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Kempuraj D, Huang M, Kandere K, et al. Azelastine is more potent than olopatadine n inhibiting interleukin-6 and tryptase release from human umbilical cord blood-derived cultured mast cells. Ann Allergy Asthma Immunol. 2002;88(5):501-6doi: 10.1016/s1081-1206(10)62389-7.
Kempuraj, D., Huang, M., Kandere, K., Boucher, W., Letourneau, R., Jeudy, S., Fitzgerald, K., Spear, K., Athanasiou, A., & Theoharides, T. C. (2002). Azelastine is more potent than olopatadine n inhibiting interleukin-6 and tryptase release from human umbilical cord blood-derived cultured mast cells. Annals of allergy, asthma & immunology : official publication of the American College of Allergy, Asthma, & Immunology, 88(5), 501-6. https://doi.org/10.1016/s1081-1206(10)62389-7
Kempuraj, Duraisamy, et al. "Azelastine is more potent than olopatadine n inhibiting interleukin-6 and tryptase release from human umbilical cord blood-derived cultured mast cells." Annals of allergy, asthma & immunology : official publication of the American College of Allergy, Asthma, & Immunology vol. 88,5 (2002): 501-6. doi: https://doi.org/10.1016/s1081-1206(10)62389-7
Kempuraj D, Huang M, Kandere K, Boucher W, Letourneau R, Jeudy S, Fitzgerald K, Spear K, Athanasiou A, Theoharides TC. Azelastine is more potent than olopatadine n inhibiting interleukin-6 and tryptase release from human umbilical cord blood-derived cultured mast cells. Ann Allergy Asthma Immunol. 2002 May;88(5):501-6. doi: 10.1016/s1081-1206(10)62389-7. PMID: 12027072.
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Ann Allergy Asthma Immunol. 2002 May;88(5):501-6. doi: 10.1016/s1081-1206(10)62389-7.

Azelastine is more potent than olopatadine n inhibiting interleukin-6 and tryptase release from human umbilical cord blood-derived cultured mast cells.

Annals of allergy, asthma & immunology : official publication of the American College of Allergy, Asthma, & Immunology

Duraisamy Kempuraj, Man Huang, Kristiana Kandere, William Boucher, Richard Letourneau, Sheila Jeudy, Kim Fitzgerald, Kathleen Spear, Achilles Athanasiou, Theoharis C Theoharides

Affiliations

  1. Department of Pharmacology and Experimental Therapeutics, Tufts University School of Medicine and New England Medical Center, Boston, Massachusetts 02111, USA.

PMID: 12027072 DOI: 10.1016/s1081-1206(10)62389-7

Abstract

BACKGROUND: Mast cells are involved in early- and late-phase reactions by releasing vasoactive molecules, proteases, and cytokines. Certain histamine-1 receptor antagonists and other antiallergic drugs seem to inhibit the release of mediators from rat and human mast cells.

OBJECTIVE: Azelastine and olopatadine are antiallergic agents present in the ophthalmic solutions azelastine hydrochloride (Optivar, Asta Medica/Muro Pharmaceuticals, Tewksbury, MA), and olopatadine hydrochloride (Patanol, Alcon Laboratories, Fort Worth, TX), respectively. We investigated the effect of these drugs on interleukin-6 (IL-6), tryptase, and histamine release from cultured human mast cells (CHMCs).

METHODS: CHMCs were grown from human umbilical cord blood-derived CD34+ cells in the presence of stem cell factor and IL-6 for 14 to 16 weeks. Sensitized CHMCs were pretreated with various concentrations of azelastine or olopatadine for 5 minutes. CHMCs were then challenged with anti-immunoglobulin E, and the released mediators were quantitated.

RESULTS: The greatest inhibition of mediator release was seen with 24 microM azelastine; this level of inhibition was matched with the use of 133 microM olopatadine. At this concentration, these drugs inhibited IL-6 release by 83% and 74%, tryptase release by 55% and 79%, and histamine release by 41% and 45%, respectively. Activated CHMCs were characterized by numerous filopodia that were inhibited by both drugs as shown by electron microscopy.

CONCLUSIONS: These results indicate that azelastine and olopatadine can inhibit CHMCs activation and release of IL-6, tryptase, and histamine. On an equimolar basis, azelastine was a more potent inhibitor than olopatadine.

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