bluuebunny/crossref_metadata_2025_split huggingface dataset:
Risk management and legal issues with the use of social media in the healthcare setting
Authors: Lambert Kristen M. , Barry Pauline , Stokes Gwen 
Published: April 2012

AbstractSocial media have infiltrated all of our lives, both personally and professionally. Most of us could never have envisioned the impact that social media have had on us, particularly in the healthcare arena. Who would have thought even five years ago that a discussion on the ASHRM exchange would involve the use of Twitter in the operating room or that a physician would be reprimanded by a state medical board and have her privileges revoked due to posting information online about a trauma patient? In the coming years, social media use will only increase, causing concern for risk managers across the continuum. Furthermore, although case law and statutory regulations addressing the use of social media are minimal today, it is anticipated that we will see legal challenges to this evolving medium in the future.
Synthesis of a carbon‐11 labelled agonist of the α7 nicotinic acetylcholine receptors
Authors: Dollé F. , Hinnen F. , Valette H. , Demphel S. , Coulon C. , Ottaviani M. , Bottlaender M. , Crouzel C. 
Published: April 2012

AbstractThe lead compound of a new series of azabicyclic carbamates, described by Astra Laboratories, namely Astra‐255082 (N‐(4‐bromophenyl)carbamic acid quinuclidin‐3‐yl ester) has been labelled with carbon‐11 using no‐carrier‐added [11C]phosgene.
The development of additional radioligands of varying pharmacokinetics for the 5‐HT1A receptor
Authors: Lang L. , Jagoda E. M. , Eckelman W. C. 
Published: April 2012

AbstractSix compounds have been prepared to further probe the structure activity relationships based on the 5‐HT1A receptor ligand, WAY 100635. The goal is to obtain a series of radiotracers with varying pharmacokinetic properties. Substitution of a pyrimidine for a pyridine moiety, increased the specific binding ratio in the phenylcarboxamide series, but decreased the ratio in the cyclohexanecarboxamide series. A series of compounds with varying pharmacokinetic properties are now available to study a range of properties involving 5‐HT1A receptor binding.
Carbon‐11 labelling of a half mustard prodrug by reductive alkylation using [11C]acetaldehyde. A potential tracer for evaluation of adept or gdept using pet
Authors: Khanum N. , Luthra S. K. , Zhao Y. , Aboagye E. , Price P. M. , Burke P. , Brady F. 
Published: April 2012

AbstractA half mustard anticancer prodrug carrying N‐chloroethyl and N′‐ethyl groups was labelled in the N′‐ethyl group by reductive alkylation using [11C]acetaldehyde.
Synthesis of 2, 16α‐ and 4, 16α‐[16α‐18F]difluoroestradiols and their 11β‐methoxy derivatives for estrogen receptor imaging
Authors: Seimbille Y. , Rousseau J. , Bénard F. , Ali H. , Van Lier J. E. 
Published: April 2012

AbstractWe have prepared the 2‐ and 4‐fluoro derivatives of 16α‐[18F]fluoroestradiol (FES) (4a, b) and 11β‐OMe‐FES (4c, d). Electrophilic substitution of estrone or 11β‐OMe‐estrone with N‐fluoropyridinium salt gave the 2‐and 4‐F derivatives 1, which were converted to the triols 2 and subsequently to the reactive 16β, 17β‐cyclic sulfates 3. Stereoselective opening of the cyclic sulfates via nucleophilic fluorination with Me4NF or [18F]F‐ and removal of the protecting ether and sulfate groups via rapid acid hydrolysis gave 4a‐d or [16α‐18F]‐(4a‐d).
Radiolabelling of the potential anti‐cancer agent, 5‐fluoro‐2‐(4‐amino‐3‐methylphenyl)benzothiazole (5F203) with fluorine‐18
Authors: Brown G. D. , Wilson H. K. , Westwell A. D. , Hutchinson I. , Stevens M. F. G. , Price P. M. , Aboagye E. , Luthra S. K. , Brady F. 
Published: April 2012

