Assessment of PSMA Targeting Ligands Bearing Novel Chelates with Application to Theranostics: Stability and Complexation Kinetics of 68Ga3+, 111In3+, 177Lu3+ and 225Ac3+
Recent successes in the treatment of metastatic castration-resistant prostate cancer (mCRPCa) by systemic endoradiotherapy has sparked renewed interest in developing small molecule ligands targeting prostate-specific membrane antigen (PSMA) and chelators capable of stable complexation of metal radionuclides for imaging and therapy. As the size and coordination number of metals for imaging, such as 68Ga3+, and for targeted therapy, such as 177Lu3+ and 225Ac3+, are substantially different, they may show a preference for macrocycles of different denticity. (Source: Nuclear Medicine and Biology)
Source: Nuclear Medicine and Biology - October 3, 2017 Category: Nuclear Medicine Authors: James M. Kelly, Alejandro Amor-Coarasa, Anastasia Nikolopoulou, Dohyun Kim, Clarence Williams, Shankar Vallabhajosula, John W. Babich Source Type: research
Consensus nomenclature rules for radiopharmaceutical chemistry — Setting the record straight
Over recent years, within the community of radiopharmaceutical sciences, there has been an increased incidence of incorrect usage of established scientific terms and conventions, and even the emergence of ‘self-invented’ terms. In order to address these concerns, an international Working Group on ‘Nomenclature in Radiopharmaceutical Chemistry and related areas’ was established in 2015 to achieve clarification of terms and to generate consensus on the utilisation of a standardised nomenclature pertinent to the field. (Source: Nuclear Medicine and Biology)
Source: Nuclear Medicine and Biology - October 2, 2017 Category: Nuclear Medicine Authors: Heinz H. Coenen, Antony D. Gee, Michael Adam, Gunnar Antoni, Cathy S. Cutler, Yasuhisa Fujibayashi, Jae Min Jeong, Robert H. Mach, Thomas L. Mindt, Victor W. Pike, Albert D. Windhorst Source Type: research
Consensus nomenclature rules for radiopharmaceutical chemistry – setting the record straight
Over recent years, within the community of radiopharmaceutical sciences, there has been an increased incidence of incorrect usage of established scientific terms and conventions, and even the emergence of ‘self-invented’ terms. In order to address these concerns, an international Working Group on ‘Nomenclature in Radiopharmaceutical Chemistry and related areas’ was established in 2015 to achieve clarification of terms and to generate consensus on the utilisation of a standardised nomenclature pertinent to the field. (Source: Nuclear Medicine and Biology)
Source: Nuclear Medicine and Biology - October 2, 2017 Category: Nuclear Medicine Authors: Heinz H. Coenen, Antony D. Gee, Michael Adam, Gunnar Antoni, Cathy S. Cutler, Yasuhisa Fujibayashi, Jae Min Jeong, Robert H. Mach, Thomas L. Mindt, Victor W. Pike, Albert D. Windhorst Source Type: research
Editorial Board
(Source: Nuclear Medicine and Biology)
Source: Nuclear Medicine and Biology - September 19, 2017 Category: Nuclear Medicine Source Type: research
Table of Contents
(Source: Nuclear Medicine and Biology)
Source: Nuclear Medicine and Biology - September 19, 2017 Category: Nuclear Medicine Source Type: research
Astatine-211 Labeled Anti-HER2 5F7 Single Domain Antibody Fragment Conjugates: Radiolabeling and Preliminary Evaluation
This study evaluated two reagents, [211At]SAGMB and iso-[211At]SAGMB, for this purpose. (Source: Nuclear Medicine and Biology)
Source: Nuclear Medicine and Biology - September 18, 2017 Category: Nuclear Medicine Authors: Jaeyeon Choi, Ganesan Vaidyanathan, Eftychia Koumarianou, Choong Mo Kang, Michael R. Zalutsky Source Type: research
Preclinical evaluation of heat-denatured [18F]FDG-labeled red blood cells for detecting splenic tissues with PET in rats
Heat-denatured 99mTc-labeled red blood cells (RBCs) are used for detecting splenic tissues with scintigraphy. The present study aimed to evaluate the feasibility of using heat-denatured [18F]fluorodeoxyglucose ([18F]FDG)-labeled RBCs in detecting splenic tissues using positron emission tomography (PET) in rats. (Source: Nuclear Medicine and Biology)
Source: Nuclear Medicine and Biology - September 16, 2017 Category: Nuclear Medicine Authors: Yohji Matsusaka, Tadaki Nakahara, Kazuhiro Takahashi, Yu Iwabuchi, Yuji Ogata, Chiyoko Nishime, Mayumi Kajimura, Masahiro Jinzaki Tags: Original article Source Type: research
[99mTc]duramycin for cell death imaging: impact of kit formulation, purification and species difference
[99mTc]duramycin is a SPECT tracer for cell death imaging. We evaluated the impact of kit formulation, purification and species difference on the pharmacokinetic profile and cell death targeting properties of [99mTc]duramycin in order to define the optimal conditions for (pre-)clinical use. (Source: Nuclear Medicine and Biology)
Source: Nuclear Medicine and Biology - September 13, 2017 Category: Nuclear Medicine Authors: Luca Palmieri, Filipe Elvas, Christel Vangestel, Koon Pak, Brian Gray, Sigrid Stroobants, Steven Staelens, Leonie Wyffels Source Type: research
DOTA-Tetrazine Probes with Modified Linkers for Tumor Pretargeting
Pretargeted radioimmunoimaging and -therapy approaches building on the bioorthogonal inverse-electron-demand Diels-Alder (IEDDA) reaction between strained trans-cyclooctenes (TCO) and electron-deficient tetrazines (Tz) have yielded impressive results in recent years and have proven a vital alternative to biological pretargeting systems. After improvement of the TCO-antibody conjugates, we here report on our evaluation of a new series of radiolabeled Tz-probes. (Source: Nuclear Medicine and Biology)
Source: Nuclear Medicine and Biology - September 13, 2017 Category: Nuclear Medicine Authors: Tilman L äppchen, Raffaella Rossin, Tiemen R. van Mourik, Guillaume Gruntz, Freek J.M. Hoeben, Ron M. Versteegen, Henk M. Janssen, Johan Lub, Marc S. Robillard Source Type: research
Is LogP Truly Dead?
