Piperidine-based nocaine/modafinil hybrid ligands as highly potent monoamine transporter inhibitors: efficient drug discovery by rational lead hybridization.
Piperidine-based nocaine/modafinil hybrid ligands as highly potent monoamine transporter inhibitors: efficient drug discovery by rational lead hybridization.
复制标题
基于哌啶的诺卡因/莫达非尼混合配体作为高效单胺转运蛋白抑制剂:通过合理的先导杂交实现有效的药物发现。
DOI:
10.1021/jm040117o
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发表时间:
2004
影响因子:
7.3
通讯作者:
Kozikowski,AlanP
中科院分区:
文献类型:
--
作者:
Zhou,Jia;He,Rong;Johnson,KennethM;Ye,Yanping;Kozikowski,AlanP
Some piperidine-based nocaine/modafinil hybrid ligands have been designed, synthesized, and found to display an improved potency at all three monoamine transporters and particularly for DAT and/or NET. Some highly active and selective monoamine transporter inhibitors with low nanomolar to subnanomolar potency were identified. Ligands of this type may find important applications as positron emission tomography imaging tools and in the treatment of central nervous system disorders such as depression and sleep apnea.