Neuroscience Research, GPRD, Abbott, Abbott Park, IL 60064-6117, USA.
Bioorg Med Chem Lett. 2010 Jun 15;20(12):3636-9. doi: 10.1016/j.bmcl.2010.04.105. Epub 2010 Apr 28.
Biaryl substituted 2,5-diazabicyclo[2.2.1]heptanes have been synthesized and tested for their affinity toward alpha7 neuronal nicotinic receptors (NNRs). SAR studies established that 5-N-methyl substituent, heteroaryl linker and the nature of terminal aryl group are critical for the ligand to achieve potent alpha7 NNR agonist activity.
已合成并测试了联芳基取代的 2,5-二氮杂双环[2.2.1]庚烷，以评估它们对α7 型神经元烟碱型受体（NNRs）的亲和力。SAR 研究表明，5-N-甲基取代基、杂芳基连接基和末端芳基基团的性质对于配体发挥强效的α7 NNR 激动剂活性至关重要。
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