Structure-Activity Relationship Studies of (±)- Terbutaline and (±)-Fenoterol on β_3-Adrenoceptors in the Guinea Pig Gastric Fundus
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概要
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(±)-Terbutaline and (±)-fenoterol are both arylethanolamine analogs that have tertbutyl and aryliso-propyl substituents respectively at the α position on the nitrogen of the ethanolamine side chain. In the present study, we have investigated the structure-activity relationships of (±)-terbutaline and (±)-fenoterol as β_3-adrenoceptor agonists in the guinea pig gastric fundus. (±)-Terbutaline and (±)-fenoterol induced concentration-dependent relaxation of the precontracted gastric fundus with pD_2 values of 4.45±0.10 and 5.90±0.09 and intrinsic activities of 1.00±0.03 and 0.99±0.01 respectively. The combination of the selective β_1-adrenoceptor antagonist (±)-atenolol (100 μM), and the selective β_2-adrenoceptor antagonist (±)-butoxamine (100 μM), produced a 2 and 6 fold rightward shift of the concentration-response curves for (±)-terbutaline and (±)-fenoterol respectively, without depressing the maximal responses. The order of potency of these agonists was (pD_2 value) : (±)-fenoterol (5.09±0.10)>(±)-terbutaline (4.13±0.08). In the presence of (±)-atenolol and (±)-butoxamine, however, the non-selective β_1,β_2- and β_3-adrenoceptor antagonist (±)-bupranolol caused a concentration-dependent rightward shift of the concentration-response curves for (±)-terbutaline and (±)-fenoterol. Schild plot analyses of the effects of (±)-bupranolol against these agonists gave pA_2 values of 6.21±0.07 ((±)-terbutaline) and 6.37±0.06 ((±)-fenoterol) respectively, and the slopes of the Schild plot were not significantly different from unity (p>0.05). These results suggest that the relaxant responses to (±)-terbutaline and (±)-fenoterol are mainly mediated through β_3-adrenoceptors in the guinea pig gastric fundus. The β_3-adrenoceptor agonist potencies of arylethanolamine analogs depend on the size of the end of the alkylamine side chain.
- 日本平滑筋学会の論文
著者
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KOIKE Katsuo
Department of Chemical Pharmacology, Toho University School of Pharmaceutical Sciences
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Koike Katsuo
Department Of Chemical Pharmacology Toho University School Of Pharmaceutical Sciences
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Koike Katsuo
Department Of Chemical Pharmacology Toho University Faculty Of Pharmaceutical Sciences
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Nakagawa Yoshiko
Department Of Chemical Pharmacology Toho University School Of Pharmaceutical Sciences
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Horinouchi Takahiro
Department Of Chemical Pharmacology Toho University School Of Pharmaceutical Sciences
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WAKABAYASHI Makiko
Department of Chemical Pharmacology, Toho University, School of Pharmaceutical Sciences
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Wakabayashi Makiko
Department Of Chemical Pharmacology Toho University School Of Pharmaceutical Sciences
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Horinouchi Takahiro
Department Of Cellular Pharmacology Hokkaido University Graduate School Of Medicine
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Horinouchi Takahiro
Department Of Cellular Pharmacology Graduate School Of Medicine Hokkaido University
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HORINOUCHI Takahiro
Department of Chemical Pharmacology, Toho University, School of Pharmaceutical Sciences
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