bluuebunny/crossref_metadata_2025_split huggingface dataset:
Carbon‐11 labelling of the α‐2 antagonist atipamezole
Authors: Roeda D. , Sipilä H. T. , Bramoullé Y. , Enas J. D. , Vaufrey F. , Dollé F. , Crouzel C. 
Published: April 2012

AbstractThe α‐2 antagonist Atipamezole has been labelled with carbon‐11 using [11C]CH2O and the corresponding α‐ketoaldehyde 1. For the synthesis of 1 two routes are proposed. The radiochemical yield of [11C]Atipamezole was 24% relative to [11C]CH2O and the synthesis time, including HPLC purification, was 30 minutes.
Vincristine toxicity: The effect on the biodistribution of radiopharma ceutical and in the optical microscopy of organs isolated from the treated animals
Authors: Mattos D. M. M. , Gomes M. L. , Freitas R. S. , Moreno S. , Nascimento A. L. R. , Carvalho J. J. , Bernardo‐Filho M. 
Published: April 2012

AbstractThere are many articles and textbooks quoting examples of drug‐radiopharmaceutical interactions. Such interactions arise as a result of an exaggerated pharmacological activity of the drug producing altered biodistribution of the radiopharmaceutical. Vincristine was administered into mice, one hour after the last dose, technetium‐99m‐diethylenetriaminepentaacetic acid (99mTc‐DTPA) was injected. After 0.5 hour, the animals were sacrificed and the percentage of total radioactivity (%ATI) was calculated. In the treated animals, 99mTc‐DTPA has increased in uterus, ovary, spleen, thymus, lymph nodes, kidney, lung, liver, stomach, heart and bone. Optical microscopy of a portion of ring fragment of spleen, kidney and liver were cut into strips and fixed, postfixed, dehydrated and Epon embedded. Semithin sections were prepared and stained with toluidine blue. The results revel that in kidney and liver no have alterations, but, in spleen, an increased of extracellular matrix was observed. The results can be explained by its metabolization, therapeutic, toxic and/or immunosupressive actions of this chemotherapeutic drug.
Preparation of cyclopentadienyl tricarbonyl technetium‐94m complexes
Authors: Luyt L. G. , Mull E. S. , Katzenellenbogen J. A. , Bigott H. M. , Welch M. J. 
Published: April 2012

AbstractCyclopentadienyltricarbonyl complexes with technetium‐94m have been prepared by two methods and were characterized by comparison to rhenium analogues.
Tc Oxocomplexes with the PNO/S and PNS/S donor atom sets: Labelling of a 5HT1A receptor — binding ligand
Authors: Fernandes C. , Correia J. D. G. , Gano L. , Santos I. , Seifert S. , Syhre R. , Spies H. 
Published: April 2012

AbstractMixed — ligand model complexes, [99mTc(O)(PNX)(SPh)] (XO (1a), S (2a)), were synthesized from [99mTcO4]−. These compounds were characterized by comparing their radioactive HPLC profiles with the UV profiles of the analytically pure Re compounds 1 and 2. Based on stability studies, undertaken in aqueous solutions and in glutathione challenge experiments, 2a was chosen for biodistribution studies in rats. Using this approach, the labelling of a 5‐HT1A receptor ligand (derivatized aryl‐piperazine) with 99mTc was also performed using the PNS chelate.
Comparison of the precipitation methods (ammonium sulphate and trichloroacetic acid) to evaluate the in vivo binding of 99mTc‐MDP on blood constituents
Authors: Freitas R. S. , Gomes M. L. , Mattos D. M. , Moreno S. R. , Feliciano G. D. , Lima E. , Lima‐Filho G. L. , Penas M. E. , Orlando M. M. C. , Bernardo‐Filho M. 
Published: April 2012

