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Antiallergic effects of terfenadine on immediate type hypersensitivity reactions.
Immunopharmacol Immunotoxicol. 1987; 9(2-3):257-79.II

Abstract

Terfenadine dose-dependently inhibited rat homologous PCA (2.5-10 mg/kg, p.o.) and experimentally-induced asthma in guinea pigs (0.5-5 mg/kg, p.o.). Similarly, metabolites I and II dose-dependently inhibited experimentally-induced asthma but their respective potencies were approximately 1/2 and 1/15th that of terfenadine. These results suggest that the metabolites contribute to the antiallergic effects of terfenadine. In ex vivo, terfenadine (5-20 mg/kg, p.o.) also inhibited the release of both antigen-induced histamine and SRS-A from sensitized guinea pig lung samples and that of histamine from rat peritoneal mast cells. Terfenadine dose-dependently increased the cAMP content in rat mast cells and in the lungs; in the latter, the augmented cAMP is associated with an increase in adenylate cyclase activity, but not with the inhibition of phosphodiesterase activity. The above evidence indicates that the inhibitory effects of terfenadine on mediator release from mast cells are in some way related to its antiallergic effects, and that an elevated cAMP content may be effective to enhance mediator release inhibition.

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

2449487

Citation

Akagi, M, et al. "Antiallergic Effects of Terfenadine On Immediate Type Hypersensitivity Reactions." Immunopharmacology and Immunotoxicology, vol. 9, no. 2-3, 1987, pp. 257-79.
Akagi M, Mio M, Miyoshi K, et al. Antiallergic effects of terfenadine on immediate type hypersensitivity reactions. Immunopharmacol Immunotoxicol. 1987;9(2-3):257-79.
Akagi, M., Mio, M., Miyoshi, K., & Tasaka, K. (1987). Antiallergic effects of terfenadine on immediate type hypersensitivity reactions. Immunopharmacology and Immunotoxicology, 9(2-3), 257-79.
Akagi M, et al. Antiallergic Effects of Terfenadine On Immediate Type Hypersensitivity Reactions. Immunopharmacol Immunotoxicol. 1987;9(2-3):257-79. PubMed PMID: 2449487.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Antiallergic effects of terfenadine on immediate type hypersensitivity reactions. AU - Akagi,M, AU - Mio,M, AU - Miyoshi,K, AU - Tasaka,K, PY - 1987/1/1/pubmed PY - 1987/1/1/medline PY - 1987/1/1/entrez SP - 257 EP - 79 JF - Immunopharmacology and immunotoxicology JO - Immunopharmacol Immunotoxicol VL - 9 IS - 2-3 N2 - Terfenadine dose-dependently inhibited rat homologous PCA (2.5-10 mg/kg, p.o.) and experimentally-induced asthma in guinea pigs (0.5-5 mg/kg, p.o.). Similarly, metabolites I and II dose-dependently inhibited experimentally-induced asthma but their respective potencies were approximately 1/2 and 1/15th that of terfenadine. These results suggest that the metabolites contribute to the antiallergic effects of terfenadine. In ex vivo, terfenadine (5-20 mg/kg, p.o.) also inhibited the release of both antigen-induced histamine and SRS-A from sensitized guinea pig lung samples and that of histamine from rat peritoneal mast cells. Terfenadine dose-dependently increased the cAMP content in rat mast cells and in the lungs; in the latter, the augmented cAMP is associated with an increase in adenylate cyclase activity, but not with the inhibition of phosphodiesterase activity. The above evidence indicates that the inhibitory effects of terfenadine on mediator release from mast cells are in some way related to its antiallergic effects, and that an elevated cAMP content may be effective to enhance mediator release inhibition. SN - 0892-3973 UR - https://www.unboundmedicine.com/medline/citation/2449487/Antiallergic_effects_of_terfenadine_on_immediate_type_hypersensitivity_reactions_ L2 - https://www.tandfonline.com/doi/full/10.3109/08923978709035214 DB - PRIME DP - Unbound Medicine ER -