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Synthesis and characterization of selective dopamine D2 receptor ligands using aripiprazole as the lead compound by Suwanna Vangveravong; Zhanbin Zhang; Michelle Taylor; Melissa Bearden; Jinbin Xu; Jinquan Cui; Wei Wang; Robert R. Luedtke; Robert H. Mach is a Biochemistry, Genetics and Molecular Biology article available to read on EtoBox.

What is Synthesis and characterization of selective dopamine D2 receptor ligands using aripiprazole as the lead compound about?

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 D 2 receptor subtype with high affinity (K i values 50-fold D 2 versus D 3 receptor binding selectivity and (c) be partial agonists at both the D 2 and D 3 receptor subtype.

Who reads Synthesis and characterization of selective dopamine D2 receptor ligands using aripiprazole as the lead compound?

Author

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

Publisher

Elsevier Science; Elsevier ; Elsevier Ltd.; Elsevier BV (ISSN 0968-0896)

Published

2011

Language

EN

Field

Biochemistry, Genetics and Molecular Biology (Life Sciences)