Azatadine

Azatadine is an histamine and cholinergic inhibitor with IC50 of 6.5 nM and 10 nM, respectively.

Determination of azatadine in human plasma by liquid chromatography/tandem mass spectrometry.[Pubmed:21737359]

J Chromatogr B Analyt Technol Biomed Life Sci. 2011 Aug 1;879(23):2189-93.

A sensitive method using liquid chromatography with tandem mass spectrometric detection (LC-MS/MS) was developed and validated for the analysis of antihistamine drug Azatadine in human plasma. Loratadine was used as internal standard (IS). Analytes were extracted from human plasma by liquid/liquid extraction using ethyl acetate. The organic phase was reduced to dryness under a stream of nitrogen at 30 degrees C and the residue was reconstituted with the mobile phase. 5 muL of the resulting solution was injected onto the LC-MS/MS system. A 4.6 mm x 150 mm, I.D. 5 mum, Agilent TC-C(18) column was used to perform the chromatographic analysis. The mobile phase consisted of ammonium formate buffer 0.010 M (adjusted to pH 4.3 with 1M formic acid)/acetonitrile (20:80, v/v) The chromatographic run time was 5 min per injection and flow rate was 0.6 mL/min. The retention time was 2.4 and 4.4 min for Azatadine and IS, respectively. The tandem mass spectrometric detection mode was achieved with electrospray ionization (ESI) iron source and the multiple reaction monitoring (MRM) (291.3 --> 248.2m/z for Azatadine, 383.3 --> 337.3m/z for IS) was operated in positive ion modes. The low limit of quantitation (LLOQ) was 0.05 ng/mL. The intra-day and inter-day precision of the quality control (QC) samples was 8.93-11.57% relative standard deviation (RSD). The inter-day accuracy of the QC samples was 96.83-105.07% of the nominal values.

Syntheses of molecularly imprinted polymers: Molecular recognition of cyproheptadine using original print molecules and azatadine as dummy templates.[Pubmed:19084632]

Anal Chim Acta. 2009 Jan 12;631(2):237-44.

The use of custom-made polymeric materials with high selectivities as target molecules in solid-phase extraction (SPE), known as molecularly imprinted solid-phase extraction (MISPE), is becoming an increasingly important sample preparation technique. However, the potential risk of leakage of the imprinting molecules during the desorption phase has limited application. The use of a mimicking template, called a dummy molecular imprinting polymer (DMIP), that bears the structure of a related molecule and acts as a putative imprinting molecule may provide a useful solution to this problem. In the current study, cyproheptadine (CPH) and Azatadine (AZA) were used as templates in the development of an MIP and DMIP for acrylic acid and methacrylic acid monomers. Our results indicate that DMIPs have equal recognition of CPH, avoiding the problem of leakage of original template during the desorption phase relative to MIPs synthesized in presence of the print molecule CPH. Examination of the surface structure of the two polymer products by SEM shows appreciable differences in structural morphology and function of the monomers employed. These results are well supplemented by data obtained for swelling ratios and solvent uptake. Molecular modelling of CPH and AZA suggests that both substrates are similar in shape and volume.

Fungal biotransformation of the antihistamine azatadine by Cunninghamella elegans.[Pubmed:8795241]

Appl Environ Microbiol. 1996 Sep;62(9):3477-9.

The metabolism of the antihistamine Azatadine by the zygomycete fungus Cunninghamella elegans ATCC 9245 was investigated. Within 72 h from the addition of the drug to 48-h-old cultures grown in Sabouraud dextrose broth, 95% of Azatadine was biotransformed. Two major metabolites, 7-hydroxyAzatadine (25%) and 8-hydroxyAzatadine (50%), and two minor metabolites, N-desmethylAzatadine and 9-hydroxyAzatadine, were isolated by high-performance liquid chromatography and characterized by mass spectrometric and proton nuclear magnetic resonance spectroscopic analyses.

Comparative effects of loratadine and azatadine in the treatment of seasonal allergic rhinitis.[Pubmed:1982614]

Asian Pac J Allergy Immunol. 1990 Dec;8(2):103-7.

The efficacy and safety of loratadine 10 mg once daily were compared with Azatadine 1 mg twice daily in controlling symptoms of seasonal allergic rhinitis. The study was a randomized, double-blind, parallel-group design involving 34 patients receiving either loratadine or Azatadine for 14 days. Both treatments were effective in relieving the histamine-mediated symptoms of seasonal allergic rhinitis. At baseline, 100% and 93% of the patients in the loratadine and Azatadine treatment groups, respectively, had moderate or severe symptoms of disease; at endpoint of treatment 80% of the patients in the loratadine treatment group and 92% of those in the Azatadine treatment group had mild or no disease symptoms. Sedation was reported by fewer patients in the loratadine treatment group than in the Azatadine group. Thus loratadine is an effective and safe antihistamine when given once daily for the symptomatic relief of seasonal allergic rhinitis.