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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.

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Authors

Chand N
No affiliation info available
Pillar J
No affiliation info available
Diamantis W
No affiliation info available
Perhach JL
No affiliation info available
Sofia RD
No affiliation info available

MeSH

AnimalsAscitic FluidCalcimycinCalciumDiphenhydramineHistamine H1 AntagonistsHistamine ReleaseKetotifenMaleMast CellsPhthalazinesPyridazinesRatsRats, Inbred Strains

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 -