TY - JOUR
T1 - Effect of apafant on bronchial hyperresponsiveness and down-regulation of β-adrenoceptors induced by endotoxin in guinea pigs
AU - Sugimoto, Yukio
AU - Mihara, Takuma
AU - Hayakawa, Tsuyoshi
AU - Nakayama, Yukinobu
AU - Kishida, Hisako
AU - Kamei, Chiaki
PY - 1997/8/12
Y1 - 1997/8/12
N2 - 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.
AB - 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.
KW - Apafant
KW - Bronchial hyperresponsiveness
KW - CAS 105219-56-5
KW - WEB 2086, guinea pig, in vivo studies
KW - β-Adrenoceptors, down-regulation
UR - http://www.scopus.com/inward/record.url?scp=0030748763&partnerID=8YFLogxK
UR - http://www.scopus.com/inward/citedby.url?scp=0030748763&partnerID=8YFLogxK
M3 - Article
C2 - 9272241
AN - SCOPUS:0030748763
SN - 2194-9379
VL - 47
SP - 837
EP - 841
JO - Drug Research
JF - Drug Research
IS - 7
ER -