Synthesis and Evaluation of Fluorinated Aporphines: Potential Positron Emission Tomography Ligands for D2 Receptors
Article Details
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Sromek AW, Si YG, Zhang T, George SR, Seeman P, Neumeyer JL
Synthesis and Evaluation of Fluorinated Aporphines: Potential Positron Emission Tomography Ligands for D2 Receptors
ACS Med Chem Lett. 2011 Mar 10;2(3):189-194.
- PubMed ID
- 21666830 [ View in PubMed]
- 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.
DrugBank Data that Cites this Article
- Binding Properties
Drug Target Property Measurement pH Temperature (°C) Apomorphine Dopamine D1 receptor Ki (nM) 650 N/A N/A Details Apomorphine Dopamine D1 receptor Ki (nM) 4.6 N/A N/A Details Apomorphine Dopamine D3 receptor Ki (nM) 2.6 N/A N/A Details