A Trial for Kinetic Evaluation of the Antagonistic Potency of Several β-Antagonists on Presynaptic β-Adrenoceptors
スポンサーリンク
概要
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The antagonistic potency, pA<SUB>2</SUB>, of several non-selective β-antagonists on presynaptic β-adrenoceptors was evaluated using a parallel line assay and MacKays equation against isoproterenol-induced increases in <SUP>3</SUP>H release in isolated guinea-pig pulmonary arteries preloaded with <SUP>3</SUP>H-norepinephrine. Cumulatively applied isoproterenol at 10<SUP>-9</SUP> M, 10<SUP>-8</SUP> M and 10<SUP>-7</SUP> M dose-dependently increased <SUP>3</SUP>H release evoked by transmural field stimulation at 1 Hz. β-Antagonists tested dose-dependently antagonized the isoproterenol-induced increases. The order of pA<SUB>2</SUB> was carteolol (11.23±0.09)>nadolol (9.78±0.05)>pindolol (9.59±0.03)>propranolol (9.26±0.17). Carteolol has the highest pA<SUB>2</SUB> and is a useful tool for clarifying whether or not presynaptic β-adrenoceptors tonically function.
著者
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Amano Hiro
Department Of Pharmacology Yokohama City University School Of Medicine:(present Address)division Of
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Kubo Takao
Department Of Pharmacology Showa College Of Pharmaceutical Sciences
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Kuwahara Misako
Department Of Pharmacology Yokohama City University School Of Medicine
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MISU Yoshimi
Department of Pharmacologv, faculty of Pharmaceutical Scieuces, Kyoto University
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AMANO Hiro
Department of Pharmacology, Yokohama City University School of Medicine
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