ArticleBioorganic & medicinal chemistry2011
Synthesis and characterization of selective dopamine D₂ receptor ligands using aripiprazole as the lead compound.
Article in Bioorganic & medicinal chemistry, 2011. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 16 papers.
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Who cites it
16 citing papers in PubMed, 51 citations in OpenAlex.
- Synthesis of bitopic ligands based on fallypride and evaluation of their affinity and selectivity towards dopamine DEuropean journal of medicinal chemistry · 2023Article
- Behavioural effects of APH199, a selective dopamine D4 receptor agonist, in animal models.Psychopharmacology · 2023Article
- Identification and Characterization of ML321: A Novel and Highly Selective DACS pharmacology & translational science · 2023Article
- Design and Synthesis of Conformationally Flexible Scaffold as Bitopic Ligands for Potent DInternational journal of molecular sciences · 2022Article
- Structure Activity Relationships for a Series of Eticlopride-Based Dopamine DJournal of medicinal chemistry · 2021Article
- BiasNet: A Model to Predict Ligand Bias Toward GPCR Signaling.Journal of chemical information and modeling · 2021Article
- Synthesis and In Vitro Evaluation of Novel Dopamine Receptor DBiomolecules · 2021Article
- Review
- Ligand with Two Modes of Interaction with the Dopamine DACS chemical neuroscience · 2020Article
- Leveraging a Low-Affinity Diazaspiro Orthosteric Fragment to Reduce Dopamine DJournal of medicinal chemistry · 2019Article
- Dopamine D3 receptor antagonist reveals a cryptic pocket in aminergic GPCRs.Scientific reports · 2018Article
- Advances and challenges in the search for DCellular signalling · 2018Review
- Positron emission tomography imaging of dopamine D2 receptors using a highly selective radiolabeled D2 receptor partial agonist.NeuroImage · 2013Article
- Comparison of the binding and functional properties of two structurally different D2 dopamine receptor subtype selective compounds.ACS chemical neuroscience · 2012Article
- Structure-functional selectivity relationship studies of β-arrestin-biased dopamine D₂ receptor agonists.Journal of medicinal chemistry · 2012Article
- Molecular determinants of selectivity and efficacy at the dopamine D3 receptor.Journal of medicinal chemistry · 2012Article
Corrections and comments
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Authors and funding
9 authors at 4 institutions in 1 country.
Funding
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.
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Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.