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

C. Kamei, Yukio Sugimoto, S. Nakamura, C. Zhong

Research output: Contribution to journalArticle

15 Citations (Scopus)

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 languageEnglish
Pages (from-to)1005-1008
Number of pages4
JournalArzneimittel-Forschung/Drug Research
Volume45
Issue number9
Publication statusPublished - 1995

Fingerprint

Allergic Conjunctivitis
Rats
Guinea Pigs
Ketotifen
Conjunctivitis
Histamine
Antigens
Topical Administration
Coloring Agents
Oral Administration
Perfusion
Olopatadine Hydrochloride
Allergic Rhinitis
Nasal Cavity
Rhinitis

Keywords

  • (Z)-11-[3-(dimethylamino)propylidene]-6,11-dihydrodibenz[b ,e]oxepin-2-acetic acid hydrochloride
  • antiallergic drugs
  • CAS 140462-76-6
  • CAS 34580-14-8
  • ketotifen
  • KW-4679, pharmacology
  • olopatadine

ASJC Scopus subject areas

  • Chemistry(all)
  • Organic Chemistry
  • Drug Discovery
  • Pharmacology

Cite this

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title = "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",
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.",
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T1 - 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

AU - Kamei, C.

AU - Sugimoto, Yukio

AU - Nakamura, S.

AU - Zhong, C.

PY - 1995

Y1 - 1995

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