Characterization of .BETA.-Adrenoceptors in Pig Basilar Artery from Functional and Radioligand Binding Studies.
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概要
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β-Adrenoceptors in pig basilar arteries were investigated by measuring the relaxation responses to norepinephrine and by a radioligand binding assay with [<SUP>3</SUP>H]-dihydroalprenolol (DHA). Norepinephrine induced concentration-dependent relaxations. The relaxation responses were independent of the presence of endothelial cells, and they were competitively antagonized by (±)-propranolol, atenolol, butoxamine and ICI 118, 551. Specific [<SUP>3</SUP>H]-DHA binding to β-adrenoceptors was saturable, reversible and high affinity (K<SUB>d</SUB>=1.4 nM), with a B<SUB>max</SUB> of 48.7 fmol/mg protein. Computer analysis of inhibition of [<SUP>3</SUP>H]DHA binding by atenolol, butoxamine and ICI 118, 551 gave a β<SUB>1</SUB>:β<SUB>2</SUB>-adrenoceptor ratio of approximately 65:35. The pA<SUB>2</SUB> values of these antagonists were significantly correlated with the K<SUB>i</SUB> values for β<SUB>1</SUB>-adrenoceptor determined by the radioligand binding assay. The present findings indicate that the relaxation responses to norepinephrine are predominantly mediated through the stimulation of β<SUB>1</SUB>-adrenoceptors on vascular smooth muscle cells in a pig basilar artery.
- 公益社団法人 日本薬理学会の論文
著者
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Miyamoto Atsushi
Department Of Cardiovascular Medicine School Of Medicine Hokkaido University
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Nishio Akira
Department Of Agricultural Chemistry Faculty Of Agriculture Kyushu University
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Ito Ken
Department Of Applied Physics Osaka City University
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Miyamoto Atsushi
Department of Veterinary Pharmacology, Faculty of Agriculture, Kagoshima University,
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Nishio Akira
Department of Veterinary Pharmacology, Faculty of Agriculture, Kagoshima University,
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