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ID: ALA1137095

Journal: Bioorg Med Chem Lett

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

Authors: Hocke C, Prante O, Löber S, Hübner H, Gmeiner P, Kuwert T.

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.

CiteXplore: 15225707

DOI: 10.1016/j.bmcl.2004.05.052