Pharmacological Characterization of a New Antimuscarinic Agent, Solifenacin Succinate, in Comparison with Other Antimuscarinic Agents(Pharmacology)

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概要

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• Solifenacin succinate [YM905; (3R)-1-azabicyclo [2.2.2] oct-3-yl(1S)-1-phenyl-3,4-dihydroisoquinoline-2(1H)-carboxylate monosuccinate] is a new muscarinic receptor antagonist developed for the treatment of overactive bladder. The aim of the present study was to evaluate the antimuscarinic properties of solifenacin and to compare the results with those obtained for tolterodine, oxybutynin, darifenacin, propiverine and atropine. In radioligand receptor binding assay, K_i values of solifenacin for human muscarinic M_1, M_2, M_3, M_4 and M_5 receptors were 26, 170, 12, 110 and 31 nM, respectively. In isolated rat urinary bladder, solifenacin competitively antagonized carbachol-induced contractions, with a pA_2 value of 7.44±0.09. In these in vitro studies, the antimuscarinic action of solifenacin was more potent than that of propiverine and less potent than those of tolterodine, oxybutynin, darifenacin and atropine. In anesthetized rats, solifenacin and oxybutynin increased the maximum bladder capacity in a dose-dependent manner and also decreased the maximum intravesical pressure. The dosages required to produce a 30% increase in maximum bladder capacity (ED_<30> values) of solifenacin and oxybutynin were 0.35 and 0.30mg/kg i.v., respectively, indicating approximately equal efficacies. These results support the fact that solifenacin, similarly to currently used antimuscarinic agents, is an effective agent in the treatment of overactive bladder symptoms such as urinary frequency and urge incontinence.

• 2007-01-01

著者

• SASAMATA Masao

  Applied Pharmacology Research Laboratories, Drug Discovery Research, Astellas Pharma Inc.

• MIYATA Keiji

  Applied Pharmacology Research Laboratories, Drug Discovery Research, Astellas Pharma Inc.

• Miyata Keiji

  Applied Pharmacology Res. Laboratories Drug Discovery Res. Astellas Pharma Inc. Jpn

• Miyata Keiji

  Pharmacology Laboratories Institute For Drug Discovery Research Yamanouchi Pharmaceutical Co. Ltd.

• Sasamata Masao

  Applied Pharmacology Research Laboratories Drug Discovery Research Astellas Pharma Inc.

• Sasamata Masao

  Pharmacology Research Laboratories Drug Discovery Research Astellas Pharma Inc.

• Suzuki Masanori

  Pharmacology Research Labs. Drug Discovery Research Astellas Pharma Inc.

• OKUTSU Hiroko

  Pharmacology Research Labs., Drug Discovery Research, Astellas Pharma Inc.

• NOGUCHI Yukiko

  Pharmacology Research Labs., Drug Discovery Research, Astellas Pharma Inc.

• OHTAKE Akiyoshi

  Pharmacology Research Labs., Drug Discovery Research, Astellas Pharma Inc.

• SATO Shuichi

  Pharmacology Research Labs., Drug Discovery Research, Astellas Pharma Inc.

• SAITOH Chikashi

  Pharmacology Research Labs., Drug Discovery Research, Astellas Pharma Inc.

• YUYAMA Hironori

  Pharmacology Research Labs., Drug Discovery Research, Astellas Pharma Inc.

• UKAI Masashi

  Pharmacology Research Labs., Drug Discovery Research, Astellas Pharma Inc.

• HATANAKA Toshiki

  Pharmacology Research Labs., Drug Discovery Research, Astellas Pharma Inc.

• Ukai Masashi

  Pharmacology Research Labs. Drug Discovery Research Astellas Pharma Inc.

• Okutsu Hiroko

  Pharmacology Research Labs. Drug Discovery Research Astellas Pharma Inc.

• Noguchi Yukiko

  Pharmacology Research Labs. Drug Discovery Research Astellas Pharma Inc.

• Yuyama Hironori

  Pharmacology Research Labs. Drug Discovery Research Astellas Pharma Inc.

• Saitoh Chikashi

  Pharmacology Research Labs. Drug Discovery Research Astellas Pharma Inc.

• Hatanaka Toshiki

  Pharmacology Research Labs. Drug Discovery Research Astellas Pharma Inc.

• Sato Shuichi

  Applied Pharmacology Research Laboratories Drug Discovery Research Astellas Pharma Inc.

• Ohtake Akiyoshi

  Applied Pharmacology Research Laboratories Drug Discovery Research Astellas Pharma Inc.

• Yuyama Hironori

  Pharmacology Research Laboratories, Drug Discovery Research, Astellas Pharma Inc.

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