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- Volume 6, Issue 1, 2013
Current Radiopharmaceuticals - Volume 6, Issue 1, 2013
Volume 6, Issue 1, 2013
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Sodium-Proton Exchanger Isoform-1: Synthesis of a Potent Inhibitor Labeled with Deuterium and Carbon-14
Authors: Bachir Latli, Nizar Haddad, Matt Hrapchak, Xudong Wei, Wenjun Tang, Jinhua J. Song and Chris H. SenanayakeSodium-proton exchangers, NHEs are plasma membrane proteins that are essential in the regulation of intracellular pH of the myocardium. There are nine known variously expressed isoforms of NHEs with NHE-1 being the predominant isoform in the heart. N-[4-(1-acetyl-piperidin-4-yl)-3-trifluoromethyl-benzoyl]-guanidine (1) is a potent NHE 1inhibitor with good pharmacokinetics. It was prepared labeled with deuterium an Read More
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Synthesis and Evaluation of 99mTc Chelate-conjugated Bevacizumab
Vascular endothelial growth factor (VEGF) is one of the classic factors involved in tumor-induced angiognesis in several solid tumors. Bevacizumab, a monoclonal antibody against VEGF, can be used as an imaging tool in preclinical studies. The aim of this study was to radiolabel Bevacizumab with 99mTc and to evaluate in vivo its imaging properties in an adenocarcinoma animal model. For this purpose, Bevacizumab was deriv Read More
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Biodistribution and Dosimetry of 177Lu-tetulomab, a New Radioimmunoconjugate for Treatment of Non-Hodgkin Lymphoma
The biodistribution of the anti-CD37 radioimmunoconjugate 177Lu-tetraxetan-tetulomab (177Lu-DOTA-HH1) was evaluated. Biodistribution of 177Lu-tetraxetan-tetulomab was compared with 177Lu-tetraxetan-rituximab and free 177Lu in nude mice implanted with Daudi lymphoma xenografts. The data showed that 177Lu-tetulomab had a relevant stability and tumor targeting properties in the human lymphoma mo Read More
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A Novel 99mTc-labeled Diphosphonic Acid as Potential Bone Seeking Agent: Synthesis and Biological Evaluation
Authors: Ling Qiu, Wen Cheng, Jianguo Lin, Shu Zhang and Shineng LuoA novel zoledronate derivative, 1-hydroxy-4-(2-butyl-1H-imidazol-1-yl)butane-1,1- diyldiphosphonic acid (BIBDP) was prepared and labeled with 99mTc successfully in a high radiochemical purity and good stability in vitro. The biodistribution in mice shows that 99mTc-BIBDP has high specificity and efficacy in bone uptake with a maximum of 12.14 ± 0.53 %ID/g at 120 min. Kinetics of blood clearance showed that distribution half Read More
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Peptide Imaging with Somatostatin Analogues: More than Cancer Probes
Somastostatin (SS) scintigraphy (SRS) is an effective diagnostic tool for neuroendocrine tumours (NET). High diagnostic accuracy is based on the high affinity binding between SS and its receptors (sstr) expressed both in NET and in some non neoplastic cells. Different SS analogues have been proposed in clinical practice because of the short half-life of the native peptide. Among all synthetic compounds Pentetreotide labelled w Read More
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Bone Metastases Radiopharmaceuticals: An Overview
The skeleton is one of the preferential sites for metastases of solid tumors, and metastatic disease is the most common malignancy of the bone. Diagnosis and evaluation of skeletal metastases require more frequently a combined approach of different diagnostic methods. Between the currently available imaging modalities, a major role is devoted to two radionuclide functional techniques namely scintigraphy and positr Read More
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Some Implications of Receptor Kinase Signaling Pathway for Development of Multitargeted Kinase Inhibitors
More LessEpidermal growth factor receptors (EGFRs) belong to the ErbB family of receptor tyrosine kinases (TKs). Based on the role of EGFR signaling pathway in malignant progression of various types of tumors, a growing interest in the use of EGFR-TK inhibitors as probes for molecular imaging of EGFR-overexpressing tumors via positron emission tomography (PET) and single photon emission computed tomography (SPECT) is bein Read More
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