Concepedia

Synthesis and Evaluation of Fluorinated Aporphines: Potential Positron Emission Tomography Ligands for D<sub>2</sub> Receptors

Anna W. Sromek, Yu‐Gui Si, Tangzhi Zhang, Susan R. George, Philip Seeman, John L. Neumeyer

ACS Medicinal Chemistry Letters · 2011 · 19 citations · 32 references

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Abstract

The 2-fluoroalkoxy substituted catechol-aporphines 6, 8a-f and 11-monohydroxyaporphines 11a-e were synthesized and found to have high in vitro affinity and selectivity for the dopamine D(2) receptors. The catechol aporphines, 8b and 8d, and the monohydroxy aporphines, 11a-d, were identified as candidates for development as potential PET ligands.

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