TA-2005,a Novel, Long-Acting, and Selective β_2-Adrenoceptor Agonist : Characterization of Its in Vivo Bronchodilating Action in Guinea Pigs and Cats in Comparison with Other β_2-Agonists

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Relaxant effects of the β_2-selective adrenoceptor agonist TA-2005 on bronchoconstriction in the anesthetized guinea pig and cat were evaluated in comparison with other known β_2-adrenoceptor agonists. The ED_<50> values of intravenously administered TA-2005,procaterol, formoterol, isoproterenol, salbutamol, and salmeterol to inhibit the histamine-induced bronchoconstriction of the guinea pigs were 0.024,0.053,0.056,0.099,0.23,and 2.00μg/kg, respectively, and those in serotonin-challenged cats were 0.019,0.037,0.039,0.042,0.13,and 0.52μg/kg, respectively, in the same increasing order. When guinea pigs were passively sensitized with anti-ovalbumin antiserum, the ED_<50> values of TA-2005,formoterol, procaterol, and isoproterenol to inhibit the antigen-induced bronchoconstriction were 0.09,0.30,0.65,and 7.0μg/kg, i.v., respectively, while those of TA-2005,procaterol, formoterol, and salbutamol in actively sensitized animals were 0.24,0.25,1.40,and 23.0μg/kg. When TA-2005 was administered by inhalation to guinea pigs or by the intraduodenal route to cats, it exhibited a long-lasting inhibitory effect comparable or superior to the effects of salmeterol and formoterol. These data indicate that, among the known β_2-adrenoceptor agonists examined, TA-2005 exerts the most potent bronchodilating effects with a long duration of action in vivo, and its potency ratios to the other reference drugs were greater in antigen-than spasmogen-induced bronchoconstric-tion models.
社団法人日本薬学会の論文
1994-08-15

TA-2005,a Novel, Long-Acting, and Selective β_2-Adrenoceptor Agonist : Characterization of Its in Vivo Bronchodilating Action in Guinea Pigs and Cats in Comparison with Other β_2-Agonists

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