AbstractThe determination of the radiopharmaceutical binding on blood constituents is worthwhile to understand the biodistribution and to dosimetric considerations. We studied this binding of the Tc‐99m methylenediphosphonic acid (99mTc‐MDP) used to bone evaluation. This radiopharmaceutical was administrated in Wistar rats and after 5 min, blood was withdrawn with anticoagulant. The samples were centrifuged, plasma (P) and blood cells (BC) separated, precipitated with trichloroacetic acid (TCA) or ammoniun sulfate (AS) in various concentrations (0.1, 0.5, 1.0, 5.0, 10 and 20%) and soluble (SF) and insoluble fractions (IF) isolated. The percent of radioactivity (% ATI) in the fractions was determined. The % ATI on P was 84.58 ± 8.16 and on BC was 15.39 ± 8.17. Concerning to TCA, (i) the highest % ATI in IF‐P was from (40.64 ± 9.81) to the 5.0% TCA concentrations and (ii) on IF‐BC, % ATI decreased significantly (p<0.01) from (78.08 ± 7.58 to 66.98 ± 8.40) with the used TCA concentrations. The % ATI, when AS was used on (a) IF‐P was not modified by the AS concentrations, and (b) on IF‐BC varied from 77.46 ± 3.47 to 38.03 ± 8.76 respectively with the AS concentrations from 0.1. to 10.0%. We can speculate that the binding of the studied radiopharmaceutical to blood elements and the precipitation effect may depend on the chemical characteristics of the radiopharmaceutical studied and the mechanisms involved in its fixation on the blood elements.
Evaluation of the toxic effect of chemotherapeutic drugs: Study on the biodistribution of 99mTc‐radiopharmaceuticals used in bone scintigraphy in mice
Authors: Gomes M. L. , Mattos D. M. M. , Freitas R. S. , Moreno S. R. F. , Bernardo‐Filho M. 
Published: April 2012

AbstractIt is accepted that a variety of factors can alter the biodistribuition of radiopharmaceuticals and one such factor is the drug therapy. Since patients on chemotherapeutic treatment can be submitted to a nuclear medicine procedure, we studied in mice, the effect of chemotherapeutic drugs on the biodistribution of the technetium‐99m‐radiopharmaceuticals. Mitomycin‐C or vincristine were administered in mice (n=15) during some days. After tbat, the methylenediphosphonic acid labelled with technetium‐99m (99mTc‐MDP) was also injected and the animals were sacrified. The organs were isolated and counted in a well counter. The percentages of radioactivity (%ATI) in the organs were calculated. Concerning to mitomycin‐C, the results have shown that the %ATI has increased in pancreas, ovary, uterus, stomach, kidney, spleen, thymus, heart, lung, liver and bone. Concerning to vincristine, the results have shown that the %ATI has decreased in uterus, ovary, spleen, thymus, kidney, liver, stomach, heart and brain. In general, the alterations in the uptake of the radiopharmaceutical could be justified by the metabolic process, the therapeutic effect and/or the toxic action of mitomycin‐C and vincristine in specific organs. The effect of these chemotherapeutic drugs on the biodistribution of other 99mTc‐radiopharmaceuticals are now in progress.
Statistical evaluation of the quality control results of some 99mTc‐radipharmaceuticals
Authors: Janković D. , Djokić D. , Maksin T. , Orlić M. 
Published: April 2012

AbstractThe statistical evaluation of the quality control results of 99mTc‐DTPA, 99mTc‐DMS, 99mTc‐PyP and 99mTc‐EHIDA batches produced during five consecutive years is presented. The selection of radiochromatographic methods for routine quality control of 99mTc‐radiopharmaceuticals as well as stationary or mobile phase was made. Radiochemical purity of the each radiopharmaceutical was determined in 25 batches. Distribution of these radiopharmaceuticals per organs in different time interval from injection to sacrifice of the animals were determined as well as the mean values of percentage of the radiopharmaceutical bounded per organ, characteristic for tested preparations for all chosen batches. The analysis shows that the obtained values are arranged around their statistically allowed mean values.
Fibrin glue system for brachytherapy of glioblastoma with RE‐88 and RE‐186 labeled microspheres
Authors: Häfeli U. O. , Pauer G. J. 
Published: April 2012

