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Front Cover: [Carboxyl‐11C]Labelling of Four High‐Affinity cPLA2α Inhibitors and Their Evaluation as Radioligands in Mice by Positron Emission Tomography (ChemMedChem 2/2018)
ChemMedChem ( IF 3.4 ) Pub Date : 2018-01-26 , DOI: 10.1002/cmdc.201800029 Martin J. Fisher 1 , Lindsay McMurray 1 , Shuiyu Lu 2 , Cheryl L. Morse 2 , Jeih-San Liow 2 , Sami S. Zoghbi 2 , Aneta Kowalski 2 , George L. Tye 2 , Robert B. Innis 2 , Franklin I. Aigbirhio 1 , Victor W. Pike 2
ChemMedChem ( IF 3.4 ) Pub Date : 2018-01-26 , DOI: 10.1002/cmdc.201800029 Martin J. Fisher 1 , Lindsay McMurray 1 , Shuiyu Lu 2 , Cheryl L. Morse 2 , Jeih-San Liow 2 , Sami S. Zoghbi 2 , Aneta Kowalski 2 , George L. Tye 2 , Robert B. Innis 2 , Franklin I. Aigbirhio 1 , Victor W. Pike 2
Affiliation
The Front Cover shows the in vivo evaluation of a prospective radioligand for cPLA2a, a biomarker for neuroinflammation, in a mouse brain by positron emission tomography (PET). In order to reversibly bind to the enzyme target, the 11C‐labelled indole‐5‐carboxylic acid needs to overcome the blood–brain barrier (BBB) in sufficient concentration. The data in an animal model build foundational knowledge on the pharmacokinetic behavior of compounds in this structural class and may provide guidance for future efforts to develop effective PET radioligands for cPLA2a. More information can be found in the Full Paper by Shuiyu Lu et al. on page 138 in Issue 2, 2018 (DOI: 10.1002/cmdc.201700697).
中文翻译:
封面:[Carboxyl-11C]四种高亲和力cPLA2α抑制剂的标签及其通过正电子发射断层显像法评估其在小鼠中的放射性配体(ChemMedChem 2/2018)
封面显示了通过正电子发射断层扫描(PET)在小鼠大脑中对cPLA2a(一种神经炎症的生物标记物)的预期放射性配体的体内评估。为了可逆地与酶靶结合,需要11 C标记的吲哚5羧酸以足够的浓度克服血脑屏障(BBB)。动物模型中的数据为该结构类化合物的药代动力学行为奠定了基础知识,并可能为将来开发有效的cPLA2a PET放射性配体提供指导。可以在Shuiyu Lu等人的论文全文中找到更多信息。关于在第2期,2018第138页(:10.1002 / cmdc.201700697 DOI)。
更新日期:2018-01-26
中文翻译:
封面:[Carboxyl-11C]四种高亲和力cPLA2α抑制剂的标签及其通过正电子发射断层显像法评估其在小鼠中的放射性配体(ChemMedChem 2/2018)
封面显示了通过正电子发射断层扫描(PET)在小鼠大脑中对cPLA2a(一种神经炎症的生物标记物)的预期放射性配体的体内评估。为了可逆地与酶靶结合,需要11 C标记的吲哚5羧酸以足够的浓度克服血脑屏障(BBB)。动物模型中的数据为该结构类化合物的药代动力学行为奠定了基础知识,并可能为将来开发有效的cPLA2a PET放射性配体提供指导。可以在Shuiyu Lu等人的论文全文中找到更多信息。关于在第2期,2018第138页(:10.1002 / cmdc.201700697 DOI)。