Synthesis and radioiodination of selective ligands for the dopamine D3 receptor subtype

Bioorganic & Medicinal Chemistry Letters
Carsten HockeTorsten Kuwert

Abstract

Starting from FAUC 365, a series of iodine substituted heteroaryl carboxamides has been synthesized revealing high affinity and selectivity for the dopamine D3 receptor. Binding data showed a 15-560-fold selectivity for the dopamine D3 over D2. A 2,3-dichloro substitution pattern on the phenylpiperazine moiety led to the highest subtype selectivity, whereas the 2-methoxy substituted compounds showed superior D3 affinity. Suitable precursors were radioiodinated with high radiochemical yields (53-85%) leading to potential imaging agents for the D3 receptor by SPET.

References


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Citations

Oct 22, 2008·Journal of Combinatorial Chemistry·Chul-Hee ChoRichard C Larock
Oct 13, 2010·Journal of Chemical Information and Modeling·Qi WangDavid E Reichert
Feb 6, 2007·Biochimica Et Biophysica Acta·Frank Boeckler, Peter Gmeiner
Sep 6, 2005·Bioorganic & Medicinal Chemistry Letters·Carsten HockeTorsten Kuwert
Jan 1, 2008·Bioorganic & Medicinal Chemistry Letters·Rainer TietzeOlaf Prante
May 30, 2008·Journal of Combinatorial Chemistry·Lidia De LucaGiammario Nieddu
Aug 14, 2010·The Journal of Organic Chemistry·Rafaela M GayGilson Zeni
Apr 11, 2007·The Journal of Organic Chemistry·Lidia De LucaGiammario Nieddu
May 27, 2005·Journal of Medicinal Chemistry·Amy Hauck NewmanMichael A Nader

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