Synthesis and Characterization of Orally Active Nonpeptide Vasopressin V_2 Receptor Antagonists
スポンサーリンク
概要
- 論文の詳細を見る
The present study was undertaken to evaluate whether a novel series of 2,6-diaza-5-oxobicyclo[5.4.0]undeca-1(7), 8,10-triene derivatives exhibited antagonistic activity for vasopressin V_1 and V_2 receptors. Most of these compounds were synthesized and showed a high affinity potential for V_2 receptor and low to moderate affinity potential for V_1 receptor. The most potent and V_2-selective compound, N-[4-[2,6-diaza-6-[2-(4-methylpiper-azinyl)-2-oxoethyl]-5-oxobicyclo[5.4.0]undeca-1(7), 8,10-trien-2-yl]-carbonyl]phenyl][2-(4-methylphenyl)phenyl]-formamide (11b), exhibited IC_<50>'s of 2.9 nM for the V_2 receptor and 200 nM for the V_1 receptor, respectively.When administered orally to rat, 11b showed an approximately 18-fold increased urine volume in comparison with control rat.
- 公益社団法人日本薬学会の論文
- 1999-04-15
著者
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TANAKA Hirokazu
Exploratory Research Laboratories, Fujisawa Pharmaceutical Co., Ltd.
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Hemmi K
Exploratory Research Laboratories Fujisawa Pharmaceutical Co. Ltd.
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Hosogai Naomi
Exploratory Research Laboratories Fujisawa Pharmaceutical Co. Ltd.
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Hemmi Keiji
Exploratory Research Laboratories Fujisawa Pharmaceutical Co. Ltd.
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Hemmi Keiji
Exploratory Research Laboratories Fujiawa Pharmaceutical Co. Ltd.
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ZENKOH TATSUYA
Exploratory Research Laboratories, Fujisawa Pharmaceutical Co., Ltd
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Ohkawa Takehiko
Exploratory Research Laboratories Fujisawa Pharmaceutical Co. Ltd.
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Zenkoh Tatsuya
Exploratory Research Laboratories Fujisawa Pharmaceutical Co. Ltd.
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Setoi H
Fujisawa Pharmaceutical Co. Ltd. Osaka Jpn
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TOMITA Masayuki
Exploratory Research Laboratories, Fujisawa Pharmaceutical Co., Ltd.,
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SETOI Hiroyuki
Exploratory Research Laboratories, Fujisawa Pharmaceutical Co., Ltd.,
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Tomita Masayuki
Exploratory Research Laboratories Fujisawa Pharmaceutical Co. Ltd.
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Tanaka Hirokazu
Exploratory Research Laboratories Fujisawa Pharmaceutical Co. Ltd. :(present Address)external Scient
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Tanaka Hirokazu
Exploratory Research Laboratories Fujisawa Pharmaceutical Co. Ltd.
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