Novel Histamine H_3 Receptor Antagonists : Synthesis and Evaluation of Formamidine and S-Methylisothiourea Derivatives
スポンサーリンク
概要
- 論文の詳細を見る
In order to obtain a new, potent and selective histamine H_3 receptor antagonist, chemical modifications of thioperamide, a well-known H_3 receptor antagonist, were conducted. A new series of compounds has een synthesized by modifying the thiourea and cyclohexyl groups of thioperamide, and tested for H_3 receptor affinity by receptor binding assay using plasma membrane from rat cerebral cortex. The thiourea group of thioperamide was found to be replaceable with a basic moiety such as formamidine or S-methylisothiourea. Replacement of the cyclohexyl group in thioperamide by a 1-adamantyl or an exo-2-norbornyl group increased the affinity for H_3 receptor. Among the compounds synthesized, N-(1-adamantyl)-N', N'-[3-(4(5)-1H-imidazolyl)pentamethylene]formamidine 3f (AQ0145) showed the highest H_3 receptor affinity, having a potent antagonistic activity. This compound was at least 1000-fold more active towards H_3 than towards H_1 and H_2 receptors.
- 公益社団法人日本薬学会の論文
- 1997-02-15
著者
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村上 和夫
阪大院薬
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近藤 俊哉
Faculty Of Pharmaceutical Sciences Nagoya City University
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後藤 隆雄
トーアエイヨー株式会社
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Kondo T
Research Division The Green Cross Corporation
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Goto Takaaki
Faculty Of Pharmaceutical Sciences Tohoku University
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Goto T
トーアエイヨー
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Fukaya C
Yoshitomi Pharmaceutical Ind. Ltd. Osaka Jpn
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Fukaya Chikara
Quality Control Production Division Yoshitomi Pharmaceutical Industries Ltd.
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Fukaya Chikara
Research Division The Green Cross Corporation
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Sugiura M
Research Division The Green Cross Corporation
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Goto T
Hokuriku Univ. Kanazawa Jpn
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Murakami K
Osaka Univ. Osaka Jpn
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Murakami K
阪大院薬
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SAKASHITA Hiroshi
Research Division, The Green Cross Corporation
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GOTO Tomokazu
Research Division, The Green Cross Corporation
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MUARKAMI Kazuki
Research Division, The Green Cross Corporation
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SUGIURA Masanori
Research Division, The Green Cross Corporation
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KONDO Takao
Research Division, The Green Cross Corporation
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Sakashita H
Yamanouchi Pharmaceutical Co. Ltd. Ibaraki Jpn
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Sakashita Hiroshi
Research Division The Green Cross Corporation
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Murakami Kazuki
Research Division, The Green Cross Corporation
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