ArticleJournal of medicinal chemistry2016
Highly Selective Dopamine D3 Receptor (D3R) Antagonists and Partial Agonists Based on Eticlopride and the D3R Crystal Structure: New Leads for Opioid Dependence Treatment.
Article in Journal of medicinal chemistry, 2016. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 64 papers.
What it found
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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
64 citing papers in PubMed, 87 citations in OpenAlex.
- Article
- 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
- A Ligand-Triggered Receptor Conformation Enables the Design of Selective Agonists for the Dopamine 3 Receptor (DJACS Au · 2026Article
- Bioisosteric Replacement of Amides with 1,2,3-Triazoles Improves Dopamine D4 Receptor Ligand Pharmacokinetics.ACS pharmacology & translational science · 2026Article
- Cannabinoid CB1 receptor and mu-opioid receptor interaction: new insights from conditional knockout mice.Neuropsychopharmacology : official publication of the American College of Neuropsychopharmacology · 2026Article
- Discovery, Characterization, and Optimization of a Novel Positive Allosteric Modulator-Antagonist of the DJournal of medicinal chemistry · 2025Article
- Locomotor activity depends on β-arrestin recruitment by the dopamine DPharmacological research · 2025Article
- Selective dopamine D3 receptor partial agonist (±)VK4-40 reduces the reinforcing strength of d-amphetamine but not cocaine in rhesus monkeys responding under a progressive-ratio schedule of reinforcement.Drug and alcohol dependence · 2024Article
- Presynaptic and Postsynaptic Mesolimbic Dopamine DBiological psychiatry · 2024Article
- Involvement of dopamine D3 receptor in impulsive choice decision-making in male rats.Neuropharmacology · 2024Article
- The selective DNeuropsychopharmacology : official publication of the American College of Neuropsychopharmacology · 2024Article
- Modeling impaired insight after drug use in rodents.Behavioral neuroscience · 2024Review
- Substance Addiction Rehabilitation Drugs.Pharmaceuticals (Basel, Switzerland) · 2024Review
- Modifications to 1-(4-(2-Bis(4-fluorophenyl)methyl)sulfinyl)alkyl Alicyclic Amines That Improve Metabolic Stability and Retain an Atypical DAT Inhibitor Profile.Journal of medicinal chemistry · 2024Article
- In vitro safety evaluation of dopamine D3R antagonist, R-VK4-116, as a potential medication for the treatment of opioid use disorder.PloS one · 2024Article
- Synthesis of bitopic ligands based on fallypride and evaluation of their affinity and selectivity towards dopamine DEuropean journal of medicinal chemistry · 2023Article
- Oxycodone: A Current Perspective on Its Pharmacology, Abuse, and Pharmacotherapeutic Developments.Pharmacological reviews · 2023Review
- Carbazole and tetrahydro-carboline derivatives as dopamine DActa pharmaceutica Sinica. B · 2023Article
- Comment on: Effects of selective dopamine D3 receptor partial agonist/antagonists on oxycodone self-administration and antinociception in monkeys.Neuropsychopharmacology : official publication of the American College of Neuropsychopharmacology · 2023Article
- Effects of selective dopamine D3 receptor partial agonist/antagonists on oxycodone self-administration and antinociception in monkeys.Neuropsychopharmacology : official publication of the American College of Neuropsychopharmacology · 2023Article
4 more citing papers are in PubMed but not listed here.
Corrections and comments
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Authors and funding
11 authors at 4 institutions in 1 country.
Funding
Abstract
The recent and precipitous increase in opioid analgesic abuse and overdose has inspired investigation of the dopamine D3 receptor (D3R) as a target for therapeutic intervention. Metabolic instability or predicted toxicity has precluded successful translation of previously reported D3R-selective antagonists to clinical use for cocaine abuse. Herein, we report a series of novel and D3R crystal structure-guided 4-phenylpiperazines with exceptionally high D3R affinities and/or selectivities with varying efficacies. Lead compound 19 was selected based on its in vitro profile: D3R Ki = 6.84 nM, 1700-fold D3R versus D2R binding selectivity, and its metabolic stability in mouse microsomes. Compound 19 inhibited oxycodone-induced hyperlocomotion in mice and reduced oxycodone-induced locomotor sensitization. In addition, pretreatment with 19 also dose-dependently inhibited the acquisition of oxycodone-induced conditioned place preference (CPP) in rats. These findings support the D3R as a target for opioid dependence treatment and compound 19 as a new lead molecule for development.
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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.