Despite its abundant expression in the brain, the cannabinoid type-1 (CB1) receptor was discovered only in 1988. During the last decade, efforts from several research groups have made it possible to visualize the CB1 receptor in vivo to unravel its role in the brain physiology and pathology. This review discusses strategies for (radio)synthesis of radioligands for in vivo imaging of CB1 receptors.
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http://dx.doi.org/10.1002/jlcr.3017 | DOI Listing |
J Immunother Cancer
January 2025
Department of Nuclear Medicine and Minnan PET Center, Xiamen Cancer Center, The First Affiliated Hospital of Xiamen University, School of Medicine, Xiamen University, Xiamen, Fujian, China
Background: Fibroblast activation protein (FAP)-targeted radioligand therapy, with immunomodulatory effects, has shown efficacy in both preclinical and clinical studies. We recently reported on a novel dimeric FAP-targeting radiopharmaceutical, Ga/Lu-DOTA-2P(FAPI), which demonstrated increased tumor uptake and prolonged retention in various cancers. However, further exploration is required to understand the therapeutic efficacy and underlying mechanisms of combining Ga/Lu-DOTA-2P(FAPI) radioligand therapy with PD-1/PD-L1 immunotherapy.
View Article and Find Full Text PDFJ Med Chem
January 2025
Department of Radiology, University of Pennsylvania, Philadelphia, Pennsylvania 19104, United States.
Radioactive prostate-specific membrane antigen (PSMA)-targeting agents are clinically useful for the diagnosis and treatment of patients with PSMA-positive metastatic castration-resistant prostate cancer (mCRPC). Neuroendocrine-differentiated prostate cancer (NEPC), a highly aggressive subtype that is strongly associated with a poor clinical prognosis, may present with reduced PSMA expression and evade detection with PSMA-targeted agents. Several studies have shown elevated uptake of somatostatin receptor 2 (SSTR2) ligands in PSMA-negative NEPC.
View Article and Find Full Text PDFChemMedChem
January 2025
Universitatsspital Basel, Radiopharmazeutische Chemie, Petersgraben 4, 4031, Basel, SWITZERLAND.
The C-X-C chemokine receptor 4 (CXCR4) is highly upregulated in most cancers, making it an ideal target for delivering radiation therapy to tumors. We previously demonstrated the feasibility of targeting CXCR4 in vivo using a radiolabeled derivative of EPI-X4, an endogenous CXCR4 antagonist, named DOTA-K-JM#173. However, this derivative showed undesirable accumulation in the kidneys, which would limit its clinical use.
View Article and Find Full Text PDFEur J Nucl Med Mol Imaging
January 2025
Department of Nuclear Medicine, Xiangya Hospital, Central South University, Changsha, 410008, P.R. China.
Purpose: Temporal lobe epilepsy (TLE) is a brain network disorder closely associated with synaptic loss and has a genetic basis. However, the in vivo whole-brain synaptic changes at the network-level and the underlying gene expression patterns in patients with TLE remain unclear.
Methods: In this study, we utilized a positron emission tomography with the synaptic vesicle glycoprotein 2 A radioligand [F]SynVesT-1 cohort and two independent transcriptome datasets to investigate the topological properties of the synaptic density similarity network (SDSN) in TLE and its correlation with significantly dysregulated risk genes.
Pharmaceuticals (Basel)
November 2024
Department of Nuclear Medicine, Medical University of Innsbruck, 6020 Innsbruck, Austria.
: Dual-modality probes, combining positron emission tomography (PET) with fluorescence imaging (FI) capabilities in a single molecule, are of high relevance for the accurate staging and guided resection of tumours. We herein present a pair of candidates targeting the cholecystokinin-2 receptor (CCK2R), namely [Ga]Ga-CyTMG and [Ga]Ga-CyFMG. In these probes, the SulfoCy5.
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