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 |
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Authors: | Matulenko Mark A Surber Bruce Fan Leimin Kolasa Teodozyi Nakane Masaki Terranova Marc A Uchic Marie E Miller Loan N Chang Renjie Donnelly-Roberts Diana L Namovic Marian T Moreland Robert B Brioni Jorge D Stewart Andrew O |
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Affiliation: | Neuroscience Research, Global Pharmaceutical Research and Development, Abbott Laboratories, AP9A/L16, 100 Abbott Park Road, Abbott Park, IL 60064-6115, USA. mark.a.matulenko@abbott.com |
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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. |
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