Novel N1-(benzyl)cinnamamidine derived NR2B subtype-selective NMDA receptor antagonists
Novel N1-(benzyl)cinnamamidine derived NR2B subtype-selective NMDA receptor antagonists
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DOI：
10.1016/s0960-894x(02)01060-0
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发表时间：
2003-02-24
影响因子：
2.7
通讯作者：
Wafford, KA
中科院分区：
文献类型：
--
作者：
Curtis, NR;Diggle, HJ;Wafford, KA
制备了新型 (E)-N-1-(苄基)肉桂脒并作为 NR2B 亚型 NMDA 受体配体进行评估。通过适当取代任一苯环实现了优异的亲和力。 2-甲氧基苄基化合物 1h 在 NR2B 中的 IC50 比含有 NR2A 的细胞低 1000 倍。用 2-萘基取代苯乙烯基单元的耐受性良好。 (C) 2003 Elsevier Science Ltd. 保留所有权利。
Novel (E)-N-1-(benzyl)cinnamamidines were prepared and evaluated as NR2B subtype NMDA receptor ligands. Excellent affinity was achieved by appropriate substitution of either phenyl ring. The 2-methoxybenzyl compound 1h had similar to1000-fold lower IC50 in NR2B than NR2A-containing cells. Replacement of the styryl unit by 2-naphthl was well tolerated. (C) 2003 Elsevier Science Ltd. All rights reserved.