AbstractBrain tumors such as glioblastoma recur in their original location in almost 50% of the cases. To prevent this we developed a radiopharmaceutical system that can be applied as a gel immediately after resection of a brain tumor to deliver local booster doses. The gel, which strongly adheres to tissue in the treatment area, consists of fibrin glue containing the β‐emitters Re‐188 and Re‐186 in microsphere‐bound form. Its radioisotope‐dependent maximum treatment range in tissue is 11 and 6 mm, respectively. The dosimetry of this fibrin glue system was determined using gafchromic film measurements. No toxic effects were seen in vivo, but histological examination showed dose‐dependent radiation effects. The effectiveness of Re‐188/Re‐186‐containing fibrin glue was demonstrated in a rodent glioblastoma model. All control animals died within 17 ± 3 days, whereas 60% of the treated animals survived 36 days, the final length of the experiment.
Labeling of antibodies with 149Tb for targeted alpha therapy
Authors: Vranješ S. D. , Miederer M. , Čomor J. J. , Soloviev D. , Beyer G.‐J. 
Published: April 2012

AbstractMonoclonal antibodies CHX‐A‐DTPA‐HuM195 specific to CD 33 antigens on leukemia cells were labeled with carrier free 149Tb and 149Gd. Labeling yield and radiochemical purity were determined and in vitro studies concerning immunoreactivity, internalization and killing of leukemia HL‐60 cells were performed.
Preparation of 213bi‐dota‐biotin in high specific activity for pretargeted alpha radiotherapy of cancer
Authors: Hylarides Mark D. , Axworthy Don B. , Fritzberg Alan R. 
Published: April 2012

AbstractThe alpha emitter, Bismuth‐213, (213Bi) T1/2 = 45 min, obtained from an 225Ac generator, was chelated to DOTA‐biotin in high radiochemical yield and specific activity. The radiolabeled product showed good radiochemical stability and was used in preclinical therapy studies using a pretargeting format.
A no‐carrier‐added 72Se/72As isotope generator
Authors: Novgorodov A. F. , Schmidt A. , Brockmann J. , Qaim S. M. , Rösch F. 
Published: April 2012

AbstractA no‐carrier‐added 72Se/72As generator has been developed for the isolation of 72As, relevant for eventual application in the syntheses of 72As‐labelled radiopharmaceuticals. Avoiding the addition of Se carrier and using a thermochromatographic destillation process, no‐carrier‐added 72As is nearly quantitatively released within 10 min. 72Se remains almost quantitatively (> 99.7%) in solution when a temperature of the separation process of 100°C is applied.
Preparation, biodistribution, and micropet imaging of 45Ti‐transferrin
Authors: Vävere A. L. , Jones L. A. , Mccarthy T. J. , Rowland D. J. , Welch M. J. 
Published: April 2012

AbstractSeveral titanium complexes are currently being investigated for their ability to exhibit antitumor activity both in vitro and in vivo (1). Sun et al. recently showed the first specific Ti(IV)‐protein complex through binding experiments with transferrin (2). This suggests that transferrin could be the mode of transport for titanium anticancer drugs since tumor cells show high levels of transferrin receptors on the cell surface (3). Transferrin has a molecular weight of 80 kDa and is only 30% saturated with iron, leaving available binding sites for other metal ions (4).Titanium‐45 has a half‐life of 3.09 hours and a positron branching ratio of 85% with an Eβ+max of 1.04 MeV. The work of Ishiwata et al. investigated 45Ti as a potential metal for labeling pharmaceuticals for PET imaging (5). In the current study, the biodistribution of 45Ti‐transferrin was examined to investigate the mode of transport of titanium compounds to tumors.
Radiofluoridations of m — substituted nitrobenzenes
Authors: Constantinou M. , Shah F. , Pike V. W. 
Published: April 2012

AbstractThe fluoridation of a range of m‐substituted nitrobenzenes with no‐carrier‐added [18F]fluoride was investigated. Electron‐deficient m‐substituted nitrobenzenes react with no‐carrier‐added [18F]fluoride to give 18F‐labelled m‐disubstituted benzenes in low to moderate yields.
Radiosynthesis of 1‐[18F]fluoromethyl‐4‐methyl‐benzene and a series of o‐, m‐ or p‐substituted 1‐halomethyl‐ [18F]fluoromethyl‐benzenes
Authors: Namolingam V. , Luthra S. K. , Brady F. , Pike V. W. 
Published: April 2012

