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Radiochemistry

A special issue of Molecules (ISSN 1420-3049).

Deadline for manuscript submissions: closed (30 May 2012) | Viewed by 53831

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Nuklearmedicinsk Afdeling—Hobrovej 18-22, Postboks 365, 9100 Aalborg, Denmark
Interests: radiochemistry; radiopharmacy; GMP-production; drug degradation; receptor kinetics; analytical methods; chelation; medicinal chemistry
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Special Issue Information

Dear Colleagues,

Radiochemistry is the chemistry of radioactive materials. The research interest in this field of chemistry has experienced a big growth during the last decades, driven by a demand of being able to visualize biological processes in the human body. This special issue of Molecules, dedicated to radiochemistry, calls for both fundamental and applied contributions in this field of growing academic and industrial interests. Special attention will be paid to paper which has a high degree of novelty, which can contribute to making everyday life easier for radio chemists, which can have a (potential) diagnostic impact or/and which contribute to the understanding of biological processes in vivo.

Dr. Svend Borup Jensen
Guest Editor

Keywords

  • incorporation of radioactive isotopes into biological interesting compounds
  • radioactive labeled compounds metabolic pathway
  • synthesis of precursor and reference materials
  • quality control of radiopharmaceuticals
  • purification technics
  • non-commercial equipment
  • PET molecules
  • SPEC molecules

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Published Papers (4 papers)

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Research

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1495 KiB  
Article
Detection, Quantification, and Microlocalisation of Targets of Pesticides Using Microchannel Plate Autoradiographic Imagers
by Mabruka H. Tarhoni, Vasanthy Vigneswara, Marie Smith, Susan Anderson, Peter Wigmore, John E. Lees, David E. Ray and Wayne G. Carter
Molecules 2011, 16(10), 8535-8551; https://doi.org/10.3390/molecules16108535 - 11 Oct 2011
Cited by 17 | Viewed by 9199
Abstract
Organophosphorus (OP) compounds are a diverse chemical group that includes nerve agents and pesticides. They share a common chemical signature that facilitates their binding and adduction of acetylcholinesterase (AChE) within nerve synapses to induce cholinergic toxicity. However, this group diversity results in non-uniform [...] Read more.
Organophosphorus (OP) compounds are a diverse chemical group that includes nerve agents and pesticides. They share a common chemical signature that facilitates their binding and adduction of acetylcholinesterase (AChE) within nerve synapses to induce cholinergic toxicity. However, this group diversity results in non-uniform binding and inactivation of other secondary protein targets, some of which may be adducted and protein activity influenced, even when only a relatively minor portion of tissue AChE is inhibited. The determination of individual OP protein binding targets has been hampered by the sensitivity of methods of detection and quantification of protein-pesticide adducts. We have overcome this limitation by the employment of a microchannel plate (MCP) autoradiographic detector to monitor a radiolabelled OP tracer compound. We preincubated rat thymus tissue in vitro with the OP pesticides, azamethiphos-oxon, chlorfenvinphos-oxon, chlorpyrifos-oxon, diazinon-oxon, and malaoxon, and then subsequently radiolabelled the free OP binding sites remaining with 3H-diisopropylfluorophosphate (3H-DFP). Proteins adducted by OP pesticides were detected as a reduction in 3H-DFP radiolabelling after protein separation by one dimensional polyacrylamide gel electrophoresis and quantitative digital autoradiography using the MCP imager. Thymus tissue proteins of molecular weights ~28 kDa, 59 kDa, 66 kDa, and 82 kDa displayed responsiveness to adduction by this panel of pesticides. The 59 kDa protein target (previously putatively identified as carboxylesterase I) was only significantly adducted by chlorfenvinphos-oxon (p < 0.001), chlorpyrifos-oxon (p < 0.0001), and diazinon-oxon (p < 0.01), the 66 kDa protein target (previously identified as serum albumin) similarly only adducted by the same three pesticides (p < 0.0001), (p < 0.001), and (p < 0.01), and the 82 kDa protein target (previously identified as acyl peptide hydrolase) only adducted by chlorpyrifos-oxon (p < 0.0001) and diazinon-oxon (p < 0.001), when the average values of tissue AChE inhibition were 30%, 35%, and 32% respectively. The ~28 kDa protein target was shown to be heterogeneous in nature and was resolved to reveal nineteen 3H-DFP radiolabelled protein spots by two dimensional polyacrylamide gel electrophoresis and MCP autoradiography. Some of these 3H-DFP proteins spots were responsive to adduction by preincubation with chlorfenvinphos-oxon. In addition, we exploited the useful spatial resolution of the MCP imager (~70 mm) to determine pesticide micolocalisation in vivo, after animal dosing and autoradiography of brain tissue sections. Collectively, MCP autoradiographic imaging provided a means to detect targets of OP pesticides, quantify their sensitivity of adduction relative to tissue AChE inhibition, and highlighted that these common pesticides exhibit specific binding character to protein targets, and therefore their toxicity will need to be evaluated on an individual compound basis. In addition, MCP autoradiography afforded a useful method of visualisation of the localisation of a small radiolabelled tracer within brain tissue. Full article
(This article belongs to the Special Issue Radiochemistry)
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868 KiB  
Article
Specific Radioactivity of Neutron Induced Radioisotopes: Assessment Methods and Application for Medically Useful 177Lu Production as a Case
by Van So Le
Molecules 2011, 16(1), 818-846; https://doi.org/10.3390/molecules16010818 - 19 Jan 2011
Cited by 12 | Viewed by 12632
Abstract
The conventional reaction yield evaluation for radioisotope production is not sufficient to set up the optimal conditions for producing radionuclide products of the desired radiochemical quality. Alternatively, the specific radioactivity (SA) assessment, dealing with the relationship between the affecting factors and the inherent [...] Read more.
The conventional reaction yield evaluation for radioisotope production is not sufficient to set up the optimal conditions for producing radionuclide products of the desired radiochemical quality. Alternatively, the specific radioactivity (SA) assessment, dealing with the relationship between the affecting factors and the inherent properties of the target and impurities, offers a way to optimally perform the irradiation for production of the best quality radioisotopes for various applications, especially for targeting radiopharmaceutical preparation. Neutron-capture characteristics, target impurity, side nuclear reactions, target burn-up and post-irradiation processing/cooling time are the main parameters affecting the SA of the radioisotope product. These parameters have been incorporated into the format of mathematical equations for the reaction yield and SA assessment. As a method demonstration, the SA assessment of 177Lu produced based on two different reactions, 176Lu (n,γ)177Lu and 176Yb (n,γ) 177Yb (β- decay) 177Lu, were performed. The irradiation time required for achieving a maximum yield and maximum SA value was evaluated for production based on the 176Lu (n,γ)177Lu reaction. The effect of several factors (such as elemental Lu and isotopic impurities) on the 177Lu SA degradation was evaluated for production based on the 176Yb (n,γ) 177Yb (β- decay) 177Lu reaction. The method of SA assessment of a mixture of several radioactive sources was developed for the radioisotope produced in a reactor from different targets. Full article
(This article belongs to the Special Issue Radiochemistry)
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Review

