leukotriene-b4 has been researched along with epinastine* in 2 studies
2 other study(ies) available for leukotriene-b4 and epinastine
| Article | Year |
|---|---|
Pharmacological studies on the novel antiallergic drug HQL-79: II. Elucidation of mechanisms for antiallergic and antiasthmatic effects.
The effects of 4-benzhydryloxy-1-[3-(1H-tetrazol-5-yl)-propyl]piperidine (HQL-79), a newly developed antiallergic drug, on various chemical mediators and on chemical mediator release were investigated. Orally administered HQL-79 strongly inhibited the histamine-induced skin reaction in rats, and histamine- and 5-hydroxytryptamine (5-HT)-induced bronchoconstriction in guinea pigs. HQL-79 inhibited antigen-induced release of leukotriene (LT) B4, LTC4, histamine and prostaglandin (PG) D2 from the chopped lung tissues of actively sensitized guinea pigs. On the other hand, release of PGE2, one of the bronchoprotective prostanoids, was significantly enhanced by HQL-79. In an in vivo experiment, chronic administration of HQL-79 clearly reduced PGD2 contents and enhanced PGE2 contents in the lungs of repeatedly antigen-exposed guinea pigs. In biochemical studies, HQL-79 inhibited mouse spleen PGD synthase in a concentration-dependent manner. None of the antiallergics such as epinastine, terfenadine, oxatomide and cetirizine inhibited the PGD synthase. HQL-79 did not affect PGE synthase in sheep vesicular gland microsomes. These results suggest that antiallergic and antiasthmatic effects of HQL-79 could be ascribed to antihistaminic- and anti-5-HT effects, chemical mediator release inhibition, PGE2-release enhancement and PGD synthase inhibition. It is considered, in particular, that the differential modulation of PGD2 and PGE2 production is a conspicuous pharmacological feature of HQL-79. Topics: Animals; Anti-Allergic Agents; Anti-Asthmatic Agents; Antigens; Capillary Permeability; Dibenzazepines; Dinoprostone; Dose-Response Relationship, Drug; Free Radical Scavengers; Guinea Pigs; Histamine; Histamine H1 Antagonists; Histamine Release; Ileum; Imidazoles; In Vitro Techniques; Intramolecular Oxidoreductases; Ketotifen; Leukotriene B4; Leukotriene C4; Lipocalins; Lung; Male; Mice; Mice, Inbred ICR; Muscle Contraction; Piperidines; Prostaglandin D2; Prostaglandin-Endoperoxide Synthases; Rats; Rats, Wistar; Respiratory Hypersensitivity; Serotonin; Sheep; Skin Physiological Phenomena; Trachea | 1998 |
Accumulation of granulocytes in the lung and skin of guinea pigs. Inhibition by the anti-H1 antiallergic agent epinastine.
The aim of this study was to investigate whether the antiallergic/H1-antagonistic drug epinastine (WAL 801, Alesion, CAS 108929-04-0) inhibited inflammatory granulocyte infiltration in respiratory or dermal tissue. A late-phase bronchial eosinophilia was induced in sensitized and challenged guinea pigs, and a skin chamber technique was developed for assessing leukotriene-B4 (LTB4) induced transdermal chemotaxis in vivo in this species. Oral epinastine as well as the reference compounds beta-methasone and the LTB4-receptor antagonist 7-[3-(4-acetyl-3-methoxy-2-propylphenoxy) propoxy]-3,4-dihydro-8-propyl-2H-1-benzopyran-2-carboxylic acid (ADCA) demonstrated a dose-dependent inhibition of granulocyte accumulation. The rank order of oral activity was epinastine > betamethasone > ADCA for bronchial eosinophilia and betamethasone > epinastine = ADCA for transdermal chemotaxis. These animal studies suggest a non-antihistamine activity of epinastine which may contribute to its clinical efficacy as an antiallergic drug. Topics: Animals; Betamethasone; Bronchi; Chemotaxis, Leukocyte; Dibenzazepines; Dose-Response Relationship, Drug; Female; Granulocytes; Guinea Pigs; Histamine H1 Antagonists; Imidazoles; Leukotriene B4; Lung; Male; Passive Cutaneous Anaphylaxis; Pulmonary Eosinophilia; Skin | 1994 |