Involvement of .BETA.3-Adrenoceptor in the Relaxation Response in Guinea Pig Taenia Caecum.
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概要
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β-Adrenoceptors in the guinea pig taenia caecum were investigated by measuring relaxation responses to agonists and by a radioligand binding assay using [<SUP>3</SUP>H]CGP 12177. The rightward shift of the isoprenaline concentration-response curve was observed by butoxamine, a β<SUB>2</SUB>-selective antagonist, and the pA<SUB>2</SUB> value for butoxamine was 6.46. In control preparations, catecholamines caused relaxation with the following rank order of potency: isoprenaline > adrenaline > noradrenaline. However, in the presence of 10<SUP>-6</SUP> M phentolamine, 3 × 10<SUP>-4</SUP> M atenolol and 10<SUP>-4</SUP> M butoxamine, the rank order of potency of the agonists was: isoprenaline > noradrenaline > adrenaline. CGP 12177 caused graded relaxation of the guinea pig taenia caecum, and this response was not influenced by 10<SUP>-6</SUP> M phentolamine, 3 × 10<SUP>-4</SUP> M atenolol, 10<SUP>-4</SUP> M butoxamine or 10<SUP>-6</SUP> M propranolol. The Scatchard plot of the specific [<SUP>3</SUP>H]CGP 12177 binding to microsomal fractions from the guinea pig taenia caecum showed two affinity sites of the receptor: high affinity (K<SUB>D</SUB>=0.64 nM) and low affinity (K<SUB>D</SUB>=142.21 nM) sites. The pK<SUB>D</SUB> value of the high affinity site of [<SUP>3</SUP>H]-CGP 12177 was in agreement with its pA<SUB>2</SUB> value, and that of the low affinity site was in agreement with its pD<SUB>2</SUB> value. These results suggest that isoprenaline-, noradrenaline- and adrenaline-induced relaxations of the guinea pig taenia caecum predominantly involve β<SUB>2</SUB>- and β<SUB>3</SUB>-adrenoceptors, whereas CGP 12177-induced relaxation is mediated solely through β<SUB>3</SUB>-adrenoceptors.
- 公益社団法人 日本薬理学会の論文
著者
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Koike Katsuo
Department Of Chemical Pharmacology Toho University Faculty Of Pharmaceutical Sciences
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Takayanagi Issei
Department Of Chemical Pharmacology Faculty Of Pharmaceutical Sciences University Of Tokyo:(correspo
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Horinouchi Takahiro
Department Of Cellular Pharmacology Graduate School Of Medicine Hokkaido University
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Muramatsu Midori
Department of Chemical Pharmacology, Toho University School of Pharmaceutical Sciences
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Ohki Shin-ichi
Department of Chemical Pharmacology, Toho University School of Pharmaceutical Sciences
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