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.
| Original language | English |
|---|---|
| Pages (from-to) | 1005-1008 |
| Number of pages | 4 |
| Journal | Arzneimittel-Forschung/Drug Research |
| Volume | 45 |
| Issue number | 9 |
| Publication status | Published - Jan 1 1995 |
Keywords
- (Z)-11-[3-(dimethylamino)propylidene]-6,11-dihydrodibenz[b ,e]oxepin-2-acetic acid hydrochloride
- CAS 140462-76-6
- CAS 34580-14-8
- KW-4679, pharmacology
- antiallergic drugs
- ketotifen
- olopatadine
ASJC Scopus subject areas
- Drug Discovery