ArticleJournal of medicinal chemistry2011
Synthesis and pharmacological evaluation of fluorine-containing D₃ dopamine receptor ligands.
Article in Journal of medicinal chemistry, 2011. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 26 papers.
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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.
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Who cites it
26 citing papers in PubMed, 44 citations in OpenAlex.
- Design and Synthesis of DMolecules (Basel, Switzerland) · 2023Article
- Synthesis of bitopic ligands based on fallypride and evaluation of their affinity and selectivity towards dopamine DEuropean journal of medicinal chemistry · 2023Article
- Selective Activation of D3 Dopamine Receptors Ameliorates DOI-Induced Head Twitching Accompanied by Changes in Corticostriatal Processing.International journal of molecular sciences · 2023Article
- Design and Synthesis of Conformationally Flexible Scaffold as Bitopic Ligands for Potent DInternational journal of molecular sciences · 2022Article
- Characterization of Sigma-2 Receptor-Specific Binding Sites Using [Pharmaceuticals (Basel, Switzerland) · 2022Article
- Evaluation of SubstitutedMolecules (Basel, Switzerland) · 2021Article
- Interaction of Ligands for PET with the Dopamine D3 Receptor: In Silico and In Vitro Methods.Biomolecules · 2021Article
- Article
- Leveraging a Low-Affinity Diazaspiro Orthosteric Fragment to Reduce Dopamine DJournal of medicinal chemistry · 2019Article
- Selectivity of probes for PET imaging of dopamine D3 receptors.Neuroscience letters · 2019Review
- Insights From Molecular Dynamics Simulations of a Number of G-Protein Coupled Receptor Targets for the Treatment of Pain and Opioid Use Disorders.Frontiers in molecular neuroscience · 2019Review
- Dopamine D3 receptor partial agonist LS-3-134 attenuates cocaine-motivated behaviors.Pharmacology, biochemistry, and behavior · 2018Article
- Validation of gallbladder absorbed radiation dose reduction simulation: human dosimetry of [EJNMMI physics · 2018Article
- Synthesis and pre-clinical evaluation of a potential radiotracer for PET imaging of the dopamine DMedChemComm · 2018Article
- Automation of the Radiosynthesis of Six DifferentEJNMMI radiopharmacy and chemistry · 2017Article
- Pd-Catalyzed Synthesis of Piperazine Scaffolds Under Aerobic and Solvent-Free Conditions.Organic letters · 2016Article
- In Vitro and In Vivo Characterization of Selected Fluorine-18 Labeled Radioligands for PET Imaging of the Dopamine D3 Receptor.Molecules (Basel, Switzerland) · 2016Article
- Absorbed radiation dosimetry of the DAmerican journal of nuclear medicine and molecular imaging · 2016Article
- Identifying Medication Targets for Psychostimulant Addiction: Unraveling the Dopamine D3 Receptor Hypothesis.Journal of medicinal chemistry · 2015Article
- Characterization of [(3) H]LS-3-134, a novel arylamide phenylpiperazine D3 dopamine receptor selective radioligand.Journal of neurochemistry · 2014Article
Corrections and comments
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Authors and funding
8 authors at 3 institutions in 1 country.
Funding
Abstract
A series of fluorine-containing N-(2-methoxyphenyl)piperazine and N-(2-fluoroethoxy)piperazine analogues were synthesized, and their affinities for human dopamine D(2), D(3), and D(4) receptors were determined. Radioligand binding studies identified five compounds, 18a, 20a, 20c, 20e, and 21e, which bind with high affinity at D(3) (K(i) = 0.17-5 nM) and moderate to high selectivity for D(3) vs D(2) receptors (ranging from ∼25- to 163-fold). These compounds were also evaluated for intrinsic activity at D(2) and D(3) receptors using a forskolin-dependent adenylyl cyclase assay. This panel of compounds exhibits varying receptor subtype binding selectivity and intrinsic activity at D(2) vs D(3) receptors. These compounds may be useful for behavioral pharmacology studies on the role of D(2)-like dopamine receptors in neuropsychiatric and neurological disorders. Furthermore, compound 20e, which has the highest binding affinity and selectivity for the D(3) receptor (K(i) = 0.17 nM for D(3), 163-fold selectivity for D(3) vs D(2) receptors), represents a candidate fluorine-18 radiotracer for in vivo PET imaging studies on the regulation of D(3) receptor expression.
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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.