AbstractThe novel potential antitumour agent 5‐fluoro‐2‐(4‐amino‐3‐methylphenyl)benzothiazole (5F203) has been radiolabelled with fluorine‐18 by reaction of an amino protected trimethyltin precursor with molecular fluorine (18F‐F) followed by alkaline deprotection of the amino group. [18F]5F203 was obtained in ca 10% radiochemical yield in ca. 60 mins from end of bombardment.
FDG‐2‐nitroimidazole: A new potential hypoxia tracer using glucose transport
Authors: Patt M. , Sorger D. , Scheunemann M. , Stöcklin G. 
Published: April 2012

AbstractA promising new radiotracer for the detection of hypoxic tissue in vivo with PET has been synthesized in good yields starting from tetra‐O‐acetyl‐2‐[18F]FDG available in high amounts in 2‐[18F]FDG synthesis. The new tracer representing an adduct of 2‐nitroimidazole and 2‐[18F]FDG is not phosphorylated in vitro by hexokinase thus excluding a second non‐hypoxia dependent trapping mechanism. Furthermore it has been shown to interfere with glucose transport proteins since it inhibits the cellular uptake of [18F]FDG in a concentration‐dependent manner.
Synthesis and first evaluation of new 18F‐labelled sulfonylureas for the determination of the beta‐cell status in vivo
Authors: Schirrmacher R. , Shiue G. , Shiue S. J. , Alavi A. , Feilen P. J. , Schneider S. , Beyer J. , Rösch F. 
Published: April 2012

AbstractThe syntheses and first in vitro evaluations for two fluoride bearing sulfonylurea derivatives are reported. Firstly, the tolbutamide derivative 1‐[4‐(2‐[18F]fluoroethoxy)benzenesulfonyl]‐3‐butyl urea (2‐[18F]fluoroethyl‐tolbutamide) could be labeled efficiently with [18F]fluoride. Subsequently, the glibenclamid derivative N‐(2‐(4‐(N‐((cyclohexylamino)carbonyl)sulfonylamino)phenyl)ethyl) 2‐(5‐chloro‐2‐[18F]fluorethoxy)phenyl) formamide (2‐[18F]fluoroethyl‐glibenclamide) was labeled with [18F]fluoride in high yields. Its ability to induce insuline secretion from rat beta‐cells in relation to the original glibenclamide was determined.
Cyclopentadienyl tricarbonyl technetium‐99m octanoic acid: A novel radiotracer for evaluation of fatty acid metabolism in the liver
Authors: Lee B. C. , Choe Y. S. , Lee K.‐H. , Chi D. Y. , Kim S. E. , Choi Y. , Kim B.‐T. 
Published: April 2012

AbstractCyclopentadienyl tricarbonyl 99mTc octanoic acid (99mTc‐CpTOA; 1) was prepared in high radiochemical yield (40–63%) and shown to be stable (90% at 6 h) in human serum. Biological studies demonstrated longer retention and slower metabolism of 99mTc‐CpTOA in CCl4‐treated mice than in normal mice, possibly due to impaired β‐oxidation. These results along with good water solubility of the radioactive extracts from the liver indicated that this radiotracer was mainly metabolized via β‐oxidation in the liver. This study thus suggests that 99mTc‐CpTOA 1 holds promise for evaluation of fatty acid metabolism in the liver.
Chemical modifications of 99mTc tricarbonyl labeled single chain antibody fragments for improved in vivo behavior in tumor targeting
Authors: Stichelberger A. , Jager H. , Waibel R. , Novak‐Hofer I. , Chester K. , Schubiger P. A. 
Published: April 2012

AbstractOne of the major limitations of using intact immunoglobulins for targeting tumors is the poor penetration into tissues. Although small single chain Fv (scFv) antibody fragments have been used because of their improved kinetics, some exhibit high renal accumulation. In this study we show a significant reduction of renal accumulation of His‐tagged scFv's directly labelled with 99mTc‐tricarbonyl by use of succinic anhydride. Further decrease of renal uptake will make this approach hopefully suitable for therapeutic application, using 188/186Re(I)‐tricarbonyl.
Metabolism and localization properties of 99mTc labeled synthetic neurotensin analogs
Authors: Nock B. , Maina T. , Nikolopoulou A. , Tsipra C. , Poppe M. , Conrath P. , Tourwé D. , Chiotellis E. 
Published: April 2012

