Synthesis and Biological Evaluation of N-Fluoroalkyl and 2-Fluoroalkoxy Substituted Aporphines: Potential PET Ligands for Dopamine D(2) Receptors |
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| Authors: | Sromek Anna W Si Yu-Gui Zhang Tangzhi George Susan R Seeman Philip Neumeyer John L |
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| Affiliation: | Alcohol & Drug Abuse Research Center, McLean Hospital, Harvard Medical School, 115 Mill Street, Belmont, MA 02478-9106 USA. |
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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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| Keywords: | Aporphine D2 agonist neurological disorders positron emission tomography dopamine receptors |
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