ArticleJournal of medicinal chemistry2015
High Affinity Dopamine D3 Receptor (D3R)-Selective Antagonists Attenuate Heroin Self-Administration in Wild-Type but not D3R Knockout Mice.
Article in Journal of medicinal chemistry, 2015. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 38 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.
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Who cites it
38 citing papers in PubMed, 52 citations in OpenAlex.
- Can the incentive-sensitization theory of addiction incorporate addiction to opioid drugs?Psychopharmacology · 2026Review
- Impact of environmental enrichment on heroin-induced neuroadaptations in the insula, nucleus accumbens and ventral tegmental area.Neuropharmacology · 2026Article
- Bioisosteric Replacement of Amides with 1,2,3-Triazoles Improves Dopamine D4 Receptor Ligand Pharmacokinetics.ACS pharmacology & translational science · 2026Article
- Discovery, Characterization, and Optimization of a Novel Positive Allosteric Modulator-Antagonist of the DJournal of medicinal chemistry · 2025Article
- The selective DNeuropsychopharmacology : official publication of the American College of Neuropsychopharmacology · 2024Article
- Blockade of the Dopamine DNeuroscience bulletin · 2023Article
- Pharmacology and Therapeutic Potential of Benzothiazole Analogues for Cocaine Use Disorder.Journal of medicinal chemistry · 2023Article
- Dopamine D3 Receptor Modulates Akt/mTOR and ERKInternational journal of molecular sciences · 2023Article
- A highly DNeuropsychopharmacology : official publication of the American College of Neuropsychopharmacology · 2022Article
- Design, Synthesis and Pharmacological Evaluation of Novel Conformationally RestrictedBiomolecules · 2022Article
- Reflections of six neuroscientists: The influences of training at minority serving institutions.Journal of neuroscience research · 2022Article
- Chiral Cyclic Aliphatic Linkers as Building Blocks for Selective Dopamine DJournal of medicinal chemistry · 2021Article
- Effects of the selective dopamine DBehavioural brain research · 2021Article
- Low-dose polypharmacology targeting dopamine D1 and D3 receptors reduces cue-induced relapse to heroin seeking in rats.Addiction biology · 2021Article
- Pharmacogenomics of oxycodone: a narrative literature review.Pharmacogenomics · 2021Review
- Amide Bond Bioisosteres: Strategies, Synthesis, and Successes.Journal of medicinal chemistry · 2020Review
- 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
Corrections and comments
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Authors and funding
13 authors at 7 institutions in 1 country.
Funding
Abstract
The dopamine D3 receptor (D3R) is a promising target for the development of pharmacotherapeutics to treat substance use disorders. Several D3R-selective antagonists are effective in animal models of drug abuse, especially in models of relapse. Nevertheless, poor bioavailability, metabolic instability, and/or predicted toxicity have impeded success in translating these drug candidates to clinical use. Herein, we report a series of D3R-selective 4-phenylpiperazines with improved metabolic stability. A subset of these compounds was evaluated for D3R functional efficacy and off-target binding at selected 5-HT receptor subtypes, where significant overlap in SAR with D3R has been observed. Several high affinity D3R antagonists, including compounds 16 (Ki = 0.12 nM) and 32 (Ki = 0.35 nM), showed improved metabolic stability compared to the parent compound, PG648 (6). Notably, 16 and the classic D3R antagonist SB277011A (2) were effective in reducing self-administration of heroin in wild-type but not D3R knockout mice.
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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.