Abstract1‐[18F]Fluoromethyl‐4‐methyl‐benzene was prepared from its bromo analogue. Additionally, a number of o‐, m‐ or p‐substituted 1‐halomethyl‐[18F]fluoromethyl‐benzenes were prepared by nucleophilic substitution reactions with [18F]fluoride on their dihalo analogues to provide new prospective bifunctional labelling agents.
Synthesis and Cu1+ Assisted radiosynthesis of 2‐radioiodo phloretinic acid, a potential glut tracer
Authors: Mertens J. , Boumon R. , Steegmans P. 
Published: April 2012

Abstract2‐Bromo‐phloretinic acid (2‐Br‐PLA): 2‐bromo‐4‐(3‐oxo‐3(2,4,6‐trihydroxyphenyl) propyl)benzoic acid, the precursor molecule for the radiosynthesis of 2‐radioiodophloretinic acid (2‐*I‐PLA): 2‐radioiodo‐4‐(3‐oxo‐3(2, 4, 6‐trihydroxyphenyl)‐propyl)benzoic acid, was prepared by a twelve step synthesis starting from hydrocinnamic acid. The radiosynthesis was carried out by applying the Cu(I)‐assisted nucleophilic non‐isotopic exchange reaction in acidic reducing medium.The amount of copper to reach high yields was found to be critical. At substrate to copper ratios generally used in this type of synthesis dehalogenation of the starting compound occurred, decreasing the labelling yield considerably. In optimal conditions a labelling yield of 95% was reached.
A simple and improved method for [11C]phosgene production with iron(III) oxide
Authors: Kuge Y. , Nishijima K. , Seki K. , Ohkura K. , Tsukamoto E. , Nagatsu K. , Tanaka A. , Tamaki N. 
Published: April 2012

Abstract[11C]COCl2 is a precursor for several useful radiopharmaceuticals. [11C]COCl2 is generally produced by catalytic oxidation of [11C]CCl4 produced from [11C]CH4. In order to develop a simplified method for [11C]COCl2 production; we examined effects of oxidizing agents (Fe2O3, CuO) on the [11C]COCl2 yields. The yields of [11C]COCl2, assessed by the yields of [11C]diphenylurea, was increased by using Fe2O3 powder mixed with iron granule, compared with those by Fe alone or CuO alone. Yields of [11C]CGP‐12177 were also significantly higher with Fe2O3 than without Fe2O3. The present results show that Fe2O3 mixed with iron granule improve the conversion of [11C]CCl4 to [11C]COCl2 and the yields of [11C]CGP‐12177. Thus, we have developed a simple and improved method for [11C]COCl2 production with iron oxide (Fe2O3).
Metabolism of [11C‐methyl]choline in tumour bearing mice and synthesis and isolation of its catabolite [11C‐methyl]betaine
Authors: Brown G. D. , Osman S. , Wilson H. K. , Aboagye E. , Price P. M. , Luthra S. K. , Brady F. 
Published: April 2012

AbstractThe uptake and metabolism of [11C‐methyl]choline was examined in tumour bearing mice. Tumours showed [11C‐methyl]choline, [11C‐methyl]betaine and [11C‐methyl]phosphocholine, whereas in plasma only [11C‐methyl]choline and [11C‐ methyl]betaine were observed. To correct for the contribution of [11C‐methyl]betaine to [11C‐methyl]choline derived radioactivity in tissues, [11C‐methyl]betaine has been prepared from [11C‐methyl]choline, isolated by HPLC and the position of incorporation of C‐11 label confirmed by [11/13C]co‐labelling and NMR.
Production of ultra high quantities of 18F‐fluoride Via 18O2 gas target: A progress report
Authors: Becker D. , Buckley K. R. , Chun K. S. , Hurtado E. T. , Jivan S. , Zeisler S. , Ruth T. J. 
Published: April 2012

