Muscarinic Receptor Binding of the Novel Radioligand, [3H]Imidafenacin in the Human Bladder and Parotid Gland

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概要

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• The aim of the current study was to demonstrate highly specific and direct binding activity of tritium ([3H])-labeled imidafenacin for labeling muscarinic receptors in human bladder and parotid gland. Specific binding of [3H]imidafenacin in human tissues was saturable, reversible, and of high affinity. The Kd value for specific [3H]imidafenacin binding in the human bladder was approximately 3 times higher than that in the parotid gland. Unlabeled imidafenacin as well as the clinically used antimuscarinic agents, oxybutynin, tolterodine, and solifenacin, competed with [3H]imidafenacin for binding sites in the human bladder and parotid gland in a concentration-dependent manner, which indicated pharmacological specificity of [3H]imidafenacin binding sites. The Ki for imidafenacin in the human bladder approximately corresponded to pharmacological potency for the competitive blockade of carbachol-induced contractions of bladder, indicating a close correlation between binding affinity of imidafenacin to bladder muscarinic receptors and its pharmacological effects in the bladder. In conclusion, the current study is the first to provide direct evidence to demonstrate that imidafenacin bound muscarinic receptors in the human bladder, supporting its clinical relevance as a therapeutic agent for overactive bladder. [3H]Imidafenacin may also be a useful radioligand for labeling the M3 subtype of muscarinic receptors with higher selectivity than other radioligands.

著者

• Masuyama Keisuke

  Department Of Otolaryngology-head And Neck Surgery Interdisciplinary Graduate School Of Medicine And

• Yamada Shizuo

  Department Of Biophamacy School Of Pharmaceutical Sciences University Of Shizuoka

• Araki Isao

  Department Of Urology University Of Yamanashi Faculty Of Medicine

• Ito Yoshihiko

  Department Of Mathematics Faculty Of Education Kumamoto University

• Ozono Seiichiro

  Department Of Hamamatsu University School Of Medicine

• Takeda Masayuki

  Department Of Biochemistry And Engineering Faculty Of Engineering Tohoku University

• Yoshida Akira

  Department Of Agricultural Chemistry Nagoya University

• Otsuka Atsushi

  Department Of Dermatology Kyoto University

• Masuyama Keisuke

  Department of Urology and Otolaryngology, School of Medicine, University of Yamanashi, Japan

• Kuraoka Shiori

  Department of Pharmacokinetics and Pharmacodynamics, School of Pharmaceutical Sciences, University of Shizuoka, Japan

• Okura Takashi

  Laboratory of Drug Disposition & Pharmacokinetics, Faculty of PharmaScience, Teikyo University, Japan

• Deguchi Yoshiharu

  Laboratory of Drug Disposition & Pharmacokinetics, Faculty of PharmaScience, Teikyo University, Japan

• Okura Takashi

  Laboratory of Drug Disposition & Pharmacokinetics, Faculty of PharmaScience, Teikyo University, Japan

• Deguchi Yoshiharu

  Laboratory of Drug Disposition & Pharmacokinetics, Faculty of PharmaScience, Teikyo University, Japan

• Araki Isao

  Department of Urology, Shiga University of Medical Sciences, Japan

• Yoshida Akira

  Department of Pharmacokinetics and Pharmacodynamics, School of Pharmaceutical Sciences, University of Shizuoka, Japan

• Ozono Seiichiro

  Department of Urology, Hamamatsu University School of Medicine, Japan

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