Evaluation of β_<1L>-Adrenoceptors in Rabbit Heart by Tissue Segment Binding Assay
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概要
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[3H]-CGP12177 biphasically bound to β-adrenoceptors with high and low affinities in the segments and crude membranes of rabbit left ventricle. The low-affinity sites for [3H]-CGP12177 in the segments was double in density, compared to the density of high-affinity sites. Total abundance of the β-adrenoceptors decreased to approximately 10% upon tissue homogenization, and the proportion of low-affinity sites was the same as that of the high-affinity sites in the membranes. The majority of the high-affinity binding sites of [3H]-CGP12177 in the segments and the membranes were β1H-adrenoceptor, being highly sensitive to propranolol and β1-antagonists (atenolol and ICI-89,406), whereas the low-affinity binding sites showed a β1L-profile (less sensitive to propranolol and β1-, β2-, and β3-antagonists). Furthermore, a part of the β1L-adrenoceptors was insensitive to atenolol, ICI-89,406, and/or isoproterenol. The present binding study clearly shows that β1L-adrenoceptors occur as a distinct phenotype from β1H-adrenoceptors in rabbit ventricle. However, quantitative imbalance between β1H- and β1L-adrenoceptors and divergent ligand–β1L-adrenoceptor interactions suggest a possibility that the β1L-adrenoceptor may not reflect a simple conformational change or allosteric state in the β1-adrenoceptor molecule.
- 2009-07-20
著者
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Miwa Soichi
Department Of Cellular Pharmacology Hokkaido University Graduate School Of Medicine
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MURAMATSU Ikunobu
Division of Pharmacology, Department of Biochemistry and Bioinformative Sciences, School of Medicine
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SUZUKI Fumiko
Division of Pharmacology, Department of Biochemistry and Bioinformative Sciences, School of Medicine
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MORISHIMA Shigeru
Division of Pharmacology, Department of Biochemistry and Bioinformative Sciences, School of Medicine
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Gauthier Chantal
Inserm Umr 915 L'institut Du Thorax
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Suzuki Fumiko
Division Of Pharmacology Department Of Biochemistry And Bioinformative Sciences University Of Fukui
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Muramatsu Ikunobu
Organization For Life Sci. Advancement Programs Univ. Of Fukui Jpn
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Muramatsu Ikunobu
Division Of Pharmacology Department Of Biochemistry And Bioinformative Sciences School Of Medicine U
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Muramatsu Ikunobu
Division Of Pharmacology Department Of Biochemistry And Bioinformative Sciences University Of Fukui
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Suzuki Fumio
Division Of Pharmacology Department Of Biochemistry And Bioinformative Sciences University Of Fukui
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Muramatsu I
Division Of Pharmacology Department Of Biochemistry And Bioinformative Sciences University Of Fukui
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YOSHIKI Hatsumi
Division of Pharmacology, Department of Biochemistry and Bioinformative Sciences, School of Medicine
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NISHIMUNE Atsushi
Division of Pharmacology, Department of Biochemistry and Bioinformative Sciences, School of Medicine
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IKEDA Takeshi
Organization for Life Science Advancement Programs, University of Fukui
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SASAKI Masato
Division of Surgery 2, Department of Surgery, School of Medicine, University of Fukui
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AUDIGANE Leslie
Organization for Life Science Advancement Programs, University of Fukui
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Audigane Leslie
Organization For Life Science Advancement Programs University Of Fukui
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Yoshiki Hatsumi
Division Of Pharmacology Department Of Biochemistry And Bioinformative Sciences School Of Medicine U
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Suzuki Fumiko
Division Of Pharmacology Department Of Biochemistry And Bioinformative Sciences School Of Medicine U
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Miwa Soichi
Division Of Pharmacology Department Of Biochemistry And Bioinformative Sciences School Of Medicine U
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Miwa Soichi
Dep. Of Cellular Pharmacology Hokkaido Univ. Graduate School Of Medicine Jpn
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Nishimune Atsushi
Division Of Pharmacology Department Of Biochemistry And Bioinformative Sciences School Of Medicine U
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Morishima Shigeru
Division Of Pharmacology Department Of Biochemistry And Bioinformative Sciences School Of Medicine U
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