AbstractThere is a real need to develop a superior high yield target system for the production of large quantities of 18F‐fluoride with the increasing numbers of clinical PET centers worldwide. Therefore we have investigated a route to higher yield target system for 18F‐fluoride production which relies on gas target designs. (1)
3′‐End‐labeling procedure for phosphorothioate oligonucleotides and oligonucleotide‐conjugates
Authors: Mier W. , Rossmann M. , Mohammed A. , Haberkorn U. , Eisenhut M. 
Published: April 2012

AbstractOligonucleotides offer an enormous potential for therapeutical and diagnostic applications. Unfortunately the cellular uptake is a fundamental problem for the application of antisense oligonucleotides. Oligonucleotides are large charged molecules which are unable to penetrate the cellular membrane by diffusion. The resulting low cellular uptake can be circumvented by employing derivatized oligonucleotides. For this purpose we have recently developed oligonucleotide derivatives which are conjugated to octreotate, a cyclic octapeptide (1). Upon binding to somatostatin receptors (known to be overexpressed in various tumors), these conjugates can be internalized by receptor mediated endocytosis. Therefore the new conjugates consist of the oligonucleotide, which is linked via the 5′‐end to the N‐terminus of octreotate. The oligonucleotide sequence is complementary to the sequence of the protooncogene bcl‐2, which is known to be overexpressed in lymphoma. To monitor the fate of modified oligonucleotides in vivo as well as to enable the use of modified oligonucleotides for the scintigraphic imaging, labeling procedures had to be developed. This procedure also had to be suitable for the labeling of phosphorothioate‐modified oligonucleotides. Due to pharmacological advantages as compared to unmodified phosphodiester oligonucleotides, these synthetic oligonucleotides are utilized for in vivo applications. Using [γ‐32P]‐ATP and T4 polynucleotide kinase, oligonucleotides can be conveniently labeled at the 5′‐end. In order to enable the labeling of 5′‐conjugated oligonucleotides at the 3′‐end, the labeling with calf thymus terminal deoxynucleotidyl transferase (terminal transferase) and dideoxyadenosine‐5′‐[α‐32P]triphosphate ([α‐32P]‐ddATP) was investigated.
Synthesis and evaluation of a radioiodinated benzothiazole derivative as a radioligand for in vivo quantitation of β‐amyloid deposits in aging and alzheimer's disease
Authors: Wang Y. , Klunk W. E. , Huang G.‐F. , Debnath M. L. , Holt D. P. , Mathis C. A. 
Published: April 2012

AbstractAmyloid deposits in the form of senile plaques and fibrillary tangles have been targeted as a biomarker for the early diagnosis of Alzheimer's disease (AD) and evaluation of the efficacy of therapeutic treatments (1–3). For in vivo quantitation of amyloid deposits in AD, efforts have been made to develop radiopharmaceuticals for PET and/or SPECT imaging that readily penetrate the blood brain barrier and selectively localize in the area of beta‐amyloid deposits in AD brain. To date, these agents such as radiolabeled monoclonal antibodies (4), plaque‐related proteins (5, 6), analogues of Congo red (7–11), and membrane dyes (12) have found limited use due to either marginal brain uptake or high non‐specific binding.
Effect of thermal sterilization on ferulic, coumaric and cinnamic acids: dimerization and antioxidant activity
Authors: Arrieta‐Baez Daniel , Dorantes‐Álvarez Lidia , Martinez‐Torres Rocio , Zepeda‐Vallejo Gerardo , Jaramillo‐Flores Maria Eugenia , Ortiz‐Moreno Alicia , Aparicio‐Ozores Gerardo 
Published: April 2012