AbstractRecent reports have demonstrated that neurotensin (NT) receptors are overexpressed at high density in such devastating human neoplasms like exocrine ductal pancreatic carcinomas. Consequently, radiolabeled NT analogs can be used in the early diagnosis or even treatment of such tumors. In the present study we report on the synthesis and preclinical evaluation of four 99mTc labeled synthetic NT analogs based on the NT(8–13) sequence, known to specifically interact with the NTR1 subtype found in neoplastic cells. The biological half life of these analogs has been increased by strategic reduction of amide bonds, replacement of amino acid residues and coupling of a tetramine bifunctional chelator at the N‐terminal of resulting peptides. The affinity for the NTR1 subtype was found high in competition binding assays in WiDr cell membrane preparations. Labeling with 99mTc was quantitative under mild conditions leading to single radioactive species in high specific activities. The stability of labeled peptides in plasma, urine and kidney homogenates was found dependent on the above described modifications. The rate of internalization in WiDr cells was very high for all radiolabeled peptides, with >90% of the radioactivity accumulating in the cells within 30 min. In vivo distribution of the two most stable 99mTc NT analogs in mice xenografts revealed a specific accumulation of radioactivity in NTR1 subtype — rich cancer tissue combined with a very rapid clearance of background activity through the kidneys and the urinary system.
Effect of increased temperature on labelling efficiency of some 99mTc‐radiopharmaceuticals
Authors: Maksin T. , Djokić D. , Janković D. 
Published: April 2012

AbstractThe influence of increased temperature on the labelling efficiency with 99mTc for some compounds: pyrophosphate (PyP), dicarboxypropane diphosphonate (DPD), dimercaptosuccinate (DMS) and Sn‐colloid was investigated. The samples were exposed at 37°C for different time intervals and after that each of them was labelled with 99mTc (pertechnetate were simply injected into vials with samples). The radiochemical analyses were performed by paper and TL chromatography using different chromatography papers (Whatman N°1, SG, Schleicher&Schull) and proper mobile phases (80% methanol, 1N NaCl, acetone). Those results indicate the increases of impurity in the case of 99mTc‐PyP. In the case of 99mTc‐DPD and 99mTc‐DMS unsuitable complexes for bone and kidney image respectively were formed. There were no changes in results of quality control for 99mTc‐Sn colloid. Therefore it is very important for producer and also user of Tc‐radiopharmaceuticals to know the possible effect of bed storage and transportation condition on their quality.
Rutin labeled with technetium‐99M and its biodistribution inwistarrats
Authors: Bernardo L. C. , Oliveira M. B. N. , da Silva C. R. , Moura R. S. , Bernardo‐Filho M. 
Published: April 2012

AbstractThe use of natural products as medicines is growing along the years in the world. The rutin, a compound isolated fromRuta graveolens, is a flavonoid which has been suggested to have the capacity to protect the capillary endothelium and to reduce the triacylglycerol levels. Besides, it seems to present antioxidant characteristics and to be a great free radical scavenger. The use of technetium‐99m (99mTc) can be justified for its physical and chemistry properties. The aim of this study is to label rutin with 99mTc and to study its biodistribution inWistarrats. Firstly, rutin was dissolved in ethyl alcohol, and later incubated with stannous chloride. After that, 99mTc, as sodium pertechnetate, was added. The labeling efficiency was determined through the instant thin layer chromatography (ITLC‐SG). The biodistribution study of the rutin labeled with 99mTc was performed withWistarrats and the highest uptake was found in kidneys (0.535±0.09 % ID/g). It is possible to conclude that the rutin was successfully labeled with 99mTc.
[111In]‐DOTA‐Lys8‐Vasotocin: A new promising peptide for oxytocin receptor expressing tumors
Authors: Chinol M. , Nacca A. , Bussolati G. , Cassoni P. , Paganelli G. 
Published: April 2012

AbstractOxytocin receptors (OTR) are expressed by a large variety of human tumors. We have developed a new reagent specifically designed to transfer radionuclides to OTR‐expressing tumors. We selected Lys8‐vasotocin (LVT), an analogue of oxytocin (OT), with high affinity for OTR and coupled the chelating agent DOTA. The new reagent (DOTA‐LVT) was radiolabeled with 111In and showed specific binding to OTR positive cell lines. In vivo experiments demonstrated the receptor mediated binding of 111In‐DOTA‐LVT to OTR expressing tumors. The present study has shown that the new reagent may be promising to convey radioisotopes to OTR positive tumors although further improvements are warranted.
Synthesis and peptide coupling of a new DOTA‐based prochelator, forming neutral complexes with yttrium‐90 and indium‐111
Authors: Eisenwiener Klaus‐Peter , Reubi Jean‐Claude , Wenger Sandra , Mäcke Helmut R. 
Published: April 2012

