氮杂三环辛烷 σ（sigma）受体配体的氧桥异构体：合成、体外结合和分子模拟。
Oxo-bridged isomers of aza-trishomocubane sigma (sigma) receptor ligands: Synthesis, in vitro binding, and molecular modeling.
机构信息
School of Chemistry, University of Sydney, NSW 2006, Australia.
出版信息
Bioorg Med Chem Lett. 2010 Jan 1;20(1):145-8. doi: 10.1016/j.bmcl.2009.11.019. Epub 2009 Nov 12.
PMID:19954972
Abstract
Isomeric oxo-bridged analogs of aza-trishomocubane sigma (sigma) receptor ligands were synthesized and shown to display a reduced affinity for the sigma receptor. In the case of phenethyl derivative 4, there was a concomitant introduction of high-affinity for the alpha(2C) adrenergic receptor, and moderate affinity for the dopamine transporter. Molecular modeling was undertaken to rationalize these results.
摘要
合成了氮杂三环辛烷 σ（sigma）受体配体的同型氧桥类似物，并证明其对 sigma 受体的亲和力降低。在苯乙胺衍生物 4 的情况下，同时引入了对 alpha(2C)肾上腺素能受体的高亲和力和对多巴胺转运体的中等亲和力。进行了分子建模以合理化这些结果。
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