School of Chemistry, The University of Sydney, Sydney, NSW 2006, Australia.
Bioorg Med Chem Lett. 2011 Jan 1;21(1):38-41. doi: 10.1016/j.bmcl.2010.11.075. Epub 2010 Nov 21.
In our continued exploration of trishomocubane derivatives with central nervous system (CNS) activity, N-arylalkyl-8-aminopentacyclo[5.4.0.0(2,6).0(3,10).0(5,9)]undecanes (10-13) displaying affinity for the sigma (σ) receptor were also found, in several cases, to interact with the dopamine transporter (DAT). Compound 12 was identified as the first trishomocubane-derived high affinity DAT ligand (K(i) = 1.2 nM), with greater than 8300-fold selectivity over the monoamine transporters NET and SERT, and only low to moderate affinity for σ(1) and σ(2) receptors.
在我们对具有中枢神经系统 (CNS) 活性的三环癸烷衍生物的持续探索中，我们还发现了具有 sigma (σ) 受体亲和力的 N-芳基烷基-8-氨基五环[5.4.0.0(2,6).0(3,10).0(5,9)]十一烷（10-13），在某些情况下，它们还与多巴胺转运体（DAT）相互作用。化合物 12 被确定为第一个三环癸烷衍生的高亲和力 DAT 配体（K(i) = 1.2 nM），对单胺转运体 NET 和 SERT 的选择性超过 8300 倍，对 σ(1) 和 σ(2) 受体的亲和力较低至中等。
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