Synthesis and Evaluation of Fluorinated Aporphines: Potential Positron Emission Tomography Ligands for D2 Receptors

The 2-fluoroalkoxy-substituted catechol-aporphines 6, 8a−f and 11-mono-hydroxyaporphines 11a−e were synthesized and found to have high in vitro affinity and selectivity for the dopamine D2 receptors. The catechol aporphines, 8b and 8d, and the monohydroxy aporphines, 11a−d, were identified as candid...

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Published in:ACS medicinal chemistry letters 2011-03, Vol.2 (3), p.189-194
Main Authors: Sromek, Anna W, Si, Yu-Gui, Zhang, Tangzhi, George, Susan R, Seeman, Philip, Neumeyer, John L
Format: Article
Language:English
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Letter
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Summary:The 2-fluoroalkoxy-substituted catechol-aporphines 6, 8a−f and 11-mono-hydroxyaporphines 11a−e were synthesized and found to have high in vitro affinity and selectivity for the dopamine D2 receptors. The catechol aporphines, 8b and 8d, and the monohydroxy aporphines, 11a−d, were identified as candidates for development as potential PET ligands.
ISSN:1948-5875
1948-5875
DOI:10.1021/ml1001689