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

Arzneimittelforschung. 1995 Sep;45(9):1005-8.

Abstract

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.

MeSH terms

  • Administration, Oral
  • Administration, Topical
  • Allergens / pharmacology
  • Animals
  • Anti-Allergic Agents / administration & dosage
  • Anti-Allergic Agents / therapeutic use*
  • Ascaris
  • Conjunctivitis, Allergic / drug therapy*
  • Conjunctivitis, Allergic / immunology
  • Dibenzoxepins / administration & dosage
  • Dibenzoxepins / therapeutic use*
  • Guinea Pigs
  • Histamine / pharmacology
  • Male
  • Olopatadine Hydrochloride
  • Rats
  • Rats, Wistar
  • Rhinitis, Allergic, Seasonal / drug therapy*
  • Rhinitis, Allergic, Seasonal / immunology

Substances

  • Allergens
  • Anti-Allergic Agents
  • Dibenzoxepins
  • Olopatadine Hydrochloride
  • Histamine