1H NMR Probe for in Situ Monitoring of Dopamine Metabolism and Its Application to Inhibitor Screening

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• 作者：Ryosuke Ueki ; Koya Yamaguchi ; Hiroshi Nonaka ; Shinsuke Sando
• 刊名：The Journal of the American Chemical Society
• 出版年：2012
• 出版时间：August 1, 2012
• 年：2012
• 卷：134
• 期：30
• 页码：12398-12401
• 全文大小：272K
• 年卷期：v.134,no.30(August 1, 2012)
• ISSN：1520-5126

文摘

Dopamine (DA) is a monoamine neurotransmitter that plays important roles in the brain, and whose levels in the brain are associated with several neurological and psychiatric disorders. Therefore, DA metabolism inhibitors have been used as therapeutic agents. Here, we report a ¹H NMR probe for the in situ analysis of DA metabolism, and its application to DA inhibitor screening. We designed doubly ¹³C-labeled DA (¹³C₂-DA) as the probe. The combination of the ¹³C₂-DA and ¹H鈥搟¹³C鈥?sup>13C鈥瞹 NMR technique allowed the selective and thus in situ monitoring of DA metabolism. Using ¹³C₂-DA, we successfully measured the efficacies of different inhibitors in a tissue sample, allowing us to improve the in situ inhibitory efficacy of the known DA metabolism inhibitor, clorgyline.