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Cubyl amides: Novel P2X(7) receptor antagonists

  作者 Gunosewoyo, H; Guo, JL; Bennett, MR; Coster, MJ; Kassiou, M  
  选自 期刊  Bioorganic & Medicinal Chemistry Letters;  卷期  2008年18-13;  页码  3720-3723  
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[摘要]Polycyclic amides 2 and 5 -9 were successfully synthesised and their lipophilicity profiles were evaluated using reverse-phase HPLC. All synthesised compounds possessed P2X(7)R antagonistic properties when tested on rat spinal cord microglia cells. Extensive screening for binding to other neuroreceptor subtypes demonstrated their P2X(7) selectivity. (C) 2008 Elsevier Ltd. All rights reserved.

 
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