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1496 KiB  
Review
Sorption Speciation of Lanthanides/Actinides on Minerals by TRLFS, EXAFS and DFT Studies: A Review
by Xiaoli Tan, Ming Fang and Xiangke Wang
Molecules 2010, 15(11), 8431-8468; https://doi.org/10.3390/molecules15118431 - 17 Nov 2010
Cited by 153 | Viewed by 17381
Abstract
Lanthanides/actinides sorption speciation on minerals and oxides by means of time resolved laser fluorescence spectroscopy (TRLFS), extended X-ray absorption fine structure spectroscopy (EXAFS) and density functional theory (DFT) is reviewed in the field of nuclear disposal safety research. The theoretical aspects of the [...] Read more.
Lanthanides/actinides sorption speciation on minerals and oxides by means of time resolved laser fluorescence spectroscopy (TRLFS), extended X-ray absorption fine structure spectroscopy (EXAFS) and density functional theory (DFT) is reviewed in the field of nuclear disposal safety research. The theoretical aspects of the methods are concisely presented. Examples of recent research results of lanthanide/actinide speciation and local atomic structures using TRLFS, EXAFS and DFT are discussed. The interaction of lanthanides/actinides with oxides and minerals as well as their uptake are also of common interest in radionuclide chemistry. Especially the sorption and inclusion of radionuclides into several minerals lead to an improvement in knowledge of minor components in solids. In the solid-liquid interface, the speciation and local atomic structures of Eu(III), Cm(III), U(VI), and Np(IV/VI) in several natural and synthetic minerals and oxides are also reviewed and discussed. The review is important to understand the physicochemical behavior of lanthanides/actinides at a molecular level in the natural environment. Full article
(This article belongs to the Special Issue Radiochemistry)
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364 KiB  
Review
Radiolabeled Small Molecule Protein Kinase Inhibitors for Imaging with PET or SPECT
by Justin W. Hicks, Henry F. VanBrocklin, Alan A. Wilson, Sylvain Houle and Neil Vasdev
Molecules 2010, 15(11), 8260-8278; https://doi.org/10.3390/molecules15118260 - 15 Nov 2010
Cited by 56 | Viewed by 13337
Abstract
Imaging protein kinase expression with radiolabeled small molecule inhibitors has been actively pursued to monitor the clinical potential of targeted therapeutics and treatments as well as to determine kinase receptor density changes related to disease progression. The goal of the present review is [...] Read more.
Imaging protein kinase expression with radiolabeled small molecule inhibitors has been actively pursued to monitor the clinical potential of targeted therapeutics and treatments as well as to determine kinase receptor density changes related to disease progression. The goal of the present review is to provide an overview of the breadth of radiolabeled small molecules that have been synthesized to target intracellular protein kinases, not only for imaging in oncology, but also for other areas of interest, particularly the central nervous system. Considerable radiotracer development has focused on imaging receptor tyrosine kinases of growth factors, protein kinases A, B and C, and glycogen synthase kinase–3β. Design considerations, structural attributes and relevant biological results are summarized. Full article
(This article belongs to the Special Issue Radiochemistry)
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