ReviewAdvances in pharmacology (San Diego, Calif.)2014
Beyond small-molecule SAR: using the dopamine D3 receptor crystal structure to guide drug design.
Review in Advances in pharmacology (San Diego, Calif.), 2014. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 35 papers.
What it found
Each row is one number read from the abstract, on the scale the paper reported it, with its interval. Left of the dashed line favours the treatment, right favours the comparator. Under each row is the sentence it came from. New to these charts? A ten-minute tutorial.
The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.
The trial behind it
Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
Neither the registry nor the abstract names a trial number. If this is a trial report, that itself is worth knowing.
Who cites it
35 citing papers in PubMed.
- Developing the Dopamine D3 Receptor (D3R) Antagonist, (R)-VK4-116, as a Non-Opioid Medication for the Treatment of Opioid Use Disorder.Medicinal research reviews · 2026Review
- ESG-1-60 and ESG-1-61: Novel dopamine DBritish journal of pharmacology · 2025Article
- Review on allosteric modulators of dopamine receptors so far.Health science reports · 2024Article
- Dopamine DJournal of medicinal chemistry · 2023Article
- A highly DNeuropsychopharmacology : official publication of the American College of Neuropsychopharmacology · 2022Article
- Chiral Cyclic Aliphatic Linkers as Building Blocks for Selective Dopamine DJournal of medicinal chemistry · 2021Article
- Structure Activity Relationships for a Series of Eticlopride-Based Dopamine DJournal of medicinal chemistry · 2021Article
- Scaffold Hybridization Strategy Leads to the Discovery of Dopamine DACS chemical neuroscience · 2021Article
- Allosteric Modulators of G Protein-Coupled Dopamine and Serotonin Receptors: A New Class of Atypical Antipsychotics.Pharmaceuticals (Basel, Switzerland) · 2020Review
- Evidence for a Stereoselective Mechanism for Bitopic Activity by Extended-Length Antagonists of the DACS chemical neuroscience · 2020Article
- Exception That Proves the Rule: Investigation of Privileged Stereochemistry in Designing Dopamine DACS medicinal chemistry letters · 2020Article
- (±)VK4-40, a novel dopamine DBritish journal of pharmacology · 2020Article
- Dopamine D3 receptor-based medication development for the treatment of opioid use disorder: Rationale, progress, and challenges.Neuroscience and biobehavioral reviews · 2020Review
- Discovery, Optimization, and Characterization of ML417: A Novel and Highly Selective DJournal of medicinal chemistry · 2020Article
- 2016 Philip S. Portoghese Medicinal Chemistry Lectureship: Designing Bivalent or Bitopic Molecules for G-Protein Coupled Receptors. The Whole Is Greater Than the Sum of Its Parts.Journal of medicinal chemistry · 2020Article
- Newly Developed Dopamine DThe Journal of pharmacology and experimental therapeutics · 2019Article
- Investigation of Novel Primary and Secondary Pharmacophores and 3-Substitution in the Linking Chain of a Series of Highly Selective and Bitopic Dopamine DJournal of medicinal chemistry · 2019Article
- The Significance of Chirality in Drug Design and Synthesis of Bitopic Ligands as DJournal of medicinal chemistry · 2019Article
- Novel and Potent Dopamine DACS pharmacology & translational science · 2019Article
- A new era of rationally designed antipsychotics.Nature · 2018Article
Corrections and comments
PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.
Authors and funding
4 authors.
Funding
Abstract
The dopamine D3 receptor is a target of pharmacotherapeutic interest in a variety of neurological disorders including schizophrenia, restless leg syndrome, and drug addiction. The high protein sequence homology between the D3 and D2 receptors has posed a challenge to developing D3 receptor-selective ligands whose behavioral actions can be attributed to D3 receptor engagement, in vivo. However, through primarily small-molecule structure-activity relationship (SAR) studies, a variety of chemical scaffolds have been discovered over the past two decades that have resulted in several D3 receptor-selective ligands with high affinity and in vivo activity. Nevertheless, viable clinical candidates remain limited. The recent determination of the high-resolution crystal structure of the D3 receptor has invigorated structure-based drug design, providing refinements to the molecular dynamic models and testable predictions about receptor-ligand interactions. This chapter will highlight recent preclinical and clinical studies demonstrating potential utility of D3 receptor-selective ligands in the treatment of addiction. In addition, new structure-based rational drug design strategies for D3 receptor-selective ligands that complement traditional small-molecule SAR to improve the selectivity and directed efficacy profiles are examined.
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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.