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Journal of Labelled Compounds & Radiopharmaceuticals

M A Motaleb, I T Ibrahim, M O Sarhan, W A Zaghary
A newly synthesized s-triazine derivative 1,1',1"-(((1,3,5-triazine-2,4,6-triyl) tris (azanediyl)) tris (benzene-4,1-diyl))tris (ethan-1-one), (1), was synthesized as a part of an ongoing research for development of novel s-triazine based radiopharmaceuticals. In-vitro cell viability assay against different human cancer cell lines showed very promising inhibitory activity of the synthesized compound. This findings encouraged the radioiodination of 1 to study the degree of its localization in tumor site for evaluating the possibility of its use as a tumor imaging agent...
September 7, 2018: Journal of Labelled Compounds & Radiopharmaceuticals
Soumen Das, Anupam Mathur, Navin Sakhare, Madhava B Mallia, H D Sarma, S S Sachdev, A Dash
123 I-Iodophenylpentadecanoic acid (IPPA) is a metabolic agent used in nuclear medicine for diagnosis of myocardial defects. Efforts are underway worldwide to develop a 99m Tc substitute of the above radiopharmaceutical for the aforementioned application. Herein, we report synthesis and biodistribution studies of 99m Tc labeled fatty acids (8, 11 and 15 carbons) obtained via 'click chemistry' for its potential use in myocardial imaging. ω-Bromo fatty acids (8C/11C/15C) were synthetically modified at bromo terminal to introduce a heterocyclic triazole with glycine sidearm in a five step procedure...
September 1, 2018: Journal of Labelled Compounds & Radiopharmaceuticals
Brad D Maxwell
The isotopic labeling of molecules for agrichemical and pharmaceutical uses is becoming more challenging as molecules become larger, involve more stereochemistry and as intellectual property rights become more complex. As such, isotope chemists need to continually add new isotopic methods to their armamentarium to successfully label complex molecules with carbon-13 and carbon-14. Recently, there has been a surge in the use of radicals to form new carbon-carbon bonds and for the incorporation of functional groups which can be used to incorporate isotopically labeled carbons...
August 29, 2018: Journal of Labelled Compounds & Radiopharmaceuticals
Wulian Chen, Chaomin Zhao, Xiaojun Deng
An efficient and simple synthetic route of deuterium-labeled 2-quinoxalinecarboxylic acid-d4 (QCA-d4 ) and 3-methylquinoxaline-2-carboxylic acid-d4 (MQCA-d4 ) is presented with 99.9% and 99.6% isotopic enrichment using aniline-d5 as labeled starting material. Their chemical structures were confirmed by 1 H NMR, and their isotopic abundance was determined by mass spectrometry analysis.
August 21, 2018: Journal of Labelled Compounds & Radiopharmaceuticals
Wangwei Ao, Yuan Li, Yinsheng Zhang
To more accurately and rapidly achieve quantitative detection of clinical crizotinib samples, stable isotope labeled crizotinib was required as an internal standard. We have developed a method to prepare racemic [D9 ] crizotinib using a base-catalyzed H/D exchange of both nitroso compound 2 and the acetophenone compound 6 with D2 O and NaBD4 reduction of 7 as the key steps to introduce the 9 deuterium atoms. Starting with 4-hydroxypiperidine, 14-step synthesis furnished the desired racemic [D9 ] crizotinib 18...
August 17, 2018: Journal of Labelled Compounds & Radiopharmaceuticals
Masoumeh Zoghi, Sima Attar Nosrati, Faramarz Rogni, Saaed Rajabifar
The new GnRH-Ιanalogue developed in this paper was based on the D-Trp6 -GnRH-Ι-scaffold, and its potency was increased by the replacement Gly-NH2 by NH-NH2 binding to the Gly at position 10. Triptorelin-Hydrazide analogue was synthesized using solid phase. For 111 In labeling, synthesized peptide was followed by conjugation with DOTA using pSCN-Bn-DOTA. The conjugated Triptorelin-Hydrazide was labeled with 500-550 MBq of 111 In-chloride (in 0.2 M HCl). At optimized conditions after labeling, radio-chromatography showed radiochemical purity of approximately equal to 98% (RTLC) and greater than 95% (HPLC)...
