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
; 14(20): 5095-8, 2004 Oct 18.
Article
em En
| MEDLINE
| ID: mdl-15380206
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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Base de dados:
MEDLINE
Assunto principal:
Piperazinas
/
Receptores de Dopamina D2
/
Acetamidas
Idioma:
En
Ano de publicação:
2004
Tipo de documento:
Article