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Inhibition of chemiluminescence in granulocytes and alveolar macrophages by azelastine

  • Allergy, Histamine und Kinins
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Abstract

The effect of azelastine, an orally effective antiasthmatic/antiallergic drug, on the generation of oxygenderived free radicals in phagocytes was investigated using different chemiluminescence-assays. The chemiluminescence (CL) of both human polymorphonuclear granulocytes (PMNL) and guinea-pig alveolar macrophages (AM) was induced either by phorbol myristate acetate (PMA) or zymosan and amplified either by lucigenin or DMNH (7-dimethylamino-naphthalene-1,2-dicarbonic-acidhydrazide). The inhibitory effect of azelastine was dependent on the inducer employed and the condition and type of cells used. Azelastine reduced PMA-induced CL concentration-dependently in both PMNL (IC30=3.9 μM) and AM (IC30=9.8 μM). In AM zymosan-induced CL was inhibited 21.7% by 10 μM azelastine, whereas in PMNL it remained unchanged up to 10 μM azelastine. Azelastine has a significantly stronger inhibitory effect (IC30=4.2 μM) on oxygen free radical generation in AM primed by fetal calf serum than in unprimed AM. Based on present results it is likely that azelastine inhibitis oxygen-derived free radical generation by interaction with protein kinase C.

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  1. Department of Pharmacology, ASTA Pharma AG, Weismüller-Straße 45, D-6000, Frankfurt, FRG

    J. Schmidt, B. Kaufmann, R. Lindstaedt & I. Szelenyi

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Schmidt, J., Kaufmann, B., Lindstaedt, R. et al. Inhibition of chemiluminescence in granulocytes and alveolar macrophages by azelastine. Agents and Actions 31, 229–236 (1990). https://doi.org/10.1007/BF01997613

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