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

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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

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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.

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