: Biochemical researchers utilize Antazoline Hydrochloride in assays designed to probe receptor-ligand interactions, enzyme activities, and signal transduction pathways. Its ability to selectively inhibit histamine-mediated events allows for the dissection of complex biochemical networks and the identification of downstream effectors. By incorporating it into functional assays, scientists can differentiate between histamine-dependent and independent mechanisms, enhancing the specificity and interpretability of experimental outcomes. This application extends to high-throughput screening platforms, where the compound's predictable activity streamlines the identification of active compounds and the elucidation of molecular targets. Through these diverse applications, Antazoline Hydrochloride Ph. Eur. continues to facilitate advancements in pharmaceutical, biochemical, and analytical research, underscoring its enduring value to the scientific community.
The dc-polarographic investigation of antazoline hydrochloride in aqueous acidic media is described. Using potassium chloride-hydrochloric acid mixture as the supporting electrolyte (pH = 3.25), antazoline hydrochloride was electrochemically reduced at the dropping mercury electrode, with the production of two waves with E1/2 values of --1.35 and --1.65 V respectively. As revealed from the study of the effect of mercury column height, pH of the medium and concentration of the depolarizer, the polarographic reduction of the antazolinium cation is preceded by a catalytic H-wave. The diffusion-controlled nature of the electrode process permitted the quantitative determination of antazoline hydrochloride in concentrations down to 1.0 . 10(-4)M. Application of the presented procedure to the analysis of different dosage forms of the compound studied proved successful and compared favourably with official estimations of anatazoline salts. In view of its simplicity, accuracy and sensitivity, the presented polarographic method can be recommended for routine analysis of antazoline formulations.
Issa I M, Omar N M, El-Shabouri S R, et al. Polarographic estimation of antazoline hydrochloride[J]. Die Pharmazie, 1978, 33(8): 513-515.
In order to evaluate the pharmacokinetics characteristic of antazoline hydrochloride in Beagle dogs, a sensitive and specific HPLC method was developed and validated using phenacetin as the internal standard (IS). The analyte and the IS were extracted from dog plasma by ethyl acetate under the basic condition. The analyte was separated by a C18 column and detected with a variable wavelength UV-detector. The mobile phase consisted of methanol-5mmolL(-1) tetrabutyl ammonium bromide (45:55, v/v) containing 0.5% glacial acetic acid in a flow rate of 1.0mLmin(-1). Standard calibration graph for antazoline was linear over a curve range of 20-1600ngmL(-1) (R>0.99) and the lower limit of quantification was 20ngmL(-1) using a plasma sample of 500μL. The intra- and inter-day precision values were less than 14.3% relative standard deviation (RSD). The intra-day assay accuracy was in the range of 98.1-100.6% and the inter-day assay accuracy in the range of 99.2-101.1%. The extraction recoveries were on the average of 88.4% for antazoline and 76.8% for IS. Plasma samples were stable at least for 1 month at -20℃. This method was successfully applied to pharmacokinetics study of antazoline after intravenous administration to Beagle dogs.
Li X, Chu Y, Ke Y, et al. Determination of antazoline hydrochloride in Beagle dog plasma by HPLC-UV and its application to pharmacokinetics[J]. Journal of Chromatography B, 2013, 929: 97-101.
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