Design, synthesis, and evaluation of coumarin-based molecular probes for imaging of myelination.
Design, synthesis, and evaluation of coumarin-based molecular probes for imaging of myelination.
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DOI：
10.1021/jm101489w
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发表时间：
2011-04-14
影响因子：
7.3
通讯作者：
Wang Y
中科院分区：
文献类型：
--
作者：
Wang C;Wu C;Zhu J;Miller RH;Wang Y
髓鞘形成是脊椎动物神经系统中最基本的生物过程之一。中枢神经系统（CNS）髓鞘形成的异常和改变见于许多神经退行性疾病，如多发性硬化症（MS）。长期以来的目标是直接检测和量化髓磷脂含量，以促进髓磷脂相关疾病的诊断和治疗。在我们的研究过程中，我们开发了一系列的小分子探针（SMP）作为髓磷脂显像剂。其中包括香豆素衍生物，具有良好的脑通透性和髓磷脂结合特性。在这里，我们报告了香豆素为基础的SMPs作为髓鞘显像剂的设计和合成的完整说明。对这些SMPs在中枢神经系统和周围神经系统（PNS）中的系统评估使我们能够确定一些先导剂，这些先导剂可能用作外科手术中术中神经定位的荧光染料或髓鞘形成的正电子发射断层扫描（PET）成像的放射性示踪剂。
Myelination represents one of the most fundamental biological processes in the vertebrate nervous system. Abnormalities and changes in myelination in the central nervous system (CNS) are seen in many neurodegenerative disorders such as multiple sclerosis (MS). A long-standing goal has been to directly detect and quantify myelin content in order to facilitate diagnosis and therapeutic treatments of myelin-related diseases. In the course of our studies, we have developed a series of small-molecule probes (SMP) as myelin-imaging agents. Among them are coumarin derivatives, which exhibit promising brain permeability and myelin-binding properties. Herein we report a full account of the design and synthesis of coumarin-based SMPs as myelin-imaging agents. Systematic evaluation of these SMPs in both the CNS and peripheral nervous system (PNS) allowed us to identify some lead agents for potential use as fluorescent dyes for intraoperative nerve mapping in surgical operations or as radiotracers for positron emission tomography (PET) imaging of myelination.
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影响因子：
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作者：
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DOI：
10.1073/pnas.0405665101
发表时间：
2004-09-14
影响因子：
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作者：
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