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Synthesis and Characterization of Selective Dopamine D₂ Receptor Ligands Using Aripiprazole as the Lead Compound

Synthesis and Characterization of Selective Dopamine D₂ Receptor Ligands Using Aripiprazole as the Lead Compound

Suwanna Vangveravong, Zhanbin Zhang, Michelle Taylor, Melissa Bearden, Jinbin Xu, Jinquan Cui, Wei Wang, Robert R Luedtke, Robert H Mach

Bioorg Med Chem. 2011 Jun 1;19(11):3502-11.

PMID: 21536445

Abstract:

A series of compounds structurally related to aripiprazole (1), an atypical antipsychotic and antidepressant used clinically for the treatment of schizophrenia, bipolar disorder, and depression, have been prepared and evaluated for affinity at D(₂-like) dopamine receptors. These compounds also share structural elements with the classical D(₂-like) dopamine receptor antagonists, haloperidol, N-methylspiperone, domperidone and benperidol. Two new compounds, 7-(4-(4-(2-methoxyphenyl)piperazin-1-yl)butoxy)-3,4-dihydroquinolin-2(1H)-one oxalate (6) and 7-(4-(4-(2-(2-fluoroethoxy)phenyl)piperazin-1-yl)butoxy)-3,4-dihydroquinolin-2(1H)-one oxalate (7) were found to (a) bind to the D₂ receptor subtype with high affinity (K(i) values < 0.3 nM), (b) exhibit >50-fold D₂ versus D₃ receptor binding selectivity and (c) be partial agonists at both the D₂ and D₃ receptor subtype.

Chemicals Related in the Paper:

Catalog Number	Product Name	Structure	CAS Number	Price
AP119532262	Aripiprazole Related Compound C		119532-26-2	Price
AP889443203	Aripiprazole Related Compound B		889443-20-3	Price

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