AbstractAs a result of positive effects of the chelators DOTA and DOTAGA, when coupled to Tyr3‐octreotide, we designed a new potential chelator, DOTAtaGA, which combines these effects. DOTAtaGA has a spacer between the pharmacophoric part of the peptide and the chelator and forms neutral complexes with Yiii and InIII, as in the case of Y‐DOTA‐Tyr3‐octreotide. The corresponding prochelator DOTAtaGA(tBu)3 (1, 4, 7, 10‐tetraazacyclododecane‐1‐(1‐carboxy‐3‐carbo‐tertbutoxypropyl)‐4, 10 (carbotertbutoxymethyl)‐7‐acetamide) was synthesized in 3 steps with an overall yield of 16.5%. It was coupled to Tyr3‐octreotide, and the resulting peptide DOTAtaGA‐Tyr3‐octreotide has a ten times higher binding affinity to the somatostatin receptor subtype 2 than DOTA‐TOC.
Syntheses of new derivatives of amino acids and peptides and studies of their radioprotective activity
Authors: Kazaryan S. H. , Grigoryan K. P. , Gevondyan A. I. , Minasyan S. H. , Tonoyan V. J. , Bajinyan S. A. , Poghosyan A. S. , Malakyan M. H. , Sorenson J. R. S. 
Published: April 2012

AbstractThe synthesis of ethyl esters of 2‐salicylidene derivatives of tyrosine, γ‐amino butyric acid (GABA), and glycyl‐glycine was carried out. These Schiff base ligands present themselves as pale‐yellow crystals. These Schiff bases have been used to prepare Mn (II) complexes by allowing them to react with Mn (II) ion. Their possible structures were determined using several analytical and physical‐chemical techniques. These Mn (II) complexes are obtained as gray crystals.Cytogenetic studies of bone marrow cells from whole‐body 4.2 Gy (0.42 Gy/min dose rate) irradiated white inbred rats revealed that prior administration of 10mg/kg of the Mn chelate of the ethyl ester of the 2‐salicylidene derivative of tyrosine was radioprotective. Compared to two control groups: (I) — animals exposed to irradiation only and (II) — animals treated with vehicle before irradiation, there was a 7‐fold decrease in number of chromosome aberrations. Mn‐chelates of 2‐salicylidene GABA and glycyl‐glycine were less radioprotective.The studies compounds have just as superoxide scavanging activity.
Cellular processing of indirectly astatinated and iodinated mAb A33 in SW1222 cultured cells
Authors: Orlova A. , Sjöström A. , Ericson A. , Lebeda O. , Lundqvist H. , Carlsson J. , Tolmachev V. 
Published: April 2012

AbstractIn principle, alpha‐emitting radionuclides, such as 211At, are more efficient than beta‐emitters to inactive single disseminated cancer cells. However, cellular processing of astatinated proteins has not yet been studied in detail. In this study an anti‐colorectal cancer monoclonal antibody (mAb) A33 was indirectly labeled with 211At and for comparison with 125I. Binding and retention of radioactivity was studied in the colorectal cancer cell‐line SW1222. A similar pattern of binding and retention of the two radiohalogens was seen. The main difference found, that the retention time of astatinated mAb in SW1222 was almost two times longer, might be of advantage in radionuclide therapy.
The analogs of acetyl choline: Choline and thiocholine esters of amino acids and peptides
Authors: Kazaryan S. H. , Grigoryan K. P. , Gevondyan A. I. , Bajinyan S. A. , Malakyan M. H. 
Published: April 2012