August 14, 2018: Journal of Labelled Compounds & Radiopharmaceuticals
Seth Jones, Remo Weck, Annina Burhop, Jens Atzrodt, Volker Derdau
Radiolabelled azidophenyl analogues can make powerful photoaffinity probes for the identification of molecular targets. We describe our efforts to prepare tritiated azidophenyl analogues of the taxols cabazitaxel and docetaxel. Late-stage tritiation by isotope exchange with diiodo precursors resulted in reduction of the azide moiety, which could only be overcome by addition of high excess of a sacrificial azide. Iodine-deuterium exchange experiments on a model system established that deiodination with concomitant azide reduction is a general problem when performing such isotope-exchange reactions on azide-containing aryl iodides...
August 12, 2018: Journal of Labelled Compounds & Radiopharmaceuticals
Daniel P Holt, Alvin S Kalinda, Lauren E Bambarger, Sanjay K Jain, Robert F Dannals
In this practitioner protocol, the radiochemical synthesis of [11 C] PABA is described in detail, and a quality control summary of three validation productions is presented. The results indicate that the radiotracer product can be produced in good radiochemical yield (14% at end-of-synthesis (EOS)) at high specific activity (molar activity 11 Ci/μmole EOS; 407 GBq/μmole) and high chemical and radiochemical purity as a sterile, pyrogen-free solution suitable for injection conforming to current Good Manufacturing Practice (cGMP) requirements...
August 8, 2018: Journal of Labelled Compounds & Radiopharmaceuticals
Hung-Man Yu, Chen-Hsin Chan, Jyun-Hong Chen, Chuan-Yi Chien, Ping-Yen Wang, Wei-Cheng Juan, Chun-Hung Yang, Hao-Ting Hsia, Mei-Hui Wang, Wuu-Jyh Lin
The aim of this study was to formulate and evaluate the freeze-dried kit of NOTA-hexavalent lactoside (NOTA-HL) for the preparation of 68 Ga-labeled glycoligand for PET imaging of the asialoglycoprotein receptor (ASGPR). 68 GaCl3 was obtained from a commercial 68 Ge/68 Ga generator. Single-vial kits of HL were formulated. Optimization of radiolabeling with 68 Ga, various evaluations of NOTA-HL kits, and in vitro stability study of 68 Ga-HL were carried out. PET/CT imaging of normal mice injected with 68 Ga-NOTA-HL was performed...
August 8, 2018: Journal of Labelled Compounds & Radiopharmaceuticals
Nicolas Philippe, Luc Rivron, Béatrice De Bruin, Joseph Schofield, Sébastien Roy
Carbon-14 labeled (6E,10E,14E,18E)-2,6,10,15,19,23-hexamethyltetracosa-2,6,10,14,18,22-hexaene, also known as squalene, was synthesized as a tool for pharmacokinetic studies. Two simple and efficient labeling approaches were developed to give [2-14 C]-squalene and [3-14 C]-squalene from a halogenated precursor derived from turbinaric acid. They were obtained in 13.5% radiochemical yield in 6 steps and in 38% radiochemical yield in 3 steps respectively from carbon-14 labeled potassium cyanide with a radiochemical purity higher than 98% in both cases...
August 1, 2018: Journal of Labelled Compounds & Radiopharmaceuticals
Crist N Filer, Demetri Orphanos
The 2-step synthesis of [1-14 C]tyramine hydrochloride is described with the product being characterized by TLC, HPLC, and UV spectroscopy. Several methods are provided to purify [1-14 C]tyramine hydrochloride, and its storage and stability are also discussed.
July 14, 2018: Journal of Labelled Compounds & Radiopharmaceuticals
Lu Chen, Yong Gong, Rhys Salter
Ketamine is a well-known general anesthetic that inhibits cerebral NMDA receptors. Norketamine is a major circulating metabolite of this drug. A nasal spray formulation of esketamine, the S enantiomer of ketamine, is under development for the management of treatment-resistant depression. To assess the pharmacokinetic properties, C-14 labeled ketamine and norketamine were prepared separately from commercially available [14 C]CuCN through a five-step sequence with the C-14 label at the quaternary carbon of the cyclohexyl ring...
July 10, 2018: Journal of Labelled Compounds & Radiopharmaceuticals
Masafumi Tanaka, Akira Hosotani, Takahiro Mukai
Discoidal lipid nanoparticles mimicking native high-density lipoproteins (HDL) are promising delivery vehicles of drugs and/or imaging agents. However, little is known about the in vivo biodistribution of such discoidal lipid nanoparticles compared to liposomes, clinically available spherical lipid nanoparticles. Recently, it has been reported that synthetic polymers instead of apolipoproteins can be complexed with phospholipid to form discoidal nanoparticles. In the present study, with the aim of developing phospholipid-synthetic polymer complexes for future clinical applications, the biodistribution of such particles in normal mice was investigated...
