Abstract
The effects of a newly synthesized PAF antagonist E6123, (S)-(+)-6-(2-chlorophenyl)-3-cyclopropanecarbonyl-8, 11-dimethyl-2,3,4,5-tetrahydro-8H-pyrido [4′,3′:4,5]thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepine, on in vivo inhaled PAF-induced pulmonary changes were investigated. E6123 inihibited PAF inhalation-induced bornchoconstriction in guinea pigs with an ED 50 value (p.o) of 1.3 μg/kg which was lower than those of other PAF-antagonists such as WEB2347 (ED 50 = 26 μg/kg) and Y-24180 (ED 50 = 12 μg/kg). E6123 significantly inhibited PAF inhalation-induec eosinophil infiltraton into the bronchiole and trachea, and bronchial hyperreactivity in guinea pigs after oral administration at 1 and 10 μg/kg, respectively. E6123 inhibited the PAF-induced incrased intracellular free calcium ion concentration ([Ca 2+]i) in guinea pig eosinophils with an IC 5 value of 14 concentration ([Ca 2+]) in guinea pig eosinophils with an IC 50 value of 14 nM. The present results suggest that E6123 may be beneficial for the treatment of asthma, in which PAF is assumed to be involved.
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