ArticleJournal of medicinal chemistry2012
Structure-functional selectivity relationship studies of β-arrestin-biased dopamine D₂ receptor agonists.
Article in Journal of medicinal chemistry, 2012. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 64 papers.
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Who cites it
64 citing papers in PubMed.
- Biased Allosteric Modulation in GPCR Drug Discovery.Handbook of experimental pharmacology · 2026Review
- Molecular Glues: A New Approach to Modulating GPCR Signaling Bias.Biochemistry · 2025Review
- The multifaceted functions of β-arrestins and their therapeutic potential in neurodegenerative diseases.Experimental & molecular medicine · 2024Review
- Optical Control of Dopamine D2-like Receptors with Cell-Specific Fast-Relaxing Photoswitches.Journal of the American Chemical Society · 2023Article
- The histamine H3 receptor modulates dopamine D2 receptor-dependent signaling pathways and mouse behaviors.The Journal of biological chemistry · 2023Article
- Phosphoproteomic Analysis of Dopamine D2 Receptor Signaling Reveals Interplay of G Protein- and β-Arrestin-Mediated Effects.Journal of proteome research · 2023Article
- Open Bite Malocclusion Following Aripiprazole Treatment in Children and Adolescents.Innovations in clinical neuroscience · 2023Article
- Iron-Catalyzed Intramolecular Arene C(spAngewandte Chemie (International ed. in English) · 2022Article
- Identification of Novel Dopamine DMolecules (Basel, Switzerland) · 2022Article
- Selective Signal Capture from Multidimensional GPCR Outputs with Biased Agonists: Progress Towards Novel Drug Development.Molecular diagnosis & therapy · 2022Review
- Synthesis, biological evaluation, and molecular docking of novel hydroxyzine derivatives as potential AR antagonists.Frontiers in chemistry · 2022Article
- Synthesis, bioactivity, and molecular docking of novel arylpiperazine derivatives as potential AR antagonists.Frontiers in chemistry · 2022Article
- Structure-based design of a novel third-generation antipsychotic drug lead with potential antidepressant properties.Nature neuroscience · 2022Article
- 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
- Potent and Subtype-Selective Dopamine DJournal of medicinal chemistry · 2021Article
- Chirality of Novel Bitopic Agonists Determines Unique Pharmacology at the Dopamine D3 Receptor.Biomolecules · 2021Article
- Functionally selective activation of the dopamine receptor DScientific reports · 2021Article
- Arrestin recruitment to dopamine D2 receptor mediates locomotion but not incentive motivation.Molecular psychiatry · 2020Article
- Fluorescent ligands: Bringing light to emerging GPCR paradigms.British journal of pharmacology · 2020Review
4 more citing papers are in PubMed but not listed here.
Corrections and comments
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Authors and funding
10 authors.
Funding
Abstract
Functionally selective G protein-coupled receptor (GPCR) ligands, which differentially modulate canonical and noncanonical signaling, are extremely useful for elucidating key signal transduction pathways essential for both the therapeutic actions and side effects of drugs. However, few such ligands have been created, and very little purposeful attention has been devoted to studying what we term: "structure-functional selectivity relationships" (SFSR). We recently disclosed the first β-arrestin-biased dopamine D(2) receptor (D(2)R) agonists UNC9975 (44) and UNC9994 (36), which have robust in vivo antipsychotic drug-like activities. Here we report the first comprehensive SFSR studies focused on exploring four regions of the aripiprazole scaffold, which resulted in the discovery of these β-arrestin-biased D(2)R agonists. These studies provide a successful proof-of-concept for how functionally selective ligands can be discovered.
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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.