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Synthesis of a new 18F-fluorinated D4 receptor ligand

A potential dopaminergic D4 receptor ligand and further 18F-labelled derivatives have successfully been synthesized and pharmacologically evaluated in cooperation with the University of Erlangen.

The development of subtype specific radioligand is a basic requirement for the molecular imaging of neurodegenerative diseases using the positron-emission-tomography. In hits context the INM-5 developed successfully a radiosynthesis of 1-(2,3-dihydrobenzo­[b]­[1,4]dioxin-6-yl)-4-((6-[18F]fluoropyridin-3-yl)methyl)­piperazine and further derivatives. The results have been published in the Journal of Medicinal Chemistry (Kügler, F.; Sihver, W.*; Ermert, J.; Hübner, H.*; Gmeiner, P.*; Prante, O.*; Coenen, H.H.  Evaluation of 18F-labeled benzodioxine piperazine-based dopamine D4 receptor ligands: lipophilicity as a determinate of nonspecific binding, Journal of Medicinal Chemistry, 54 (2011) 24, 8343 – 8352).


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