| Title : 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 - Matulenko_2004_Bioorg.Med.Chem.Lett_14_5095 |
| Author(s) : Matulenko MA , Surber B , Fan L , Kolasa T , Nakane M , Terranova MA , Uchic ME , Miller LN , Chang R , Donnelly-Roberts D , Namovic MT , Moreland RB , Brioni JD , Stewart AO |
| Ref : Bioorganic & Medicinal Chemistry Lett , 14 :5095 , 2004 |
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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. |
| PubMedSearch : Matulenko_2004_Bioorg.Med.Chem.Lett_14_5095 |
| PubMedID: 15380206 |
Matulenko MA, Surber B, Fan L, Kolasa T, Nakane M, Terranova MA, Uchic ME, Miller LN, Chang R, Donnelly-Roberts D, Namovic MT, Moreland RB, Brioni JD, Stewart AO (2004)
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
Bioorganic & Medicinal Chemistry Lett
14 :5095
Matulenko MA, Surber B, Fan L, Kolasa T, Nakane M, Terranova MA, Uchic ME, Miller LN, Chang R, Donnelly-Roberts D, Namovic MT, Moreland RB, Brioni JD, Stewart AO (2004)
Bioorganic & Medicinal Chemistry Lett
14 :5095