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Antiallergic effect of epinastine (WAL 801 CL) on immediate hypersensitivity reactions: (I). Elucidation of the mechanism for histamine release inhibition.
Immunopharmacol Immunotoxicol. 1992; 14(1-2):191-205.II

Abstract

Epinastine caused an inhibition of histamine release from rat peritoneal mast cells induced by both antigen-antibody reaction and compound 48/80. Epinastine was similarly effective in inhibiting compound 48/80-induced histamine release not only from isolated rat peritoneal mast cells but also from rat mesenterial pieces. Also, histamine release from lung pieces obtained from actively sensitized guinea pigs after exposure to antigen challenge was markedly inhibited by epinastine. The drug was effective in inhibiting not only Ca2+ uptake into lung mast cells in actively sensitized guinea pigs but also Ca2+ release from the intracellular Ca store of rat peritoneal mast cells exposed to both compound 48/80 and substance P. No significant changes were observed in phosphodiesterase activity in rat peritoneal mast cells treated with epinastine, while adenylate cyclase activity was augmented by epinastine. Epinastine has no inhibitory effect on histamine release induced by Ca2+ or IP3 from permeabilized mast cells. However, the drug significantly and dose-dependently suppressed calmodulin activity suggesting that histamine release inhibition due to epinastine may be partly attributable to Ca(2+)-calmodulin dependent process(es). The drug caused no visible changes in thermodynamic behavior of lipids, either in order parameter or in differential scanning calorimetry, indicating that the drug has no influence on membrane fluidity.

Authors+Show Affiliations

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

Pub Type(s)

Journal Article

Language

eng

PubMed ID

1375955

Citation

Kamei, C, et al. "Antiallergic Effect of Epinastine (WAL 801 CL) On Immediate Hypersensitivity Reactions: (I). Elucidation of the Mechanism for Histamine Release Inhibition." Immunopharmacology and Immunotoxicology, vol. 14, no. 1-2, 1992, pp. 191-205.
Kamei C, Akagi M, Mio M, et al. Antiallergic effect of epinastine (WAL 801 CL) on immediate hypersensitivity reactions: (I). Elucidation of the mechanism for histamine release inhibition. Immunopharmacol Immunotoxicol. 1992;14(1-2):191-205.
Kamei, C., Akagi, M., Mio, M., Kitazumi, K., Izushi, K., Masaki, S., & Tasaka, K. (1992). Antiallergic effect of epinastine (WAL 801 CL) on immediate hypersensitivity reactions: (I). Elucidation of the mechanism for histamine release inhibition. Immunopharmacology and Immunotoxicology, 14(1-2), 191-205.
Kamei C, et al. Antiallergic Effect of Epinastine (WAL 801 CL) On Immediate Hypersensitivity Reactions: (I). Elucidation of the Mechanism for Histamine Release Inhibition. Immunopharmacol Immunotoxicol. 1992;14(1-2):191-205. PubMed PMID: 1375955.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Antiallergic effect of epinastine (WAL 801 CL) on immediate hypersensitivity reactions: (I). Elucidation of the mechanism for histamine release inhibition. AU - Kamei,C, AU - Akagi,M, AU - Mio,M, AU - Kitazumi,K, AU - Izushi,K, AU - Masaki,S, AU - Tasaka,K, PY - 1992/1/1/pubmed PY - 1992/1/1/medline PY - 1992/1/1/entrez SP - 191 EP - 205 JF - Immunopharmacology and immunotoxicology JO - Immunopharmacol Immunotoxicol VL - 14 IS - 1-2 N2 - Epinastine caused an inhibition of histamine release from rat peritoneal mast cells induced by both antigen-antibody reaction and compound 48/80. Epinastine was similarly effective in inhibiting compound 48/80-induced histamine release not only from isolated rat peritoneal mast cells but also from rat mesenterial pieces. Also, histamine release from lung pieces obtained from actively sensitized guinea pigs after exposure to antigen challenge was markedly inhibited by epinastine. The drug was effective in inhibiting not only Ca2+ uptake into lung mast cells in actively sensitized guinea pigs but also Ca2+ release from the intracellular Ca store of rat peritoneal mast cells exposed to both compound 48/80 and substance P. No significant changes were observed in phosphodiesterase activity in rat peritoneal mast cells treated with epinastine, while adenylate cyclase activity was augmented by epinastine. Epinastine has no inhibitory effect on histamine release induced by Ca2+ or IP3 from permeabilized mast cells. However, the drug significantly and dose-dependently suppressed calmodulin activity suggesting that histamine release inhibition due to epinastine may be partly attributable to Ca(2+)-calmodulin dependent process(es). The drug caused no visible changes in thermodynamic behavior of lipids, either in order parameter or in differential scanning calorimetry, indicating that the drug has no influence on membrane fluidity. SN - 0892-3973 UR - https://www.unboundmedicine.com/medline/citation/1375955/Antiallergic_effect_of_epinastine__WAL_801_CL__on_immediate_hypersensitivity_reactions:__I___Elucidation_of_the_mechanism_for_histamine_release_inhibition_ L2 - https://www.tandfonline.com/doi/full/10.3109/08923979209009219 DB - PRIME DP - Unbound Medicine ER -