Pharmacological identification of β-adrenoceptor subtypes mediating isoprenaline-induced relaxation of guinea pig colonic longitudinal smooth muscle
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- Chino Daisuke
- Department of Chemical Pharmacology, Faculty of Pharmaceutical Sciences, Toho University, 2-2-1 Miyama, Funabashi-City, Chiba 274-8510, Japan Department of Pharmacotherapy, Faculty of Pharmaceutical Sciences, Nihon Pharmaceutical University, 10281 Komuro, Ina-machi, Kita-Adachi-gun, Saitama 362-0806, Japan
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- Sone Tomoyo
- Department of Chemical Pharmacology, Faculty of Pharmaceutical Sciences, Toho University, 2-2-1 Miyama, Funabashi-City, Chiba 274-8510, Japan
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- Yamazaki Kumi
- Department of Chemical Pharmacology, Faculty of Pharmaceutical Sciences, Toho University, 2-2-1 Miyama, Funabashi-City, Chiba 274-8510, Japan
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- Tsuruoka Yuri
- Department of Chemical Pharmacology, Faculty of Pharmaceutical Sciences, Toho University, 2-2-1 Miyama, Funabashi-City, Chiba 274-8510, Japan
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- Yamagishi Risa
- Department of Chemical Pharmacology, Faculty of Pharmaceutical Sciences, Toho University, 2-2-1 Miyama, Funabashi-City, Chiba 274-8510, Japan
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- Shiina Shunsuke
- Department of Chemical Pharmacology, Faculty of Pharmaceutical Sciences, Toho University, 2-2-1 Miyama, Funabashi-City, Chiba 274-8510, Japan
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- Obara Keisuke
- Department of Chemical Pharmacology, Faculty of Pharmaceutical Sciences, Toho University, 2-2-1 Miyama, Funabashi-City, Chiba 274-8510, Japan
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- Yamaki Fumiko
- Department of Chemical Pharmacology, Faculty of Pharmaceutical Sciences, Toho University, 2-2-1 Miyama, Funabashi-City, Chiba 274-8510, Japan
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- Higai Koji
- Laboratory of Medical Biochemistry, Faculty of Pharmaceutical Sciences, Toho University, 2-2-1 Miyama, Funabashi-City, Chiba 274-8510, Japan
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- Tanaka Yoshio
- Department of Chemical Pharmacology, Faculty of Pharmaceutical Sciences, Toho University, 2-2-1 Miyama, Funabashi-City, Chiba 274-8510, Japan
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<p>Object We aimed to identify the β-adrenoceptor (β-AR) subtypes involved in isoprenaline-induced relaxation of guinea pig colonic longitudinal smooth muscle using pharmacological and biochemical approaches. Methods Longitudinal smooth muscle was prepared from the male guinea pig ascending colon and contracted with histamine prior to comparing the relaxant responses to three catecholamines (isoprenaline, adrenaline, and noradrenaline). The inhibitory effects of subtype-selective β-AR antagonists on isoprenaline-induced relaxation were then investigated. Results The relaxant potencies of the catecholamines were ranked as: isoprenaline > noradrenaline ≈ adrenaline, whereas the rank order was isoprenaline > noradrenaline > adrenaline in the presence of propranolol (a non-selective β-AR antagonist; 3 × 10−7 M). Atenolol (a selective β1-AR antagonist; 3 × 10−7–10−6 M) acted as a competitive antagonist of isoprenaline-induced relaxation, and the pA2 value was calculated to be 6.49 (95% confidence interval: 6.34–6.83). The relaxation to isoprenaline was not affected by ICI-118,551 (a selective β2-AR antagonist) at 10−9–10−8 M, but was competitively antagonized by 10−7–3 × 10−7 M, with a pA2 value of 7.41 (95% confidence interval: 7.18–8.02). In the presence of propranolol (3 × 10−7 M), the relaxant effect of isoprenaline was competitively antagonized by bupranolol (a non-selective β-AR antagonist), with a pA2 value of 5.90 (95% confidence interval: 5.73–6.35). Conclusion These findings indicated that the β-AR subtypes involved in isoprenaline-induced relaxation of colonic longitudinal guinea pig muscles are β1-AR and β3-AR.</p>
収録刊行物
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- Ｊｏｕｒｎａｌ ｏｆ Ｓｍｏｏｔｈ Ｍｕｓｃｌｅ Ｒｅｓｅａｒｃｈ
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Ｊｏｕｒｎａｌ ｏｆ Ｓｍｏｏｔｈ Ｍｕｓｃｌｅ Ｒｅｓｅａｒｃｈ 54 (0), 13-27, 2018
日本平滑筋学会