Effects of a new antiallergic agent, VUF-K-8788, on experimental asthmatic reactions in guinea pigs.
The effects of 7-[3-[4-(2-quinolinylmethyl)- 1-piperazinyl]propoxy]-2,3-dihydro-4H-1,4- benzothiazin-3-one (VUF-K-8788) on experimental asthmatic reactions in guinea pigs were investigated. VUF-K-8788 inhibited histamine-induced bronchoconstriction at the doses of 0.3 and 1 mg/kg per os (p.o.). VUF-K-8788 inhibited anaphylactic bronchoconstriction at doses between 0.01 and 1 mg/kg in passively sensitized guinea pigs. Terfenadine used as a reference drug also inhibited an antigen-induced bronchoconstriction. VUF-K-8788 at the doses of 0.3 and 1 mg/kg inhibited immediate- and late-phase asthmathic reactions in actively sensitized guinea pigs. Terfenadine inhibited only the immediate phase reaction. Moreover, VUF-K-8788 inhibited the infiltration of eosinophils and macrophages into bronchoalveolar lavage fluid in guinea pigs. These results indicate that VUF-K-8788 may be useful for the treatment of bronchial asthma.
Takizawa
T
T
Department of Pharmacology, Gifu Pharmaceutical University, Gifu, Japan.
Yamada
T
T
Takahashi
Y
Y
Tanaka
H
H
Wada
Y
Y
Nagai
H
H
D000403:Airway Resistance / Q000187:drug effects / Q000502:physiology; D000707:Anaphylaxis / Q000503:physiopathology; D000818:Animals; D018926:Anti-Allergic Agents / Q000627:therapeutic use*; D018927:Anti-Asthmatic Agents / Q000627:therapeutic use*; D000941:Antigens / Q000276:immunology; D001249:Asthma / Q000139:chemically induced / Q000188:drug therapy* / Q000503:physiopathology; D016535:Bronchial Hyperreactivity / Q000188:drug therapy / Q000503:physiopathology; D001992:Bronchoalveolar Lavage Fluid / Q000166:cytology; D004558:Electric Stimulation; D006168:Guinea Pigs; D006632:Histamine / Q000494:pharmacology; D006968:Hypersensitivity, Delayed / Q000188:drug therapy / Q000503:physiopathology; D006969:Hypersensitivity, Immediate / Q000188:drug therapy / Q000503:physiopathology; D007116:Immunization, Passive; D066298:In Vitro Techniques; D017998:Leukotriene D4 / Q000494:pharmacology; D008297:Male; D010879:Piperazines / Q000627:therapeutic use*; D013843:Thiazines / Q000627:therapeutic use*
D018926:Anti-Allergic Agents; D018927:Anti-Asthmatic Agents; D000941:Antigens; D010879:Piperazines; D013843:Thiazines; C121690:VUF-K 8788; D017998:Leukotriene D4; D006632:Histamine