ArticleSynapse (New York, N.Y.)2015
Dopamine D3 receptor binding of (18)F-fallypride: Evaluation using in vitro and in vivo PET imaging studies.
Article in Synapse (New York, N.Y.), 2015. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 21 papers.
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Who cites it
21 citing papers in PubMed, 27 citations in OpenAlex.
- The Binding of the High Affinity Radioligand Fallypride to the D2-dopamine Receptor is Sensitive to Injected Mass - a PET Study in Rodents.Molecular imaging and biology · 2026Article
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- Dopamine D2 receptor upregulation in dorsal striatum in the LRRK2-R1441C rat model of early Parkinson's disease revealed by in vivo PET imaging.Scientific reports · 2025Article
- Dopamine D3 Receptor in Parkinson Disease: A Prognosis Biomarker and an Intervention Target.Current topics in behavioral neurosciences · 2023Article
- Design and Synthesis of Conformationally Flexible Scaffold as Bitopic Ligands for Potent DInternational journal of molecular sciences · 2022Article
- Exercise against cocaine sensitization in mice: a [Brain communications · 2022Article
- [Frontiers in neuroscience · 2021Article
- Quantitative Rodent Brain Receptor Imaging.Molecular imaging and biology · 2020Review
- Dopamine D3 receptor: A neglected participant in Parkinson Disease pathogenesis and treatment?Ageing research reviews · 2020Review
- Partial-volume correction increases estimated dopamine D2-like receptor binding potential and reduces adult age differences.Journal of cerebral blood flow and metabolism : official journal of the International Society of Cerebral Blood Flow and Metabolism · 2019Article
- Expression of dopamine D2 and D3 receptors in the human retina revealed by positron emission tomography and targeted mass spectrometry.Experimental eye research · 2018Article
- Synthesis and pre-clinical evaluation of a potential radiotracer for PET imaging of the dopamine DMedChemComm · 2018Article
- [Molecules (Basel, Switzerland) · 2018Article
- Low Striatal Dopamine D2-type Receptor Availability is Linked to Simulated Drug Choice in Methamphetamine Users.Neuropsychopharmacology : official publication of the American College of Neuropsychopharmacology · 2018Article
- Performing multi-step chemical reactions in microliter-sized droplets by leveraging a simple passive transport mechanism.Lab on a chip · 2017Article
- PET radiotracer development for imaging high-affinity state of dopamine D2 and D3 receptors: Binding studies of fluorine-18 labeled aminotetralins in rodents.Synapse (New York, N.Y.) · 2017Article
- Sex Differences in Midbrain Dopamine D2-Type Receptor Availability and Association with Nicotine Dependence.Neuropsychopharmacology : official publication of the American College of Neuropsychopharmacology · 2016Article
- Cigarette Use and Striatal Dopamine D2/3 Receptors: Possible Role in the Link between Smoking and Nicotine Dependence.The international journal of neuropsychopharmacology · 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
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Authors and funding
6 authors at 1 institution in 1 country.
Funding
Abstract
Identification of dopamine D3 receptors (D3R) in vivo is important to understand several brain functions related to addiction. The goal of this work was to identify D3R binding of the dopamine D2 receptor (D2R)/D3R imaging agent, (18)F-fallypride. Brain slices from male Sprague-Dawley rats (n = 6) and New Zealand White rabbits (n = 6) were incubated with (18)F-fallypride and D3R selective agonist (R)-7-OH-DPAT (98-fold D3R selective). Rat slices were also treated with BP 897 (68-fold D3R selective partial agonist) and NGB 2904 (56-fold D3R selective antagonist). In vivo rat studies (n = 6) were done on Inveon PET using 18-37 MBq (18)F-fallypride and drug-induced displacement by (R)-7-OH-DPAT, BP 897 and NGB 2904. PET/CT imaging of wild type (WT, n = 2) and D2R knock-out (KO, n = 2) mice were carried out with (18)F-fallypride. (R)-7-OH-DPAT displaced binding of (18)F-fallypride, both in vitro and in vivo. In vitro, at 10 nM (R)-7-OH-DPAT, (18)F-fallypride binding in the rat ventral striatum (VST) and dorsal striatum (DST) and rabbit nucleus accumbens were reduced by ∼10-15%. At 10 μM (R)-7-OH-DPAT all regions in rat and rabbit were reduced by ≥85%. In vivo reductions for DST and VST before and after (R)-7-OH-DPAT were: low-dose (0.015 mg kg(-1)) DST -22%, VST -29%; high-dose (1.88 mg kg(-1)) DST -58%, VST -77%, suggesting D3R/D2R displacement. BP 897 and NGB 2904 competed with (18)F-fallypride in vitro, but unlike BP 897, NGB 2904 did not displace (18)F-fallypride in vivo. The D2R KO mice lacked (18)F-fallypride binding in the DST. In summary, our findings suggest that up to 20% of (18)F-fallypride may be bound to D3R sites in vivo.
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