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Antiallergic effects of astemizole on immediate type hypersensitivity reactions.
Methods Find Exp Clin Pharmacol. 1990 Oct; 12(8):531-9.MF

Abstract

Astemizole (0.5-5 mg/kg, p.o.) dose-dependently inhibited heterologous and homologous PCA reactions in rats at ID50 values of 1.48 mg/kg and 2.37 mg/kg, respectively. The inhibitory effect of astemizole on heterologous PCA was most remarkable when this compound was given p.o. 2 h prior to antigen challenge. Astemizole (0.1-5 mg/kg, p.o.) dose-dependently inhibited experimentally-induced asthma in guinea pigs at an ID50 of 0.86 mg/kg. Ex vivo, astemizole (0.5-5 mg/kg, p.o.) inhibited antigen-induced histamine release from lung pieces of sensitized guinea pigs. In in vitro experiments, the drug dose-dependently inhibited antigen-induced histamine and SRS-A releases from guinea pig lung pieces at concentrations of 0.05-10 microM. Furthermore, astemizole (0.1-10 microM) inhibited the histamine release induced by compound 48/80 and antigen-antibody reaction from rat peritoneal mast cells, and at 0.1-500 nM inhibited both leukotriene C4- and platelet-activating factor (PAF)-induced contraction of isolated guinea pig trachea at submicromolar concentrations. Astemizole not only inhibited 45Ca uptake into rat mast cells but also prevented the Ca2+ release from the intracellular Ca store induced by compound 48/80, although this compound did not affect the histamine release from permeabilized mast cells induced by Ca2+. Our results suggest that one of the antiallergic mechanisms of astemizole may be an inhibition of signal transduction from the mast cell membrane to the intracellular systems.

Authors+Show Affiliations

Department of Pharmacology, Faculty of Pharmaceutical Sciences, Okayama University, Japan.No affiliation info availableNo affiliation info availableNo affiliation info available

Pub Type(s)

Journal Article

Language

eng

PubMed ID

1709434

Citation

Tasaka, K, et al. "Antiallergic Effects of Astemizole On Immediate Type Hypersensitivity Reactions." Methods and Findings in Experimental and Clinical Pharmacology, vol. 12, no. 8, 1990, pp. 531-9.
Tasaka K, Akagi M, Izushi K, et al. Antiallergic effects of astemizole on immediate type hypersensitivity reactions. Methods Find Exp Clin Pharmacol. 1990;12(8):531-9.
Tasaka, K., Akagi, M., Izushi, K., & Mio, M. (1990). Antiallergic effects of astemizole on immediate type hypersensitivity reactions. Methods and Findings in Experimental and Clinical Pharmacology, 12(8), 531-9.
Tasaka K, et al. Antiallergic Effects of Astemizole On Immediate Type Hypersensitivity Reactions. Methods Find Exp Clin Pharmacol. 1990;12(8):531-9. PubMed PMID: 1709434.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Antiallergic effects of astemizole on immediate type hypersensitivity reactions. AU - Tasaka,K, AU - Akagi,M, AU - Izushi,K, AU - Mio,M, PY - 1990/10/1/pubmed PY - 1990/10/1/medline PY - 1990/10/1/entrez SP - 531 EP - 9 JF - Methods and findings in experimental and clinical pharmacology JO - Methods Find Exp Clin Pharmacol VL - 12 IS - 8 N2 - Astemizole (0.5-5 mg/kg, p.o.) dose-dependently inhibited heterologous and homologous PCA reactions in rats at ID50 values of 1.48 mg/kg and 2.37 mg/kg, respectively. The inhibitory effect of astemizole on heterologous PCA was most remarkable when this compound was given p.o. 2 h prior to antigen challenge. Astemizole (0.1-5 mg/kg, p.o.) dose-dependently inhibited experimentally-induced asthma in guinea pigs at an ID50 of 0.86 mg/kg. Ex vivo, astemizole (0.5-5 mg/kg, p.o.) inhibited antigen-induced histamine release from lung pieces of sensitized guinea pigs. In in vitro experiments, the drug dose-dependently inhibited antigen-induced histamine and SRS-A releases from guinea pig lung pieces at concentrations of 0.05-10 microM. Furthermore, astemizole (0.1-10 microM) inhibited the histamine release induced by compound 48/80 and antigen-antibody reaction from rat peritoneal mast cells, and at 0.1-500 nM inhibited both leukotriene C4- and platelet-activating factor (PAF)-induced contraction of isolated guinea pig trachea at submicromolar concentrations. Astemizole not only inhibited 45Ca uptake into rat mast cells but also prevented the Ca2+ release from the intracellular Ca store induced by compound 48/80, although this compound did not affect the histamine release from permeabilized mast cells induced by Ca2+. Our results suggest that one of the antiallergic mechanisms of astemizole may be an inhibition of signal transduction from the mast cell membrane to the intracellular systems. SN - 0379-0355 UR - https://www.unboundmedicine.com/medline/citation/1709434/Antiallergic_effects_of_astemizole_on_immediate_type_hypersensitivity_reactions_ DB - PRIME DP - Unbound Medicine ER -