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


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.

SUBMITTER: Sromek AW 

PROVIDER: S-EPMC3110009 | biostudies-literature | 2011 Mar

REPOSITORIES: biostudies-literature

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

Sromek Anna W AW   Si Yu-Gui YG   Zhang Tangzhi T   George Susan R SR   Seeman Philip P   Neumeyer John L JL  

ACS medicinal chemistry letters 20110301 3


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. ...[more]

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