Agents for the Treatment of Overactive Detrusor. IX. Synthesis and Pharmacological Properties of Metabolites of N-tert-Butyl-4,4-diphenyl-2-cyclopentenylamine (FK584) in Human Urine

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概要

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• We synthesized the racemates of five presumed metabolites (1b-f) of (S)-(-)-N-tert-butyl-4,4-diphenyl-2-cyclopentenylamine hydrochloride (FK584,S(-)-1a), a novel agent for the treatment of overactive detrusor syndrome, in order to confirm the structures of the metabolites and also to evaluate thier inhibitory activity against detrusor contraction. (±)-N-tert-Butyl-4-(4-hydroxyphenyl)- and 4-(4-hydroxy-3-methoxyphenyl)-4-phenyl-2-cyclopenetenyl-amines (1b-e) were synthesized via 5-(4-methoxyphenyl)- and 5-(4-benzyloxy-3-methoxyphenyl)-5-phenyl-2-cyclopenten-1-one (9g, h), respectively. Compounds 1b-f prepared in this study were identical with the metabolites in human urine in gas chromatography-mass specrometry and analytical HPLC. The inhibitory activity of compounds 1b-f against detrusor contraction in vitro induced by electrical field stimulation in guinea-pigs was less potent than that of FK584.

• 公益社団法人日本薬学会の論文
• 1996-06-15

著者

• Kinoshita T

  Exploratory Research Laboratoeis Fujisawa Pharmaceutical Co. Ltd.

• 寺井 孝雄

  New Drug Research Laboratories Fujisawa Pharmaceutical Co., Ltd.,

• Tsubaki K

  Institute For Chemical Research Kyoto University

• Terai T

  New Drug Research Laboratories Fujisawa Pharmaceutical Co. Ltd.

• TANIGUCHI Kiyoshi

  New Drug Research Laboratories, Fujisawa Pharmaceutical Co., Ltd.,

• MIYAO Yasuhiro

  Pharmaceutical and Pharmacokinetic Research Laboratories, Fujisawa Pharmaceutical Co., Ltd.,

• YAMANO Katsuhiro

  Pharmaceutical and Pharmacokinetic Research Laboratories, Fujisawa Pharmaceutical Co., Ltd.,

• YAMAMOTO Takao

  Pharmacological Research Laboratories, Fujisawa Pharmaceutical Co., Ltd.,

• TERAI Takao

  New Drug Research Laboratories, Fujisawa Pharmaceutical Co., Ltd.,

• KUSUNOKI Takahiro

  New Drug Research Laboratories, Fujisawa Pharmaceutical Co., Ltd.,

• TSUBAKI Kazunori

  New Drug Research Laboratories, Fujisawa Pharmaceutical Co., Ltd.,

• SHIOKAWA Youichi

  New Drug Research Laboratories, Fujisawa Pharmaceutical Co., Ltd.,

• 嶽 一彦

  New Drug Research Laboratories Fujisawa Pharmaceutical Co. Ltd.

• Miyao Yasuhiro

  Pharmaceutical And Pharmacokinetic Research Laboratories Fujisawa Pharmaceutical Co. Ltd.

• Yamamoto T

  Pharmacological Research Laboratories Fujisawa Pharmaceutical Co. Ltd.

• Shiokawa Y

  Medicinal Chemistry Research Laboratories Fujisawa Pharmaceutical Co. Ltd.

• Yamano Katsuhiro

  Pharmaceutical And Pharmacokinetic Research Laboratories Fujisawa Pharmaceutical Co. Ltd.

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