Search results for "radiopharmaceuticals"
showing 10 items of 140 documents
Copper radiopharmaceuticals for theranostic applications
2018
The growing advancement in nuclear medicine challenges researchers from several different fields to integrate imaging and therapeutic modalities in a theranostic radiopharmaceutical, which can be defined as a molecular entity with readily replaceable radioisotope to provide easy switch between diagnostic and therapeutic applications for efficient and patient-friendly treatment of diseases. For such a reason, the diagnostic and therapeutic potential of all five medical radionuclides of copper have thoroughly been investigated as they boost the hope for development of successful radiotheranostics. To facilitate the mutual understanding between all different specialists working on this multidi…
Approaching ‘kit-type’ labelling with 68Ga : the DATA chelators.
2015
The DATA chelators are a novel class of tri-anionic ligands based on 6-amino-1,4-diazepine-triacetic acid, which have been introduced recently for the chelation of (68)Ga. Compared with macrocyclic chelators based on the cyclen scaffold (i.e., DOTA, DO3A, and DO2A derivatives), DATA chelators undergo quantitative radiolabelling more rapidly and under milder conditions. In this study, a systematic evaluation of the labelling of four DATA chelators--DATA(M), DATA(P), DATA(Ph), and DATA(PPh)--with (68)Ga is presented. The results highlight the extraordinary potential of this new class of chelators for application in molecular imaging using (68)Ga positron emission tomography (PET).
Phantom size in brachytherapy source dosimetric studies
2004
An important point to consider in a brachytherapy dosimetry study is the phantom size involved in calculations or experimental measurements. As pointed out by Williamson [Med. Phys. 18, 776-786 (1991)] this topic has a relevant influence on final dosimetric results. Presently, one-dimensional (1-D) algorithms and newly-developed 3-D correction algorithms are based on physics data that are obtained under full scatter conditions, i.e., assumed infinite phantom size. One can then assume that reference dose distributions in source dosimetry for photon brachytherapy should use an unbounded phantom size rather than phantom-like dimensions. Our aim in this paper is to study the effect of phantom s…
Image-Guided Synthesis Reveals Potent Blood-Brain Barrier Permeable Histone Deacetylase Inhibitors
2014
Recent studies have revealed that several histone deacetylase (HDAC) inhibitors, which are used to study/treat brain diseases, show low blood-brain barrier (BBB) penetration. In addition to low HDAC potency and selectivity observed, poor brain penetrance may account for the high doses needed to achieve therapeutic efficacy. Here we report the development and evaluation of highly potent and blood-brain barrier permeable HDAC inhibitors for CNS applications based on an image-guided approach involving the parallel synthesis and radiolabeling of a series of compounds based on the benzamide HDAC inhibitor, MS-275 as a template. BBB penetration was optimized by rapid carbon-11 labeling and PET im…
Evaluation of [11C]Metergoline as a PET Radiotracer for 5HTR in Nonhuman Primates
2010
Metergoline, a serotonin receptor antagonist, was labeled with carbon-11 in order to evaluate its pharmacokinetics and distribution in non-human primates using positron emission tomography. [{sup 11}C]Metergoline had moderate brain uptake and exhibited heterogeneous specific binding, which was blocked by pretreatment with metergoline and altanserin throughout the cortex. Non-specific binding and insensitivity to changes in synaptic serotonin limit its potential as a PET radiotracer. However, the characterization of [{sup 11}C]metergoline pharmacokinetics and binding in the brain and peripheral organs using PET improves our understanding of metergoline drug pharmacology.
A simple method of bronchoprovocation using a valved holding chamber.
2004
This study was undertaken to ascertain whether the use of a valved holding chamber (VHC) during bronchial provocation testing might increase lung deposition and repeatability of the test relative to the tidal breathing method. The 2-min tidal breathing results were compared to five inhalations from a VHC device in patients using the Pari-provoII nebulizer (MMD = 2.1mkm). Lung and mouth deposition, losses though the exhaled air and losses before aerosol delivery to the patient's mouth were measured in patients using a radiolabeled 99Tc-DTPA solution and gamma camera. The study revealed that lung deposition was 67% with the VHC method, and losses with exhaled air were 29% of the inhaled amoun…
Design and pharmacology of quinuclidine derivatives as M2-selective muscarinic receptor ligands
2001
In our search for M2-selective muscarinic receptor antagonists, we synthesized 1,3-disubstituted indenes. The effects of different basic moieties with regard to binding and selectivity towards the five distinct muscarinic receptor subtypes were investigated. The results show that the quinuclidine series afforded the most promising compounds in terms of both receptor affinity and M2-subtype selectivity.
THERP and HEART integrated methodology for human error assessment
2015
Abstract THERP and HEART integrated methodology is proposed to investigate accident scenarios that involve operator errors during high-dose-rate (HDR) treatments. The new approach has been modified on the basis of fuzzy set concept with the aim of prioritizing an exhaustive list of erroneous tasks that can lead to patient radiological overexposures. The results allow for the identification of human errors that are necessary to achieve a better understanding of health hazards in the radiotherapy treatment process, so that it can be properly monitored and appropriately managed.
A new method for radiochemical separation of arsenic from irradiated germanium oxide.
2005
Abstract Radioarsenic labelled radiopharmaceuticals could be a valuable asset to Positron Emission Tomography (PET). In particular, the long half-lives of 72 As ( T 1/2 =26 h) and 74 As ( T 1/2 =17.8 d) allow to investigate slow physiological or metabolical processes, like the enrichment and distribution of antibodies in tumor tissue. This work describes the direct production of no-carrier-added (nca) arsenic isotopes *As, with *=71, 72, 73, 74 or 77, the reaction to [*As]AsI 3 and its radiochemical separation from the irradiated solid germanium oxide via polystyrene-based solid-phase extraction. The germanium oxide target, irradiated at a cyclotron or a nuclear reactor, is dissolved in con…
Post-elution processing of 44Ti/44Sc generator-derived 44Sc for clinical application
2009
The (44)Ti/(44)Sc (T(1/2)(44)Ti=60a) generator provides cyclotron-independent access to positron-emitting (44)Sc (T(1/2)=3.97d) for PET imaging. This work aims to post-elution processing of initial (44)Sc generator eluates in order to reduce its volume, HCl concentration and remove the oxalate anions. The on-line adsorption of (44)Sc on cationic resin AG 50W-X8 (200-400 mesh, H(+)-form) is achieved with >98% efficacy. Subsequently, the purified (44)Sc is desorbed by using 3ml of 0.25M ammonium acetate (pH=4.0). The post-processing takes 10min. The overall yield of the post-processing reached 90%, which is referred to the (44)Sc obtained from the (44)Ti/(44)Sc generator. In addition to the c…