Radiosynthesis and Evaluation of 5-[I]Iodoindol-3-yl-β--Galactopyranoside as a β-Galactosidase Imaging Radioligand by Marcian E. Van Dort, Kuei C. Lee, Christin A. Hamilton, Alnawaz Rehemtulla, Brian D. Ross

“…The synthesis and investigation of 5-[ 125 I]iodoindol-3-yl-β- d -galactopyranoside ([ 125 I]IBDG) as a radioligand for single-photon emission computed tomography (SPECT) imaging of β-galactosidase expression are described. …”
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99mTc(CO)3-Labeled 1-(3-Nitropyridin-2-yl) Piperazine as Potential Radioligand for 5-HT7 Receptors by Sajjad Molavipordanjani

“…The calculated Bmax, and Kd of the radioligands were 48±9.23nM and 2.94±0.09×105. Conclusion: Compound 5 can be quantitatively radiolabeled with fac-[99mTc(CO)3(H2O)3]+  resulting in the radiotracer (99mTc(CO)3-[5]). …”
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Initial clinical experience with [177Lu]Lu-PNT2002 radioligand therapy in metastatic castration-resistant prostate cancer: dosimetry, safety, and efficacy from the lead-in cohort of the SPLASH trial by Aaron R. Hansen, Stephan Probst, Jean-Mathieu Beauregard, Benjamin L. Viglianti, Jeff M. Michalski, Scott T. Tagawa, Oliver Sartor, Ronald F. Tutrone, Orhan K. Oz, Kevin D. Courtney, Ebrahim S. Delpassand, Luke T. Nordquist, Medhat M. Osman, Kim N. Chi, Richard Sparks, Noble George, Sara M. Hawley, Wenting Wu, Jessica D. Jensen, Neil E. Fleshner

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FAP-targeted radioligand therapy with 68Ga/177Lu-DOTA-2P(FAPI)2 enhance immunogenicity and synergize with PD-L1 inhibitors for improved antitumor efficacy by Liang Zhao, Long Sun, Kaili Fu, Qin Lin, Xiaoyuan Chen, Qicong Luo, Hua Wu, Jianhao Chen, Yangfan Zhou, Yizhen Pang, Guoqiang Su, Haojun Chen

“…Background Fibroblast activation protein (FAP)-targeted radioligand therapy, with immunomodulatory effects, has shown efficacy in both preclinical and clinical studies. …”
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PSMA Theranostics: Current Status and Future Directions by Kambiz Rahbar MD, Ali Afshar-Oromieh MD, Hossein Jadvar MD, PhD, Hojjat Ahmadzadehfar MD, MSc

“…There is increasing evidence of encouraging response rates and a low toxicity profile of radioligand therapy (RLT) of metastatic castration-resistant prostate cancer using 177 Lu-labeled PSMA ligands. …”
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Do you know your PSMA-tracer? Variability in the biodistribution of different PSMA ligands and its potential impact on defining PSMA-positivity prior to PSMA-targeted therapy by Jan Heilinger, Katrin Sabine Roth, Henning Weis, Antonis Fink, Jasmin Weindler, Felix Dietlein, Philipp Krapf, Klaus Schomäcker, Bernd Neumaier, Markus Dietlein, Alexander Drzezga, Carsten Kobe

“…This may impact treatment decisions and outcomes, as eligibility for PSMA-directed radioligand therapy is usually assessed by comparing tumoral uptake to normal liver uptake as a reference. …”
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Comparison of Amino Acid Positron Emission Tomographic Radiotracers for Molecular Imaging of Primary and Metastatic Brain Tumors by Csaba Juhász, Shalini Dwivedi, David O. Kamson, Sharon K. Michelhaugh, Sandeep Mittal

“…We discuss both similarities and differences in potential clinical value for each radioligand. This comparative review can guide which radiotracer to favor in future clinical trials aimed at defining the role of these molecular imaging modalities in the clinical management of brain tumor patients.…”
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Norepinephrine Transporter Imaging in the Brain of a Rat Model of Depression Using Radioiodinated (2S, αS)-2-(α-(2-iodophenoxy)benzyl)morpholine by Naoki Kanegawa, Yasushi Kiyono, Taku Sugitaa, Yuji Kuge, Yasushisa Fujibayasi, Hideo Saji

