Effect of (Z)-11-[3-(dimethylamino) propylidene]-6,11-dihydrodibenz[b,e]oxepin-2-acetic acid hydrochloride on experimental allergic conjunctivitis and rhinitis in rats and guinea pigs.
The effect of KW-4679 (Z)-11-[3-(dimethylamino) propylidene]-6,11-dihydrodibenz [b,e] oxepin-2-acetic acid hydrochloride, CAS 140462-76-6; proposed INN: olopatadine) on experimental conjunctivitis and rhinitis was studied in comparison with that of ketotifen (CAS 34580-14-8) using guinea pigs and rats, respectively. KW-4679 was effective in inhibiting the antigen- and histamine-induced conjunctivitis by both oral and topical administrations. These effects of KW-4679 were somewhat more potent than those of ketotifen. KW-4679 as well as ketotifen was more effective in inhibiting the histamine-induced conjunctivitis than that seen in antigen-induced conjunctivitis when they were given topically. KW-4679 inhibited the increased dye leakage into the nasal cavity induced not only by antigen in actively sensitized rats but also by histamine perfusion in non-sensitized rats by oral and topical administrations. Similar to ketotifen, the effect of KW-4679 on histamine-induced increase in dye leakage was almost same as that induced by antigen. The potency of KW-4679 was higher than that of ketotifen in the increased dye leakage induced by both antigen and histamine perfusion.
D000284:Administration, Oral; D000287:Administration, Topical; D000485:Allergens / Q000494:pharmacology; D000818:Animals; D018926:Anti-Allergic Agents / Q000008:administration & dosage / Q000627:therapeutic use*; D001200:Ascaris; D003233:Conjunctivitis, Allergic / Q000188:drug therapy* / Q000276:immunology; D003990:Dibenzoxepins / Q000008:administration & dosage / Q000627:therapeutic use*; D006168:Guinea Pigs; D006632:Histamine / Q000494:pharmacology; D008297:Male; D000069605:Olopatadine Hydrochloride; D051381:Rats; D017208:Rats, Wistar; D006255:Rhinitis, Allergic, Seasonal / Q000188:drug therapy* / Q000276:immunology
D000485:Allergens; D018926:Anti-Allergic Agents; D003990:Dibenzoxepins; D000069605:Olopatadine Hydrochloride; D006632:Histamine