Effect of an Atypical Adrenergic β_3-Agonist, GS-332 : Sodium (2R) [3- [3-[2-(3 Chlorophenyl)-2-Hydroxyethylamino] Cyclohexyl] Phenoxy] Acetate, on Urinary Bladder Function in Rats

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概要

• 論文の詳細を見る

• We have developed an atypical adrenergic β_3-agonist, GS-332: Sodium (2R)- [3-[3-[2-(3-Chlorophenyl)-2-hydroxyethylamino] cyclohexyl] phenoxy] acetate, which has an unique structure compared to other β_3-agonists. In vitro study, we compared effects of GS-332 on rat urinary bladder muscle strip contractility with those of clenbuterol hydrochloride (clenbuterol), an adrenergic β_2-agonist. GS-332 relaxed isolated rat urinary bladder strips in a concentration dependent manner with 50% effective concentration (EC_<50>) of 15.7 nM, and the relaxant activity of GS-332 was as potent as that of clenbuterol(EC_<50> ; 30.8 nM). The concentration-response curve of GS-332 on isolated rat urinary bladder was competed by a specific β_3-antagonist, SR59230A in a concentration-dependent manner, in which Schild slope was 1.1 and pA_2 value of SR5923OA was 7.1. In vivo study, cystometory investigated in anesthetized rats demonstrated that GS-332 was more potent in increasing the urinary storage volume than clenbuterol and less potent in inhibiting the contractile force of urinary bladder at micturition reflex than clenbuterol. These data demonstrate that GS-332, a new adrenergic β_3-agonist, may be more useful to maintain continence than clenbuterol, an adrenergic β_2-adrenergic agonist.

• 日本平滑筋学会の論文

著者

• MORITA Takashi

  Department of Biochemistry, Meiji Pharmaceutical University

• Iizuka H

  Mitsubishitokyo Seiyaku Chiba Jpn

• KONDO Shun

  Department of Urology, Dokkyo University School of Medicine, Tochigi

• Kondo S

  Dokkyo Univ. School Of Medicine Tochigi Jpn

• Kondo Shun

  Department Of Urology Dokkyo University School Of Medicine

• IIZUMI Hiroyuki

  Kazusa research laboratories, Tokyo Tanabe Co., Ltd.

• OSAKA Yoko

  Kazusa research laboratories, Tokyo Tanabe Co., Ltd.

• Osaka Yoko

  Kazusa Research Laboratories Tokyo Tanabe Co. Ltd.

• Morita Takashi

  シルバーリハビリテーション協会

• Morita Takashi

  Department Of Biochemistry Meiji College Of Pharmacy

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