“…To visualize the norepinephrine transporters (NETs) in various brain diseases, we developed radioiodinated (2S,αS)-2-(α-(2-iodophenoxy)benzyl)morpholine ((S,S)-IPBM). This radioligand achieved the basic requirements for NET imaging. …”
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Translocator Protein (18 kDa) Mapping with [I]-CLINDE in the Quinolinic Acid Rat Model of Excitotoxicity: A Longitudinal Comparison with Microglial Activation, Astrogliosis, and Ne... by Nicolas Arlicot, Claire Tronel, Sylvie Bodard, Lucette Garreau, Brice de la Crompe, Inge Vandevelde, Denis Guilloteau, Daniel Antier, Sylvie Chalon

“…Therefore, we performed ex vivo explorations with [ 125 ]-CLINDE, a TSPO-specific radioligand, to follow the time course of TSPO expression, in parallel with lesion progression, over 90 days after induction of cerebral excitotoxicity in rats intrastriatally injected with quinolinic acid. …”
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NMDA Receptor-Mediated Neuroprotective Effect of the Scutellaria baicalensis Georgi Extract on the Excitotoxic Neuronal Cell Death in Primary Rat Cortical Cell Cultures by Jinsong Yang, Xiaohong Wu, Haogang Yu, Xinbiao Liao, Lisong Teng

“…The extract exhibited a potent and dose-dependent inhibition of the glutamate-induced excitotoxicity in the culture media. Further, using radioligand binding assays, it was observed that the inhibitory effect of the extract was more potent and selective for the N-methyl-D-aspartate (NMDA) receptor-mediated toxicity. …”
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Oral Administration of the Endocannabinoid Anandamide during Lactation: Effects on Hypothalamic Cannabinoid Type 1 Receptor and Food Intake in Adult Mice by Carolina Aguirre, Valeska Castillo, Miguel Llanos

“…Capacity of hypothalamic membranes to specifically bind the radioligand 3[H]-CP55.940 was also measured. Western blots showed a 72% increase in CB1R abundance in AEA-treated 21-day-old mice, without differences in adult mice. …”
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Magnetic resonance imaging in primates. The example of the mouse lemur (Microcebus murinus): From detection of pathological aging to therapeutic evaluations by Nelly Joseph-Mathurin, Olene Dorieux, Audrey Kraska, Anne Bertrand, Mathieu Santin, Nadine El Tannir El Tayara, Marc Dhenain

“…In this case, MRI can be used as a support for quantification of radioligand uptake in specific structures. Ex vivo MR imaging is another MR protocol that can be used to describe cerebral aging in lemurs. …”
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PSMA PET/CT Identifies Intrapatient Variation in Salivary Gland Toxicity From Iodine-131 Therapy by Vineet Mohan MSc, Wouter V. Vogel MD, PhD, Gerlof D. Valk MD, PhD, Jan P. de Boer MD, PhD, Marnix G. E. H. Lam MD, PhD, Bart de Keizer MD, PhD

“…Methods: Five patients with differentiated thyroid cancer underwent [ 68 Ga]Ga-PSMA-11 PET/CT to evaluate their eligibility for peptide radioligand therapy with [ 177 Lu]Lu-PSMA-617. Uptake patterns in salivary glands were evaluated visually and quantitatively as an indicator of vital acinar cell loss after prior 131 I-therapy. …”
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Immunotargeting of Integrin αβ for Single-Photon Emission Computed Tomography and Near-Infrared Fluorescence Imaging in a Pancreatic Cancer Model by Winn Aung MBBS, PhD, Atsushi B. Tsuji PhD, Hitomi Sudo PhD, Aya Sugyo M.Ed, Takako Furukawa PhD, Yoshinori Ukai PhD, Yoshikazu Kurosawa PhD, Tsuneo Saga MD, PhD

