3-ベンジリデンミオスミンおよび3-シンナミリデンミオスミン類縁体のワモンゴキブリニコチン性アセチルコリン受容体に対する親和性

DOI 機関リポジトリ NDLデジタルコレクション 日本農学文献記事索引 Web Site ほか1件をすべて表示 一部だけ表示 被引用文献1件 参考文献20件
  • Ikeda Izumi
    Department of Life Science and Biotechnology, Faculty of Life and Environmental Science, Shimane University
  • Utsunomiya Tsuyoshi
    Department of Life Science and Biotechnology, Faculty of Life and Environmental Science, Shimane University
  • Sadamitsu Miki
    Department of Life Science and Biotechnology, Faculty of Life and Environmental Science, Shimane University
  • Ozoe Yoshihisa
    Department of Life Science and Biotechnology, Faculty of Life and Environmental Science, Shimane University
  • Mochida Kazuo
    Department of Life Science and Biotechnology, Faculty of Life and Environmental Science, Shimane University

書誌事項

タイトル別名
  • Affinity of 3-benzylidene- and 3-cinnamylidenemyosmine analogues for Periplaneta americana nicotinic acetylcholine receptors

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抄録

3-Benzylidenemyosmine analogues with substituents at the ortho-, meta-, and para-positions of the phenyl ring and 3-cinnamylidenemyosmine analogues with substituents at a para-position of the phenyl ring were synthesized. The affinity of the synthesized compounds for nicotinic acetylcholine receptors (nAChRs) in the nerve cord of the American cockroach (Periplaneta americana L.) was determined by radioligand binding assay using [3H]epibatidine. Of the compounds tested, 3-(2,4-dihydroxybenzylidene)myosmine 3 and 3-(4-hydroxybenzylidene)myosmine 4 displayed the highest potency, with IC50 values of 0.120 and 0.310 μM, respectively. 3-(4-Dimethylaminobenzylidene)myosmine 15 with a para-dimethylamino group on the benzylidene moiety displayed moderate affinity (IC50=5.49 μM). On the other hand, cinnamylidene analogues, 3-(4-dimethyl­amino­cinnamylidene)myosmine 16 and 3-cinnamylidenemyosmine 17, displayed moderate affinity, with IC50 values of 2.07 and 3.52 μM, respectively.

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