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http://dx.doi.org/10.1007/s00259-017-3868-0 | DOI Listing |
ACS Omega
August 2025
Institute of Organic Chemistry, Johannes Kepler University Linz, Altenberger Straße 69, 4040 Linz, Austria.
The P2X receptor is an emerging target for molecular imaging of inflammation in the brain and peripheral tissues. In this work, we focus on five triazole-based ligands with high affinity and selectivity for P2X receptors (, , , , and ), which are amenable to autoradiography and positron emission tomography (PET) imaging. We studied the phenomenon of conformational and rotational changes of these molecules by NMR and calculations.
View Article and Find Full Text PDFMol Divers
August 2025
Department of Radiological Medicine and Oncology, College of Basic Medical Sciences, Chongqing Medical University, Chongqing, 400016, People's Republic of China.
Cyclooxygenase-2 (COX-2) plays vital roles in promoting angiogenesis, tissue invasion, and resistance to apoptosis, so it has become an attractive biomarker for imaging and therapy of cancer. Numerous radio-tracers for detection of COX-2 in vivo have been reported, but no one has been successfully applied in clinic. In this study, the radiosynthesis and evaluation of [F]6, containing a 1,5-diarylpyrrole structure, as a radiotracer for imaging of COX-2 is described.
View Article and Find Full Text PDFJ Med Chem
August 2025
Department of Chemistry, UBC, 2036 Main Mall, Vancouver, BC V6T 1Z1, Canada.
Dual-mode fluorescent PET tracers for imaging prostate cancer hold promise for coordinating preoperative PET imaging with intraoperative surgical imaging applications. Here, we disclose two PET tracers containing three key design elements: (1) an organotrifluoroborate for one-step radiofluorination at Curie levels of [F] fluoride in good yields and high molar activity (A) values: 42-167 GBq/μmol, (2) two fluorescein moieties (FAM and FITC) for fluorescent visualization, and (3) two pharmacophores based on clinically validated scaffolds PSMA-617 and PSMA-1007. These tracers are the first-ever examples of dual-mode PSMA-targeting agents that are labeled with both fluorescein and fluorine-18.
View Article and Find Full Text PDFJ Orthop Surg Res
May 2025
Department of Orthopaedic Surgery, Maastricht University Medical Center, Maastricht, The Netherlands.
Purpose: Posterior Lumbar Interbody Fusion (PLIF) is a surgical procedure in which stabilization of spinal segments is achieved by inserting interbody cages filled with bone graft. Positron Emission Tomography (PET) is an imaging modality to assess physiological processes at cellular level, well before manifestation of morphological changes on computed tomography (CT). The goal was to determine whether F-fluoride PET/CT findings six weeks after PLIF, can predict bony fusion one year postoperatively on CT.
View Article and Find Full Text PDFInt J Mol Sci
March 2025
Department Radiopharmaceutical and Chemical Biology, Institute of Radiopharmaceutical Cancer Research, Helmholtz-Zentrum Dresden-Rossendorf, Bautzner Landstrasse 400, 01328 Dresden, Germany.
The inducible enzyme cyclooxygenase-2 (COX-2) and the subsequent synthesis of eicosanoids initiated by this enzyme are important molecular players in bone healing. In this pilot study, the suitability of a novel selective COX-2 inhibitor bearing a nitric oxide (NO)-releasing moiety was investigated as a modulator of healing a critical-size bone defect in rats. A 5 mm femoral defect was randomly filled with no material (negative control, NC), a mixture of collagen and autologous bone fragments (positive control, PC), or polycaprolactone-co-lactide (PCL)-scaffolds coated with two types of artificial extracellular matrix (aECM; collagen/chondroitin sulfate (Col/CS) or collagen/polysulfated hyaluronic acid (Col/sHA3)).
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