AbstractBACKGROUND: Some phenolic compounds, such as ferulic acid and p‐coumaric acid, exist in the form of free acids, in fruits, rice, corn and other grains. Thermal treatment (121 °C at 15–17 psi) for different times on ferulic, p‐coumaric and cinnamic acids as well as equimolar mixtures of these acids was investigated.RESULTS: Ferulic and p‐coumaric acids underwent decarboxylation, yielding dimeric products formed through their corresponding radical intermediates, while cinnamic acid was recovered unreacted. High‐performance liquid chromatography analysis showed no cross‐dimerization when equimolar mixtures of pairs of hydroxycinnamic acids were treated under the same conditions. Dimers were characterized as (E)‐4′,4″‐(but‐1‐ene‐1,3‐diyl)bis(2′‐methoxyphenol)) (dimer of 4‐vinylguaiacol) and (E)‐4,4′‐(but‐1‐ene‐1,3‐diyl)diphenol) (dimer of 4‐vinylphenol) by nuclear magnetic resonance and mass spectrometry.CONCLUSION: Sterilization by thermal processing produced dimers of ferulic and coumaric acid. The antioxidant activity of these dimers was greater than that of the respective hydroxycinnamic acids. These results may be relevant for fruits and grains that contain hydroxycinnamic acids and undergo sterilization processes such as canning. Copyright © 2012 Society of Chemical Industry
Assessment of plant biomass and nitrogen nutrition with plant height in early‐to mid‐season corn
Authors: Yin Xinhua , Hayes Robert M , McClure M Angela , Savoy Hubert J 
Published: April 2012

AbstractBACKGROUND: The physiological basis for using non‐destructive high‐resolution measurements of plant height through plant height sensing to guide variable‐rate nitrogen (N) applications on corn (Zea mays L.) during early (six‐leaf growth stage, V6) to mid (V12) season is largely unknown. This study was conducted to assess the relationships of plant biomass and leaf N with plant height in early‐ to mid‐season corn under six different N rate treatments.RESULTS: Corn plant biomass was significantly and positively related to plant height under an exponential model when both were measured at V6. This relationship explained 62–78% of the variations in corn biomass production. Leaf N concentration was, in general, significantly and positively related to plant height when both were measured at V6, V8, V10 and V12. This relationship became stronger as the growing season progressed from V6 to V12. The relationship of leaf N with plant height in early‐ to mid‐season corn was affected by initial soil N fertility and abnormal weather conditions.CONCLUSION: The relationship of leaf N concentration with plant height may provide a physiological basis for using plant height sensing to guide variable‐rate N applications on corn. Copyright © 2012 Society of Chemical Industry
Leucine‐rich repeat kinase 2 and alternative splicing in Parkinson's disease
Authors: Elliott David A. , Kim Woojin S. , Gorissen Sarsha , Halliday Glenda M. , Kwok John B.J. 
Published: April 2012

AbstractMutations of the leucine‐rich repeat kinase 2 (LRRK2) gene are the most common genetic cause of Parkinson's disease (PD) and are associated with pleiomorphic neuropathology. We hypothesize that LRRK2 mediates its pathogenic effect through alternative splicing of neurodegeneration genes. Methods used in this study included western blotting analysis of subcellular protein fractions, exon‐array analysis of RNA from cultured neuroblastoma cells transfected with LRRK2 expression vectors, and reverse‐transcription polymerase chain reaction (RT‐PCR) of RNA from cultured cells and postmortem tissue. Overexpression of the LRRK2 G2019S mutant resulted in a significant (2.6‐fold; P = 0.020) decrease in nuclear transactive response DNA‐binding protein 43 levels. Exon‐array analyses revealed that wild‐type LRRK2 had a significant effect on the expression of genes with nuclear (P < 10−22) and cell‐cycle functions (P < 10−15). We replicated changes in gene expression in 30% of selected genes by quantitative RT‐PCR. Overexpression of LRRK2 resulted in the altered splicing of two genes associated with PD, with an increased inclusion of exon 10 of microtubule‐associated protein tau (1.7‐fold; P = 0.001) and exon 5 of the alpha‐synuclein (SNCA) gene (1.6‐fold; P =0.005). Moreover, overexpression of LRRK2 (G2019S) and two mutant genes associated with neurodegeneration, TARDBP (M337V) and FUS (R521H), were associated with decreased inclusion out of the dystonin (DST) 1e precursor exons in SK‐N‐MC cells. Altered splicing of SNCA (1.9‐fold; P < 0.001) and DST genes (log2 2.3‐fold; P = 0.005) was observed in a cohort of PD, compared with neurologically healthy, brains. This suggests that aberrant RNA metabolism is an important contributor to idiopathic PD. © 2012 Movement Disorder Society