2. Academic Validation
  3. 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

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

  • Bioorg Med Chem Lett. 2004 Oct 18;14(20):5095-8. doi: 10.1016/j.bmcl.2004.07.068.
Mark A Matulenko 1,  Bruce Surber,  Leimin Fan,  Teodozyi Kolasa,  Masaki Nakane,  Marc A Terranova,  Marie E Uchic,  Loan N Miller,  Renjie Chang,  Diana L Donnelly-Roberts,  Marian T Namovic,  Robert B Moreland,  Jorge D Brioni,  Andrew O Stewart
Affiliations

Affiliation

  • 1 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
PMID: 15380206 DOI: 10.1016/j.bmcl.2004.07.068
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.

Figures