“…BxPC-3 tumor showed a higher radioligand binding in SPECT and higher fluorescence intensity as well as a delay in the probe washout in NIR imaging when compared to A4 tumor. …”
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Comparison of HER2-Targeted Antibodies for Fluorescence-Guided Surgery in Breast Cancer by Solmaz AghaAmiri, Jo Simien, Alastair M. Thompson, Julie Voss, Sukhen C. Ghosh, Servando Hernandez Vargas, Sarah Kim, Ali Azhdarinia, Hop S. Tran Cao

“…In vitro findings demonstrated HER2-mediated binding for both fluorescent immunoconjugates and were in agreement with radioligand assays using dual-labeled immunoconjugates. …”
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PET Study of Sphingosine-1-Phosphate Receptor 1 Expression in Response to Vascular Inflammation in a Rat Model of Carotid Injury by Hui Liu PhD, MD, Hongjun Jin PhD, Xuyi Yue PhD, Junbin Han PhD, Pamela Baum SRS, Dana R. Abendschein PhD, Zhude Tu PhD

“…Here, we report in vivo validation of [ 11 C]TZ3321, a potent S1PR1 radioligand, for imaging vascular inflammation in a rat model of carotid injury. …”
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Radiocobalt-Labeling of a Polypyridylamine Chelate Conjugated to GE11 for EGFR-Targeted Theranostics by Lorraine Gaenaelle Gé, Mathias Bogetoft Danielsen, Aaraby Yoheswaran Nielsen, Mathias Lander Skavenborg, Niels Langkjær, Helge Thisgaard, Christine J. McKenzie

“…The overexpression of the epidermal growth factor receptor (EGFR) in certain types of prostate cancers and glioblastoma makes it a promising target for targeted radioligand therapy. In this context, pairing an EGFR-targeting peptide with the emerging theranostic pair comprising the Auger electron emitter cobalt-58m (^58mCo) and the Positron Emission Tomography-isotope cobalt-55 (⁵⁵Co) would be of great interest for creating novel radiopharmaceuticals for prostate cancer and glioblastoma theranostics. …”
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Fully Automated Production of (((<i>S</i>)-1-Carboxy-5-(6-([¹⁸F]fluoro)-2-methoxynicotinamido)pentyl)carbamoyl)-<span style="font-variant: small-caps">l</span>-glutamic... by Philipp Krapf, Thomas Wicher, Boris D. Zlatopolskiy, Johannes Ermert, Bernd Neumaier

“…<b>Conclusions:</b> We have established a highly reliable, GMP-compliant process for the automated radiosynthesis of [¹⁸F]JK-PSMA-7 on the Trasis AllinOne (AIO) synthesizer, ensuring consistent and efficient production of this radioligand.…”
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High SUVs Have More Robust Repeatability in Patients with Metastatic Prostate Cancer: Results from a Prospective Test-Retest Cohort Imaged with 18F-DCFPyL by Rudolf A. Werner, Bilêl Habacha, Susanne Lütje, Lena Bundschuh, Takahiro Higuchi, Philipp Hartrampf, Sebastian E. Serfling, Thorsten Derlin, Constantin Lapa, Andreas K. Buck, Markus Essler, Kenneth J. Pienta, Mario A. Eisenberger, Mark C. Markowski, Laura Shinehouse, Rehab AbdAllah, Ali Salavati, Martin A. Lodge, Martin G. Pomper, Michael A. Gorin, Ralph A. Bundschuh, Steven P. Rowe

“…In patients with prostate cancer (PC) receiving prostate-specific membrane antigen- (PSMA-) targeted radioligand therapy (RLT), higher baseline standardized uptake values (SUVs) are linked to improved outcome. …”
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Purinergic Receptors of the Central Nervous System: Biology, PET Ligands, and Their Applications by Hamideh Zarrinmayeh PhD, Paul R. Territo PhD

“…We have also reviewed receptors lacking radiotracer, laying the foundation for future discoveries of novel PET radioligands to reveal these receptors roles in CNS disorders.…”
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