Synthesis and activity of 2-[4-(4-[3 H]-2-cyanophenyl) piperazinyl]-N-(2, 4, 6-[3 H] 3-3-methylphenyl) acetamide: a selective dopamine D 4 receptor agonist and …

…, R Chang, DL Donnelly-Roberts, MT Namovic…

Index: 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. Bioorganic and Medicinal Chemistry Letters, 2004 , vol. 14, # 20 p. 5095 - 5098

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Citation Number: 12

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 ...