AbstractThe synthesis was carried out to obtain choline and thiocholine esters of N‐protected and non‐protected amino acids and peptides.As the N‐protecting group the benzyloxycarbonyl group was applied, which was then removed by CH3COOH/HBr after the synthesis of β‐amino esters. Choline and thiocholine esters are obtained by the interaction of the corresponding β‐ amino esters with iodic methyl.The pharmacological studies have indicated that choline esters of both N‐protected amino acids and peptides, and non‐protected derivatives possess slight radioprotective activity.
Production of 103Pd by proton irradiation of silver
Authors: Mausner L. F. , Kolsky K. L. , Awasthi V. , Srivastava S. C. 
Published: April 2012

AbstractBrachytherapy with 103Pd (t1/2= 16.97 d) has shown significant success in treating prostate cancer. We have investigated a new high‐energy accelerator route with the Ag(p, 2pxn)103Pd reaction. Natural Ag foils were irradiated at energies from 75 to 140 MeV at the Brookhaven Linac Isotope Producer (BLIP). Radiochemical separation of Pd from the Ag target utilized chromatography with Chelex‐100TM. A thick target (0.63cm) irradiation at 140 MeV, (45_A current, 24d) produced 751GBq of 103Pd and 259 GBq of 100Pd at EOB and useful quantities of 95mTc (3.3 GBq) and 97Ru (377 GBq). A 20d decay time is required to reduce the 100Pd (t1/2 = 3.6 d) and its daughter 100Rh (t1/2 = 20.8h) to less than 2%. The radiochemical process gave a Pd chemical recovery of ∼99%, specific activity at EOB 514MBq/_g, but some Rh isotope remained. Practical production of 850 GBq per run will be possible with thick targets.
The micro‐imager — a real‐time radio‐imaging system
Authors: Filthuth Heinz 
Published: April 2012

AbstractThe Micro‐Imager (1), a new technology allows to perform quantitative analysis in real‐time on radio‐ and luminescence labelled tissue and plant sections, bacteria and cell cultures, high density micro‐arrays of DNA, on geological samples and other 2‐dimensional objects.The unique features of the instrument are very high spatial resolution (10–15 μm) and high detection sensitivity, 60% for 3H and 55Fe and 90% for all typical β‐emitters such as 14C, 35S, 1251, 1311, 33P, 32P, 99mTc.Due to the high sensitivity short living positron emitters can be very well detected such as 18F, 11C, 15O and α‐emitters as 213Bi.
An improved enantioselective synthesis of no‐carrier‐added (NCA) 6‐[18F]FLUORO‐L‐DOPA
Authors: Wang Y. X. , Zhang L. , Tang G. H. , Yin D. Z. 
Published: April 2012

Abstract6‐[18F]Fluoro‐L‐Dopa (6‐FDOPA) is the analogue of L‐Dopa, the biosynthesis precursor for dopamine. As a PET tracer, it was widely applied for the presynaptic dopamine function in cerebral studies in humans. The synthesis routes to this radiopharmaceutical could be divided into two main groups, that is, electrophilic and nucleophilic route. Lemaire et al reported a new nucleophilic synthesis procedure using a chiral phase‐transfer catalyst. A similar procedure with some improvements was described in this study. A trimethylammonium veratraldehyde triflate was synthesized and used as a precurser for the synthesis of 6‐[18F]Fluoro‐L‐Dopa by using the chiral phase‐transfer catalyst, O‐Allyl‐N‐(9)‐anthracenylcinchonidinium Bromide which was also synthesized in this study. The nca Fluorine‐18F‐fluoride was produced by the 18O(p, n) 18F nuclear reaction on enriched water. First the 6‐[19F]Fluoro‐L‐Dopa was synthesized to test the chemical structure of the synthesized end product and whole prcedure. Then the synthesis of 6‐[18F]Fluoro‐L‐Dopa was completed and identified by HPLC, TLC and MS(only the case of the 6‐[19F]Fluoro‐L‐Dopa).
An improved synthesis of 3′‐DEOXY‐3′‐[18F]fluorothymidine ([18F]FLT) and the fate of the precursor, 2, 3′‐anhydro‐5′‐O‐(4, 4′‐dimethoxytrityl)‐thymidine
Authors: Cleij M. C. , Steel C. J. , Brady F. , Ell P. J. , Pike V. W. , Luthra S. K. 
Published: April 2012

