VUF-K-8788, a Periphery-Selective Histamine H_1 Antagonist With Anti-pruritic Activities
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概要
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The pharmacological properties of 7-{3-[4-(2-quinolinylmethyl)-1-piperazinyl]-propoxy}-2,3-dihydro-4H-1,4-benzothiazin-3-one (VUF-K-8788) were investigated in vitro and in vivo. VUF-K-8788 inhibited [3H]-mepyramine from binding to the cell membrane of lung parenchyma (Ki value: 5.0 nM) and the histamine-induced contraction of isolated guinea pig ileum (pA2: 9.71) without affecting ileal contractions induced by acetylcholine, serotonin, KCl and BaCl2. The increase of vascular permeabilities induced by histamine and passive cutaneous anaphylaxis (PCA) in guinea pigs were inhibited by VUF-K-8788 in a dose-dependent fashion (ED50: 0.24 and 0.26 mg/kg, p.o., respectively). Moreover, the anti-histaminic effect of VUF-K-8788 was also observed in rats. In experiments on the effects on the central nervous system, VUF-K-8788 at 1 mg/kg, p.o. hardly antagonized the H1 receptor at all in the cerebral cortex of guinea pigs. VUF-K-8788 inhibited the PCA-induced scratching behavior completely without affecting thiopental-induced sleep in mice. These results suggested that VUF-K-8788 would be useful in the treatment of allergic disorders such as atopic dermatitis and eczema.
- 社団法人 日本薬理学会の論文
- 2001-05-01
著者
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INAGAKI Naoki
Department of Pharmacology, Gifu Pharmaceutical University
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NAGAI Hiroichi
Department of Pharmacology, Gifu Pharmaceutical University
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Wada Yasushi
Tokyo Research Laboratories Pharmaceutical Division Kowa Company Ltd
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Takizawa Toshiaki
Tokyo New Drug Research Laboratories Ii Pharmaceutical Division Kowa Company Ltd.
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Takizawa Toshiaki
興和
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Takizawa Toshiaki
岐阜薬科大学 薬理
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MATSUMOTO Jiro
Tokyo New Drug Research Laboratories II, Pharmaceutical Division, Kowa Company Ltd.
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TAKIZAWA Toshiaki
Toko Research Laboratories, Pharmaceutical Division, Kowa Company, Ltd.
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MATSUMOTO Jiro
Toko Research Laboratories, Pharmaceutical Division, Kowa Company, Ltd.
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TOHMA Tsutomu
Toko Research Laboratories, Pharmaceutical Division, Kowa Company, Ltd.
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KANKE Toru
Toko Research Laboratories, Pharmaceutical Division, Kowa Company, Ltd.
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WADA Yasushi
Toko Research Laboratories, Pharmaceutical Division, Kowa Company, Ltd.
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NAGAO Masafumi
Department of Pharmacology, Gifu Pharmaceutical University
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ZHANG Min-Qiang
Leiden/Amsterdam Center for Drug Research, Division of Medicinal Chemistry, Vrije University
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TIMMERMAN Henk
Leiden/Amsterdam Center for Drug Research, Division of Medicinal Chemistry, Vrije University
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Timmerman Henk
Leiden/amsterdam Center For Drug Research Division Of Medicinal Chemistry Vrije University
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Kanke Toru
興和
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Matsumoto Jiro
Tokyo New Drug Research Laboratories Ii Pharmaceutical Division Kowa Company Ltd.
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Nagai Hiroichi
Laboratory Of Pharmacology Department Of Bioactive Molecules Gifu Pharmaceutical University
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Inagaki Naoki
Department Of Electrical And Computer Engineering Nagoya Institute Of Technology
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Nagai Hiroichi
Department Of Clinical Pharmacology Gifu Pharmaceutical University
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Tanaka Hiroyuki
Department Of Pharmacology Gifu Pharmaceutical University
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Inagaki Naoki
Departmen T Of Pharmacology Gifu Pharmaceutical University
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Nagai Hiroichi
Department Of Applied Pharmacology Graduate School Of Medicine And Pharmaceutical Sciences University Of Toyama
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