July 4, 2018: Journal of Labelled Compounds & Radiopharmaceuticals
Jason P Holland
No abstract text is available yet for this article.
July 2018: Journal of Labelled Compounds & Radiopharmaceuticals
Delphine Vivier, Sai Kiran Sharma, Brian M Zeglis
Over the past 25 years, antibodies have emerged as extraordinarily promising vectors for the delivery of radionuclides to tumors for nuclear imaging. While radioimmunoconjugates often produce very high activity concentrations in target tissues, they also are frequently characterized by elevated activity concentrations in healthy organs as well. The root of this background uptake lies in the complex network of biological interactions between the radioimmunoconjugate and the subject. In this review, we seek to provide an overview of these interactions and thus paint a general picture of the in vivo fate of radioimmunoconjugates...
July 2018: Journal of Labelled Compounds & Radiopharmaceuticals
Wen-Ting K Tsai, Anna M Wu
The exquisite specificity of antibodies and antibody fragments renders them excellent agents for targeted delivery of radionuclides. Radiolabeled antibodies and fragments have been successfully used for molecular imaging and radioimmunotherapy (RIT) of cell surface targets in oncology and immunology. Protein engineering has been used for antibody humanization essential for clinical applications, as well as optimization of important characteristics including pharmacokinetics, biodistribution, and clearance. Although intact antibodies have high potential as imaging and therapeutic agents, challenges include long circulation time in blood, which leads to later imaging time points post-injection and higher blood absorbed dose that may be disadvantageous for RIT...
July 2018: Journal of Labelled Compounds & Radiopharmaceuticals
Mark D Bartholomä
While radioimmunotherapy (RIT) for the treatment of hematological malignancies such as indolent B-cell lymphoma has proven quite successful, clinical results of RIT in solid tumors have only been moderate in the past. The reasons were manifold and can be mostly attributed to the different biological properties of solid tumors vs hematological cancers. Furthermore, the slow clearance of the radiolabelled antibody prevents the use of radiation doses necessary to achieve clinical responses. The long biological half-life of radioimmunoconjugates results in high background levels and is the main reason for radiation related toxicities...
July 2018: Journal of Labelled Compounds & Radiopharmaceuticals
Lukas M Carter, Sophie Poty, Sai Kiran Sharma, Jason S Lewis
Intact antibodies and their truncated counterparts (eg, Fab, scFv fragments) are generally exquisitely specific and selective vectors, enabling recognition of individual cancer-associated molecular phenotypes against a complex and dynamic biomolecular background. Complementary alignment of these advantages with unique properties of radionuclides is a defining paradigm in both radioimmunoimaging and radioimmunotherapy, which remain some of the most adept and promising tools for cancer diagnosis and treatment...
July 2018: Journal of Labelled Compounds & Radiopharmaceuticals
Eduardo Aluicio-Sarduy, Paul A Ellison, Todd E Barnhart, Weibo Cai, Robert Jerry Nickles, Jonathan W Engle
Recent advances in molecular characterization of tumors have made possible the emergence of new types of cancer therapies where traditional cytotoxic drugs and nonspecific chemotherapy can be complemented with targeted molecular therapies. One of the main revolutionary treatments is the use of monoclonal antibodies (mAbs) that selectively target the disseminated tumor cells while sparing normal tissues. mAbs and related therapeutics can be efficiently radiolabeled with a wide range of radionuclides to facilitate preclinical and clinical studies...
July 2018: Journal of Labelled Compounds & Radiopharmaceuticals
Brooke N McKnight, Nerissa T Viola-Villegas
Therapeutic monoclonal antibodies have been used in cancer treatment for 30 years, with around 24 mAb and mAb:drug conjugates approved by the FDA to date. Despite their specificity, efficacy has remained limited, which, in part, derails nascent initiatives towards precision medicine. An image-guided approach to reinforce treatment decisions using immune positron emission tomography (immunoPET) companion diagnostic is warranted. This review provides a general overview of current translational research using Zr-89 immunoPET and opportunities for utilizing and harnessing this tool to its full potential...
July 2018: Journal of Labelled Compounds & Radiopharmaceuticals
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