Title of article :
Synthesis and activity of 2-[4-(4-[3H]-2-cyanophenyl)piperazinyl]-N-(2,4,6-[3H]3-3-methylphenyl)acetamide: a selective dopamine D4 receptor agonist and radioligand
Author/Authors :
Mark A. Matulenko، نويسنده , , Bruce Surber، نويسنده , , Leimin Fan، نويسنده , , Teodozyi Kolasa، نويسنده , , Masaki Nakane، نويسنده , , Marc A. Terranova، نويسنده , , Marie E. Uchic، نويسنده , , Loan N. Miller، نويسنده , , Renjie Chang، نويسنده , , Diana L. Donnelly-Roberts، نويسنده , , Marian T. Namovic، نويسنده , , Robert B. Moreland، نويسنده , , Jorge D. Brioni، نويسنده , , Andrew O. Stewart، نويسنده ,
Abstract :
The first selective dopamine D4 agonist radioligand is described. The synthesis of these piperazine radioligands relied on the transformation of brominated precursors 4a and 4b with tritium gas in the presence of a sensitive cyano functional group. The specific activity of these two radioligands was measured and [3H]6b found to be suitable for use in D4 saturation and competition binding studies. The synthesis, biological, and radioactivity of this new agonist radioligand as well as preliminary SAR will be discussed.
Keywords :
Dopamine , agonist , Radioligand.* Corresponding author. Tel.: +1 847 938 2460 , fax: +1 847 937 9195 , e-mail: mark.a.matulenko@abbott.com
