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Front Cover: Evaluation of 5H‐Thiazolo[3,2‐α]pyrimidin‐5‐ones as Potential GluN2A PET Tracers (ChemMedChem 24/2020)
ChemMedChem ( IF 3.4 ) Pub Date : 2020-11-26 , DOI: 10.1002/cmdc.202000909
Yingfang He 1 , David M. Whitehead 2 , Emmanuelle Briard 2 , Shin Numao 3 , Linjing Mu 1 , Roger Schibli 1 , Simon M. Ametamey 1 , Yves P. Auberson 2
Affiliation  

The Front Cover shows the postsynaptic location of GluN2A‐containing NMDA receptors, their ligand‐binding domain, as well as a close‐up of [18F]7b bound to the receptor with the corresponding images obtained by in vitro autoradiography of rat brain sections in a blocking study. Both [18F]7b and its tritiated analogue [3H2]15b are valuable new tools for the study of GluN2A‐containing NMDA receptors, and for the optimization of allosteric modulators binding to the dimer interface of the GluN1‐GluN2A ligand‐binding domain. More information can be found in the Full Paper by Simon M. Ametamey, Yves P. Auberson et al.
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中文翻译:

封面:评价5H-噻唑并[3,2-α]嘧啶-5-酮作为潜在的GluN2A PET示踪剂(ChemMedChem 24/2020)

封面显示了含有GluN2A的NMDA受体的突触后位置,其配体结合结构域以及与该受体结合的[ 18 F] 7b的特写,以及通过大鼠脑切片的体外放射自显影获得的相应图像在一项阻碍性研究中。[ 18 F] 7b及其tri化的类似物[ 3 H 2 ] 15b都是研究含GluN2A的NMDA受体以及优化与GluN1-GluN2A配体结合的二聚体界面结合的变构调节剂的有价值的新工具域。更多信息可以在Simon M. Ametamey,Yves P. Auberson等人的论文全文中找到。
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更新日期:2020-12-16
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