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 ,
Issue Information
روزنامه با شماره پیاپی سال 2004
Pages
4
From page
5095
To page
5098
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
Journal title
Bioorganic & Medicinal Chemistry Letters
Serial Year
2004
Journal title
Bioorganic & Medicinal Chemistry Letters
Record number
794934
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