AbstractSummaryThe fate of the precursor, 2, 3′‐anhydro‐5′‐O‐(4, 4′‐dimethoxytrityl)‐thymidine was investigated during the synthesis of [18F]FLT with the aim of improving the radiochemical yield. This precursor was shown to undergo a rapid base catalysed elimination reaction and to be consumed within 5–10 min. The by‐product was identified. Modification of the synthesis has produced between 1.85–3.70 GBq (50–100 mCi) of [18F]FLT in 60 min using an automated synthesis system.
Radiolabeling of unprotected octreotide with F‐18
Authors: Panico M. , Lang L. , Sassaman M. B. , Eckelman W. C. 
Published: April 2012

AbstractOctreotide can be labeled with fluorine‐18 as a potential radiopharmaceutical for quantitative in vivo mapping of somatostatin receptors in cancer patients. A one step synthesis that does not involve blocking and unblocking of the ε‐lysine amine would prevent preparation of the blocked starting material and would eliminate the need for hydrolysis after radiolabeling. The effect of labeling the ε‐amino of lysine versus the α‐amino moiety of D‐phenylalanine has been studied previously. In general, at high pH the ε‐amine of lysine is labeled when using reactive reagents, e.g. the Bolton Hunter reagent. At lower pH values, the α‐amino moiety is labeled, but never quantitatively (1). We found that using octreotide and the N‐succinimidyl 4‐fluorobenzoate, we could obtain radiolabeling yields of >15% for the α‐amino moiety at neutral pH. The radioligand was easily separated and did not require the blocked precursor. This yield is sufficient for carrying out experiments in large animals and human subjects.
A versatile, commercially available automated synthesizer for the development and production of pet radiotracers
Authors: Hostetler E. D. , Hamill T. G. , Francis B. E. , Burns H. D. 
Published: April 2012

AbstractThe automation of routinely produced radiotracers is an important process for any PET center. Automation allows frequent, highly reproducible syntheses with large amounts of radioactivity while minimizing exposure to the radiochemist in comparison with manual radiotracer synthesis. We found the Gilson SK233 Work Station, coupled with Gilson's 735 Sampler Software and a Gilson SPE (solid phase extraction) module, to be a versatile, user‐friendly, and cost‐effective solution to our need for automation in the development and routine synthesis of radiotracers.
Production, processing and uses of 94mTc
Authors: Bigott H. M. , Mccarthy D. W. , Wüst F. R. , Dahlheimer J. L. , Piwnica‐Worms D. R. , Welch M. J. 
Published: April 2012

AbstractTechnetium‐99m is a widely used radioisotope in nuclear medicine. The characteristics of this generator‐produced radionuclide (T1/2 = 6 h, Eγ = 140.5 keV, Iγ = 87.2 %) make it an ideal isotope for single photon emission computed tomography (SPECT). Technetium‐94m has a half‐life of 52 minutes and a positron branching ratio of 72 %, with Eβ+max of 2.44 MeV. Technetium‐94m undergoes the same chemistry as 99mTc, but has characteristics suitable for imaging using positron emission tomography (PET), with which more quantitative measurements of radiopharmaceutical uptake, biodistribution and clearance can be made.
Synthesis and in vivo evaluation (PIG) of the selective seretonin reuptake inhibitor [11C]NS 2456
Authors: Smith D. F. , Bender D. , Marthi K. , Cumming P. , Hansen S. B. , Peters D. , Nielsen E. ØStergaard , Scheel‐Krüger J. , Gjedde A. 
Published: April 2012

AbstractWe evaluated a new selective serotonin reuptake inhibitor, NS 2456, to determine whether it is suited for use in PET. Racemic NS 2456 [(1RS, 5SR)‐8‐methyl‐3‐[4‐trifluoromethoxy phenyl]‐8‐azabicyclo [3.2.1]oct‐2‐ene] and its N‐demethylated analogue, racemic NS 2463, selectively inhibit serotonin uptake in rat brain synaptosomes. For uses in PET of the living porcine brain, racemic [11C]NS2463 as well as its radiolabelled enantiomers were used. The compounds crossed the blood‐brain‐barrier rapidly and accumulated preferentially in regions rich in serotonin uptake sites. However their binding potentials were relatively low and no stereoselectivity was found. Thus, neither [11C]NS 2456 nor [11C]‐labelled enantiomers are ideal for PET neuroimaging of neuronal serotonin uptake sites.