More than 100 years ago, the importance of lipophilicity to the passive permeability of molecules through the blood-brain-barrier was recognized. In the intervening decades, various methods to measure the lipid nature of molecules were developed; with an ever-expanding database on molecule structures and measured physiochemical properties, computational methods for estimation of lipophilicity followed. Today, the simple estimate of lipophilicity known as the logP value (in its original definition, the logarithm of the distribution ratio for a molecule between immiscible organic and aqueous layers) is routinely used in drug...
Source: Nuclear Medicine and Biology - September 9, 2017 Category: Nuclear Medicine Authors: Michael R. Kilbourn, Peter J.H. Scott Source Type: research
A Six-Year Longitudinal PET Study of (+)-[11C]DTBZ Binding to the VMAT2 in Monkey Brain
The longitudinal reproducibility of in vivo binding potential measures for [11C]dihydrotetrabenazine ([11C]DTBZ) binding to the vesicular monoamine transporter 2 (VMAT2) site in primate brain was examined using a unique dataset of repeated control PET imaging studies. (Source: Nuclear Medicine and Biology)
Source: Nuclear Medicine and Biology - September 5, 2017 Category: Nuclear Medicine Authors: Michael R. Kilbourn, Robert A. Koeppe Source Type: research
Reconsider logP!
In our view, it is essential to start a general balanced but unprejudiced discussion on power and limitations of methods and predictive models in radiopharmacy. We fully agree, that lipophilicity has a significant impact on the pharmacokinetic properties of radiopharmaceuticals, and we literally stated in our manuscript: “In drug development, especially for central applications, the lipophilicity is a pivotal and early indicator of the potential in vivo pharmacokinetic and dynamic behaviour. Lipophilicity measurements, as it is widely known, provide information about unspecific binding, metabolic stability, plasma protei...
Source: Nuclear Medicine and Biology - September 1, 2017 Category: Nuclear Medicine Authors: Chrysoula Vraka, Markus Mitterhauser Source Type: research
Cross-sectional and longitudinal small animal PET shows pre and post-synaptic striatal dopaminergic deficits in an animal model of HIV
In vivo imaging biomarkers of various HIV neuropathologies, including dopaminergic dysfunction, are still lacking. Towards developing dopaminergic biomarkers of brain involvement in HIV, we assessed the pre and postsynaptic components of the dopaminergic system in the HIV-1 transgenic rat (Tg), a well-characterized model of treated HIV+ patients, using small-animal PET imaging. (Source: Nuclear Medicine and Biology)
Source: Nuclear Medicine and Biology - August 29, 2017 Category: Nuclear Medicine Authors: Sanhita Sinharay, Dianne Lee, Swati Shah, Siva Muthusamy, Georgios Z. Papadakis, Xiang Zhang, Dragan Maric, William C. Reid, Dima A. Hammoud Source Type: research
Comparison between [18F]fluorination and [18F]fluoroethylation reactions for the synthesis of the PDE10A PET radiotracer [18F]MNI-659
2-(2-(3-(4-(2-[18F]Fluoroethoxy)phenyl)-7-methyl-4-oxo-3,4-dihydroquinazolin-2-yl)ethyl)-4-isopropoxyisoindoline-1,3-dione ([18F]MNI-659, [18F]1) is a useful PET radiotracer for imaging phosphodiesterase 10A (PDE10A) in human brain. [18F]1 has been previously prepared by direct [18F]fluorination of a tosylate precursor 2 with [18F]F-. The aim of this study was to determine the conditions for the [18F]fluorination reaction to obtain [18F]1 of high quality and with sufficient radioactivity for clinical use in our institute. (Source: Nuclear Medicine and Biology)
Source: Nuclear Medicine and Biology - August 25, 2017 Category: Nuclear Medicine Authors: Wakana Mori, Makoto Takei, Kenji Furutsuka, Masayuki Fujinaga, Katsushi Kumata, Masatoshi Muto, Takayuki Ohkubo, Hiroki Hashimoto, Gilles Tamagnan, Makoto Higuchi, Kazunori Kawamura, Ming-Rong Zhang Source Type: research
In Vitro Uptake and Metabolism of [14C]Acetate in Rabbit Atherosclerotic Arteries: Biological Basis for Atherosclerosis Imaging with [11C]Acetate
Detection of vulnerable plaques is critically important for the selection of appropriate treatment and/or the prevention of atherosclerosis and ensuing cardiovascular diseases. In order to clarify the utility of [11C]acetate for atherosclerosis imaging, we determined the uptake and metabolism of acetate by in vitro studies using rabbit atherosclerotic arteries and [14C]acetate. (Source: Nuclear Medicine and Biology)
Source: Nuclear Medicine and Biology - August 24, 2017 Category: Nuclear Medicine Authors: Kazuaki Yamasaki, Atsushi Yamashita, Yan Zhao, Yoichi Shimizu, Ryuichi Nishii, Keiichi Kawai, Nagara Tamaki, Songji Zhao, Yujiro Asada, Yuji Kuge Source Type: research
