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Inhibition of calcium ionophore (A23187)-stimulated histamine release from rat peritoneal mast cells by azelastine: implications for its mode of action.
Eur J Pharmacol. 1983 Dec 23; 96(3-4):227-33.EJ

Abstract

Azelastine is a novel, orally effective, long-acting, antiallergic agent. The ability of azelastine to influence calcium ionophore A23187-induced histamine release from rat peritoneal mast cells was investigated and compared with selected antiallergic drugs. The concentrations of drugs required to inhibit A23187 (0.2 microM)-stimulated histamine release by 50% (IC50S, microM) were as follows: azelastine 5; diphenhydramine 52; and ketotifen 200. Theophylline and sodium cromoglycate in a concentration range of 0.1-1000 microM failed to exert any significant inhibition of histamine release. The inhibitory effects of azelastine on A23187-stimulated histamine release were antagonized by high concentrations of exogenous Ca2+ ions. These data suggest that azelastine inhibits A23187-stimulated histamine release by interfering with the influx of Ca2+ into the mast cells.

Authors

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Pub Type(s)

Journal Article

Language

eng

PubMed ID

6202531

Citation

Chand, N, et al. "Inhibition of Calcium Ionophore (A23187)-stimulated Histamine Release From Rat Peritoneal Mast Cells By Azelastine: Implications for Its Mode of Action." European Journal of Pharmacology, vol. 96, no. 3-4, 1983, pp. 227-33.
Chand N, Pillar J, Diamantis W, et al. Inhibition of calcium ionophore (A23187)-stimulated histamine release from rat peritoneal mast cells by azelastine: implications for its mode of action. Eur J Pharmacol. 1983;96(3-4):227-33.
Chand, N., Pillar, J., Diamantis, W., Perhach, J. L., & Sofia, R. D. (1983). Inhibition of calcium ionophore (A23187)-stimulated histamine release from rat peritoneal mast cells by azelastine: implications for its mode of action. European Journal of Pharmacology, 96(3-4), 227-33.
Chand N, et al. Inhibition of Calcium Ionophore (A23187)-stimulated Histamine Release From Rat Peritoneal Mast Cells By Azelastine: Implications for Its Mode of Action. Eur J Pharmacol. 1983 Dec 23;96(3-4):227-33. PubMed PMID: 6202531.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Inhibition of calcium ionophore (A23187)-stimulated histamine release from rat peritoneal mast cells by azelastine: implications for its mode of action. AU - Chand,N, AU - Pillar,J, AU - Diamantis,W, AU - Perhach,J L,Jr AU - Sofia,R D, PY - 1983/12/23/pubmed PY - 2001/3/28/medline PY - 1983/12/23/entrez SP - 227 EP - 33 JF - European journal of pharmacology JO - Eur J Pharmacol VL - 96 IS - 3-4 N2 - Azelastine is a novel, orally effective, long-acting, antiallergic agent. The ability of azelastine to influence calcium ionophore A23187-induced histamine release from rat peritoneal mast cells was investigated and compared with selected antiallergic drugs. The concentrations of drugs required to inhibit A23187 (0.2 microM)-stimulated histamine release by 50% (IC50S, microM) were as follows: azelastine 5; diphenhydramine 52; and ketotifen 200. Theophylline and sodium cromoglycate in a concentration range of 0.1-1000 microM failed to exert any significant inhibition of histamine release. The inhibitory effects of azelastine on A23187-stimulated histamine release were antagonized by high concentrations of exogenous Ca2+ ions. These data suggest that azelastine inhibits A23187-stimulated histamine release by interfering with the influx of Ca2+ into the mast cells. SN - 0014-2999 UR - https://www.unboundmedicine.com/medline/citation/6202531/Inhibition_of_calcium_ionophore__A23187__stimulated_histamine_release_from_rat_peritoneal_mast_cells_by_azelastine:_implications_for_its_mode_of_action_ L2 - https://linkinghub.elsevier.com/retrieve/pii/0014-2999(83)90311-4 DB - PRIME DP - Unbound Medicine ER -