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J Med Chem. 2008 Nov 13;51(21):6682-8. doi: 10.1021/jm8003637. Epub 2008 Oct 10.

Molecular probes for imaging myelinated white matter in CNS.

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Department of Radiology and Neurosciences, Case Western Reserve University, Cleveland, Ohio 44106, USA.


Abnormalities and changes in myelination in the brain are seen in many neurodegenerative disorders such as multiple sclerosis (MS). Direct detection and quantification of myelin content in vivo is desired to facilitate diagnosis and therapeutic treatments of myelin-related diseases. The imaging studies require use of myelin-imaging agents that readily enter the brain and selectively bind to myelinated regions. For this purpose, we have systematically evaluated a series of stilbene derivatives as myelin imaging agents. Spectrophotometry-based and radioligand-based binding assays showed that these stilbene derivatives exhibited relatively high myelin-binding affinities. In vitro myelin staining exhibited that the compounds selectively stained intact myelinated regions in wild type mouse brain. In situ tissue staining demonstrated that the compounds readily entered the mouse brain and selectively labeled myelinated white matter regions. These studies suggested that these stilbene derivatives can be used as myelin-imaging probes to monitor myelin pathology in vivo.

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