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. is a synthetic imidazoline derivative classified as a first-generation antihistaminic compound. As a small-molecule, non-peptide entity, it exhibits notable antagonistic activity at histamine H1 receptors, rendering it a valuable tool in the study of histaminergic signaling pathways. Its well-characterized pharmacological profile, including anticholinergic and local anesthetic properties, has established it as a reference compound in a variety of biochemical and pharmacological research contexts. The Ph. Eur. designation indicates compliance with the quality attributes defined by the European Pharmacopoeia, underscoring its suitability for rigorous laboratory and industrial applications where high analytical standards are required.
Pharmacological research: Antazoline Hydrochloride serves as a reference standard for the investigation of histamine-mediated biological responses. Its selective antagonism of H1 receptors enables researchers to dissect the molecular mechanisms underlying allergic reactions, inflammatory processes, and neurotransmitter regulation. Utilizing this compound in in vitro assays, receptor-binding studies, and functional cellular models facilitates the characterization of histaminergic pathways and the evaluation of novel antihistaminic agents.
Analytical method development: The compound is frequently employed as a calibration standard or positive control in chromatographic and spectroscopic methods designed to quantify antihistamines in pharmaceutical formulations and biological matrices. Its defined chemical structure and consistent physicochemical properties make it an ideal candidate for validating analytical techniques such as HPLC, LC-MS, and related methodologies. These applications support quality control, stability testing, and impurity profiling within research and industrial settings.
Receptor binding studies: In receptor pharmacology, Antazoline Hydrochloride is used to probe the specificity and affinity of histamine H1 receptor interactions. By serving as a competitive antagonist in radioligand binding assays or fluorescence-based screening platforms, it assists in the determination of receptor-ligand kinetics and the elucidation of binding site characteristics. This approach is critical for drug discovery programs targeting histaminergic signaling and for benchmarking the activity of experimental compounds.
Biochemical pathway elucidation: The compound's dual activity as an antihistaminic and anticholinergic agent enables its application in the mapping of intersecting neurotransmitter systems. Researchers utilize it to differentiate between histaminergic and cholinergic contributions to physiological and pathophysiological responses in tissue preparations, organ bath experiments, and electrophysiological recordings. Such studies are instrumental in advancing the understanding of central and peripheral nervous system regulation.
Formulation and excipient compatibility studies: In pharmaceutical development, Antazoline Hydrochloride is incorporated into compatibility assessments with various excipients and delivery systems. Its stability profile and reactivity are evaluated during preformulation research to inform the design of robust dosage forms and to anticipate potential interactions that could impact product performance. These investigations are essential for ensuring the integrity and efficacy of final pharmaceutical products intended strictly for research and development purposes.
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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