The Forefront for Novel Therapeutic Agents Based on the Pathophysiology of Lower Urinary Tract Dysfunction: Bladder Selectivity Based on In Vivo Drug–Receptor Binding Characteristics of Antimuscarinic Agents for Treatment of Overactive Bladder
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概要
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We have reviewed the binding of antimuscarinic agents, used to treat urinary dysfunction in patients with overactive bladder, to muscarinic receptors in target and non-target tissues in vivo. Transdermal administration of oxybutynin in rats led to significant binding in the bladder without long-term binding in the submaxillary gland and the abolishment of salivation evoked by oral oxybutynin. Oral solifenacin showed significant and long-lasting binding to muscarinic receptors in mouse tissues expressing the M3 subtype. Oral tolterodine bound more selectively to muscarinic receptors in the bladder than in the submaxillary gland in mice. The muscarinic receptor binding activity of oral darifenacin in mice was shown to be pronounced and long-lasting in the bladder, submaxillary gland, and lung. In vivo quantitative autoradiography using (+)N-[11C]methyl-3-piperidyl benzilate in rats showed significant occupancy of brain muscarinic receptors on intravenous injection of oxybutynin, propiverine, solifenacin, and tolterodine. The estimated in vivo bladder selectivity compared to brain was significantly greater for solifenacin and tolterodine than oxybutynin. Darifenacin occupied few brain muscarinic receptors. Similar findings were also observed with positron emission tomography in conscious rhesus monkeys. The newer generation of antimuscarinic agents may be advantageous in the bladder selectivity after systemic administration.
著者
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YOSHIDA AKIRA
Department of Radiological Sciences, Hiroshima Prefectural College of Health Science
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Yamada Shizuo
Department Of Biophamacy School Of Pharmaceutical Sciences University Of Shizuoka
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Ito Yoshihiko
Department Of Mathematics Faculty Of Education Kumamoto University
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Taki Yuko
Department of Pharmacokinetics, Pharmacodynamics, Global Center of Excellence (COE) and Clinical Pha
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Fujino Tomomi
Department of Pharmacokinetics and Pharmacodynamics and Global Center of Excellence (COE) Program, S
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Maruyama Shuji
Department of Pharmacokinetics and Pharmacodynamics and Global Center of Excellence (COE) Program, S
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Yoshida Akira
Department Of Cardiology Mitsubishi Kyoto Hospital
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Yoshida Akira
Department Of Breast And Endocrine Surgery Kanagawa Cancer Center
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Yoshida Akira
Department Of Agricultural Chemistry Nagoya University
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Yoshida Akira
Department Of Pharmacokinetics And Pharmacodynamics And Global Center Of Excellence (coe) Program Sc
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Fujino Tomomi
Department Of Pharmacokinetics And Pharmacodynamics And Global Center Of Excellence (coe) Program Sc
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Taki Yuko
Department Of Pharmacokinetics And Pharmacodynamics And Global Center Of Excellence (coe) Program Sc
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Maruyama Shuji
Department Of Pharmacokinetics And Pharmacodynamics And Global Center Of Excellence (coe) Program School Of Pharmaceutical Sciences University Of Shizuoka
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Ito Yoshihiko
Department of Pharmacokinetics and Pharmacodynamics and Global Center of Excellence (COE) Program, School of Pharmaceutical Sciences, University of Shizuoka, Japan
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Taki Yuko
Department of Pharmacokinetics and Pharmacodynamics and Global Center of Excellence (COE) Program, School of Pharmaceutical Sciences, University of Shizuoka, Japan
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Maruyama Shuji
Department of Pharmacokinetics and Pharmacodynamics and Global Center of Excellence (COE) Program, School of Pharmaceutical Sciences, University of Shizuoka, Japan
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Fujino Tomomi
Department of Pharmacokinetics and Pharmacodynamics and Global Center of Excellence (COE) Program, School of Pharmaceutical Sciences, University of Shizuoka, Japan
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Yoshida Akira
Department of Pharmacokinetics and Pharmacodynamics and Global Center of Excellence (COE) Program, School of Pharmaceutical Sciences, University of Shizuoka, Japan
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