Effect of apafant on bronchial hyperresponsiveness and down-regulation of β-adrenoceptors induced by endotoxin in guinea pigs

Yukio Sugimoto, Takuma Mihara, Tsuyoshi Hayakawa, Yukinobu Nakayama, Hisako Kishida, Chiaki Kamei

Research output: Contribution to journalArticle

3 Citations (Scopus)

Abstract

Intraperitoneal injection of endotoxin resulted in bronchial hyperreactivity to histamine in guinea pigs. In addition, endotoxin (lipopolysaccharide, LPS) caused a decrease in the relaxation of the lung parenchymal strips induced by the β-adrenoceptor agonist, isoproterenol (isoprenaline), and a reduction in the number of β-adrenergic binding sites in the lung membrane preparation in guinea pigs. Apafant (CAS 105219-56-5, WEB 2086) was effective in the prevention of endotoxin-induced changes, i.e., bronchial hyperreactivity to histamine, a decrease in the relaxation of lung parenchymal strips induced by isoproterenol and a reduction in the number of β-adrenergic binding sites in the lung membrane preparation in guinea pigs. Ketotifen and ozagrel also prevented the bronchial hyperresponsiveness and endotoxin-induced deterioration of the β-adrenergic system. No remarkable effect was observed with cromolyn sodium and salbutamol in the bronchial hyperreactivity to histamine induced by endotoxin in guinea pigs. Cromolyn sodium also caused no influence on the down-regulation of β-adrenoceptors.

Original languageEnglish
Pages (from-to)837-841
Number of pages5
JournalArzneimittel-Forschung/Drug Research
Volume47
Issue number7
Publication statusPublished - 1997

Fingerprint

WEB 2086
Endotoxins
Adrenergic Receptors
Guinea Pigs
Bronchial Hyperreactivity
Down-Regulation
Isoproterenol
Adrenergic Agents
Histamine
Cromolyn Sodium
Lung
Binding Sites
Ketotifen
Membranes
Albuterol
Intraperitoneal Injections
Deterioration
Lipopolysaccharides

Keywords

  • β-Adrenoceptors, down-regulation
  • Apafant
  • Bronchial hyperresponsiveness
  • CAS 105219-56-5
  • WEB 2086, guinea pig, in vivo studies

ASJC Scopus subject areas

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

Cite this

Effect of apafant on bronchial hyperresponsiveness and down-regulation of β-adrenoceptors induced by endotoxin in guinea pigs. / Sugimoto, Yukio; Mihara, Takuma; Hayakawa, Tsuyoshi; Nakayama, Yukinobu; Kishida, Hisako; Kamei, Chiaki.

In: Arzneimittel-Forschung/Drug Research, Vol. 47, No. 7, 1997, p. 837-841.

Research output: Contribution to journalArticle

Sugimoto, Yukio ; Mihara, Takuma ; Hayakawa, Tsuyoshi ; Nakayama, Yukinobu ; Kishida, Hisako ; Kamei, Chiaki. / Effect of apafant on bronchial hyperresponsiveness and down-regulation of β-adrenoceptors induced by endotoxin in guinea pigs. In: Arzneimittel-Forschung/Drug Research. 1997 ; Vol. 47, No. 7. pp. 837-841.
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