ArticleJournal of medicinal chemistry2012
New positron emission tomography (PET) radioligand for imaging σ-1 receptors in living subjects.
Article in Journal of medicinal chemistry, 2012. The graph could read no effect estimate from its abstract, so it casts no vote on the map. It is linked to trial NCT02753101 (Biodistribution and Pharmacokinetic Determination of the PET Radiopharmaceutical [18F]FTC-146 Using PET/MRI in Healthy), which is not on this map. Cited by 55 papers.
What it found
Each row is one number read from the abstract, on the scale the paper reported it, with its interval. Left of the dashed line favours the treatment, right favours the comparator. Under each row is the sentence it came from. New to these charts? A ten-minute tutorial.
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.
Biodistribution and Pharmacokinetic Determination of the PET Radiopharmaceutical [18F]FTC-146 Using PET/MRI in Healthy (Asymptomatic) Volunteers and in Patients With CRPS and Sciatica
Who cites it
55 citing papers in PubMed.
- The SigmaPharmacological reports : PR · 2026Article
- Neuromelanin-targetedEJNMMI research · 2025Article
- A Full-Spectrum Evaluation of Sigma-1 Receptor (S1R) Positron Emission Tomography (PET) Radioligands from Binding Affinity to Clinical Imaging.Molecules (Basel, Switzerland) · 2025Review
- Development of Carbon-11 Labeled Pyrimidine Derivatives as Novel Positron Emission Tomography (PET) Agents Enabling Brain Sigma-1 Receptor Imaging.Advanced science (Weinheim, Baden-Wurttemberg, Germany) · 2025Article
- Recent Advances in the Development of Sigma Receptor (Radio)Ligands and Their Application in Tumors.ACS pharmacology & translational science · 2025Review
- Neuromelanin-targeted 18 F-P3BZA PET/MR imaging of the substantia nigra in rhesus macaques.EJNMMI research · 2024Article
- Imaging brain glucose metabolism in vivo reveals propionate as a major anaplerotic substrate in pyruvate dehydrogenase deficiency.Cell metabolism · 2024Article
- Imaging of Pain using Positron Emission Tomography.iRadiology · 2024Article
- Up-and-coming Radiotracers for Imaging Pain Generators.Seminars in musculoskeletal radiology · 2023Article
- Development and Initial Assessment of [Molecular imaging and biology · 2023Article
- Recent advances in drug discovery efforts targeting the sigma 1 receptor system: Implications for novel medications designed to reduce excessive drug and food seeking.Addiction neuroscience · 2023Article
- Sigma Receptor Ligands Prevent COVID Mortality In Vivo: Implications for Future Therapeutics.International journal of molecular sciences · 2023Article
- Discovery of RC-752, a Novel Sigma-1 Receptor Antagonist with Antinociceptive Activity: A Promising Tool for Fighting Neuropathic Pain.Pharmaceuticals (Basel, Switzerland) · 2023Article
- Candidate 3-benzazepine-1-ol type GluN2B receptor radioligands (EJNMMI research · 2023Article
- Evaluation of (Journal of nuclear medicine : official publication, Society of Nuclear Medicine · 2022Article
- Development of a PET radioligand for α2δ-1 subunit of calcium channels for imaging neuropathic pain.European journal of medicinal chemistry · 2022Article
- Comparison of three novel radiotracers for GluN2B-containing NMDA receptors in non-human primates:Journal of cerebral blood flow and metabolism : official journal of the International Society of Cerebral Blood Flow and Metabolism · 2022Article
- Characterization in nonhuman primates of (R)-[European journal of nuclear medicine and molecular imaging · 2022Article
- Knocking Out Sigma-1 Receptors Reveals Diverse Health Problems.Cellular and molecular neurobiology · 2022Review
- Examination of the Novel Sigma-1 Receptor Antagonist, SI 1/28, for Antinociceptive and Anti-allodynic Efficacy against Multiple Types of Nociception with Fewer Liabilities of Use.International journal of molecular sciences · 2022Article
Corrections and comments
PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.
Authors and funding
13 authors.
Funding
Abstract
σ-1 receptor (S1R) radioligands have the potential to detect and monitor various neurological diseases. Herein we report the synthesis, radiofluorination, and evaluation of a new S1R ligand 6-(3-fluoropropyl)-3-(2-(azepan-1-yl)ethyl)benzo[d]thiazol-2(3H)-one ([(18)F]FTC-146, [(18)F]13). [(18)F]13 was synthesized by nucleophilic fluorination, affording a product with >99% radiochemical purity (RCP) and specific activity (SA) of 2.6 ± 1.2 Ci/μmol (n = 13) at end of synthesis (EOS). Positron emission tomography (PET) and ex vivo autoradiography studies of [(18)F]13 in mice showed high uptake of the radioligand in S1R rich regions of the brain. Pretreatment with 1 mg/kg haloperidol (2), nonradioactive 13, or BD1047 (18) reduced the binding of [(18)F]13 in the brain at 60 min by 80%, 82%, and 81%, respectively, suggesting that [(18)F]13 accumulation in mouse brain represents specific binding to S1Rs. These results indicate that [(18)F]13 is a promising candidate radiotracer for further evaluation as a tool for studying S1Rs in living subjects.
Indexed as
Identifiers
What OpenQuestion holds
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.