Record number :
794716
Title of article :
Synthesis and radioiodination of selective ligands for the dopamine D3 receptor subtype
Author/Authors :
Carsten Hocke، نويسنده , , Olaf Prante، نويسنده , , Stefan L?ber، نويسنده , , Harald Hübner، نويسنده , , Peter Gmeiner، نويسنده , , Torsten Kuwert، نويسنده ,
Issue Information :
روزنامه با شماره پیاپی سال 2004
Pages :
4
From page :
3963
To page :
3966
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.
Keywords :
D3 receptor , Dopamine , SPET.* Corresponding author. Tel.: +49-9131-8533699 , fax: +49-9131-8539262 , e-mail: carsten.hocke@nuklear.imed.uni-erlangen.de , Radioligand
Journal title :
Bioorganic & Medicinal Chemistry Letters
Serial Year :
2004
Link To Document :
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