ArticleMolecules (Basel, Switzerland)2016
Evaluation of the Enantiomer Specific Biokinetics and Radiation Doses of [(18)F]Fluspidine-A New Tracer in Clinical Translation for Imaging of σ₁ Receptors.
Article in Molecules (Basel, Switzerland), 2016. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 18 papers.
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Who cites it
18 citing papers in PubMed.
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- Design, synthesis, and characterization of F-18 sigma-1 receptor radiotracers for Alzheimer disease.European journal of medicinal chemistry · 2026Article
- A Full-Spectrum Evaluation of Sigma-1 Receptor (S1R) Positron Emission Tomography (PET) Radioligands from Binding Affinity to Clinical Imaging.Molecules (Basel, Switzerland) · 2025Review
- [¹⁸F]Fluspidine PET/CT imaging to assess postoperative pain-associated σ1 receptor expression in female rats under analgesia.European radiology experimental · 2025Article
- Recent Advances in the Development of Sigma Receptor (Radio)Ligands and Their Application in Tumors.ACS pharmacology & translational science · 2025Review
- [Pharmaceuticals (Basel, Switzerland) · 2024Review
- The Sigma Receptors in Alzheimer's Disease: New Potential Targets for Diagnosis and Therapy.International journal of molecular sciences · 2023Review
- Propellanes as Rigid Scaffolds for the Stereodefined Attachment of σ-Pharmacophoric Structural Elements to Achieve σ Affinity.International journal of molecular sciences · 2021Article
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- A perspective on the radiopharmaceutical requirements for imaging and therapy of glioblastoma.Theranostics · 2021Review
- Preclinical Incorporation Dosimetry of [Molecules (Basel, Switzerland) · 2020Article
- Imaging Sigma-1 Receptor (S1R) Expression Using Iodine-124-Labeled 1-(4-Iodophenyl)-3-(2-adamantyl)guanidine ([Molecular imaging and biology · 2020Article
- Approaches to PET Imaging of Glioblastoma.Molecules (Basel, Switzerland) · 2020Review
- Article
- Bridging from Brain to Tumor Imaging: (S)-(-)- and (R)-(+)-[Molecules (Basel, Switzerland) · 2018Article
- Synthesis, radiolabelling, and evaluation of [American journal of nuclear medicine and molecular imaging · 2018Article
- Biodistribution and Radiation Dosimetry ofJournal of nuclear medicine : official publication, Society of Nuclear Medicine · 2017Article
- Radiosynthesis and First-In-Human PET/MRI Evaluation with Clinical-Grade [Molecular imaging and biology · 2017Article
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Authors and funding
13 authors.
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No grant is acknowledged in the PubMed record.
Abstract
The enantiomers of [(18)F]fluspidine, recently developed for imaging of σ₁ receptors, possess distinct pharmacokinetics facilitating their use in different clinical settings. To support their translational potential, we estimated the human radiation dose of (S)-(-)-[(18)F]fluspidine and (R)-(+)-[(18)F]fluspidine from ex vivo biodistribution and PET/MRI data in mice after extrapolation to the human scale. In addition, we validated the preclinical results by performing a first-in-human PET/CT study using (S)-(-)-[(18)F]fluspidine. Based on the respective time-activity curves, we calculated using OLINDA the particular organ doses (ODs) and effective doses (EDs). The ED values of (S)-(-)-[(18)F]fluspidine and (R)-(+)-[(18)F]fluspidine differed significantly with image-derived values obtained in mice with 12.9 μSv/MBq and 14.0 μSv/MBq (p < 0.025), respectively. A comparable ratio was estimated from the biodistribution data. In the human study, the ED of (S)-(-)-[(18)F]fluspidine was calculated as 21.0 μSv/MBq. Altogether, the ED values for both [(18)F]fluspidine enantiomers determined from the preclinical studies are comparable with other (18)F-labeled PET imaging agents. In addition, the first-in-human study confirmed that the radiation risk of (S)-(-)-[(18)F]fluspidine imaging is within acceptable limits. However, as already shown for other PET tracers, the actual ED of (S)-(-)-[(18)F]fluspidine in humans was underestimated by preclinical imaging which needs to be considered in other first-in-human studies.
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