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Technetium, the missing element.

The history of the discovery of technetium is reviewed within the framework of the discovery and production of artificial radioactivity in the twentieth century. Important elements of this history are the accidental production of this element in a cyclotron in Berkeley, California, USA, a machine devised by Ernest Orlando Lawrence, and its subsequent discovery in 1937 by Carlo Perrier and Emilio Segrè in scrap metal parts sent by Lawrence to Palermo, Italy by mail. A detailed account is given of the steps taken; the history of the later discovery of the technetium-99m isotope in 1938 is likewise examined. Sources of natural and artificial technetium are briefly discussed.

Cyclotrons↗

Lanthanide concentrations in freshwater plants and molluscs, related to those in surface water, pore water and sediment. A case study in The Netherlands.

Industrial emissions of lanthanides to aquatic ecosystems increase, but knowledge of the environmental fate of these metals is limited. Here we focus attention upon the distribution of lanthanides in freshwater ecosystems, describing lanthanide partitioning between sediment, water and biota. Since lanthanides are often used as oxidation-state analogues for actinides, their distribution can reflect long-term behaviour of the radioactive transuranics. Concentrations of all 14 naturally occurring lanthanides were measured by ICP-MS in Sago pondweed (Potamogeton pectinatus), common duckweed (Lemna minor), seven different mollusc species (tissue and shell), two sediment fractions (< 2 mm and < 63 microm), surface water and sediment pore water from five locations in The Netherlands. In all samples, the typical 'saw-tooth' lanthanide pattern was observed, which implies that lanthanides are transported as a coherent group through aquatic ecosystems. Typical deviations from this pattern were found for Ce and Eu and could be explained by their redox chemistry. The variation in concentrations in abiotic fractions was limited, i.e. within one order of magnitude. However, variations of up to three orders of magnitude were observed in biotic samples, suggesting different affinities among organisms for lanthanides as a group, with significant differences only among molluscs and pondweed samples in relation to sampling location. For P. pectinatus it was shown that pore water was the most important lanthanide source, and for snails, food (plants) seems to be the dominant lanthanide source. Lanthanides were not equally distributed between mollusc shell and tissue and the ratio of lanthanide concentrations in shell and tissue were dependent on the sampling location. Shells contained much lower concentrations and were relatively enriched in Eu, and to a lesser extent in Ce. Bioconcentration factors for lanthanides in plants and snails relative to surface water were typically between 10000 and 100000 l x kg(-1) dry matter, while sediment-water partition coefficients were between 100000 and 3000000 l x kg(-1) dry matter. There was a low extent of biomagnification in the plant-to-snail system, with a maximum biomagnification factor of 5.5. Many distribution coefficients displayed a slight decrease with atomic number. This can be attributed to the general increase in ligand stability constants with atomic number, keeping the heavier lanthanides preferentially in solution.

Animals↗

Comparative uptake of plutonium from soils by Brassica juncea and Helianthus annuus.

Plutonium uptake by Brassica juncea (Indian mustard) and Helianthus annuus (sunflower) from soils with varying chemical composition and contaminated with Pu complexes (Pu-nitrate [239Pu(NO3)4], Pu-citrate [239Pu(C6H5O7)], and Pu-diethylenetriaminepentaacetic acid (Pu-DTPA [239Pu-C14H23O10N3]) was investigated. Sequential extraction of soils incubated with applied Pu was used to determine the distribution of Pu in the various soil fractions. The initial Pu activity levels in soils were 44.40-231.25 Bq g(-1) as Pu-nitrate Pu-citrate, or Pu-DTPA. A difference in Pu uptake between treatments of Pu-nitrate and Pu-citrate without chelating agent was observed only with Indian mustard in acidic Crowley soil. The uptake of Pu by plants was increased with increasing DTPA rates, however, the Pu concentration of plants was not proportionally increased with increasing application rate of Pu to soil. Plutonium uptake from Pu-DTPA was significantly higher from the acid Crowley soil than from the calcareous Weswood soil. The uptake of Pu from the soils was higher in Indian mustard than in sunflower. Sequential extraction of Pu showed that the ion-exchangeable Pu fraction in soils was dramatically increased with DTPA treatment and decreased with time of incubation. Extractability of Pu in all fractions was not different when Pu-nitrate and Pu-citrate were applied to the same soil. More Pu was associated with the residual Pu fraction without DTPA application. Consistent trends with time of incubation for other fractions were not apparent. The ion-exchangeable fraction, assumed as plant-available Pu, was significantly higher in acid soil compared with calcareous soil with or without DTPA treatment. When the calcareous soil was treated with DTPA, the ion-exchangeable Pu was comparatively less influenced. This fraction in the soil was more affected with time of incubation. The lowest extractable Pu was from a pH 6.55 Crockett soil that contained the highest clay compared to the other two soils. Extractable soil Pu was largely affected by soil pH and the amounts of clay, salt, metal oxide, and carbonate.

Biodegradation, Environmental↗

Metallic colloid nanotechnology, applications in diagnosis and therapeutics.

In recent years the fields of medicine and biology assist to an ever-growing innovation related to the development of nanotechnologies. In the pharmaceutical domain, for example, liposomes, polymer based micro and nanoparticles have been subjects of intense research and development during the last three decades. In this scenario metallic particles, which use was already suggested in the first half of the '80, are now experiencing a real renaissance. In the field of diagnosis, magnetic resonance imaging is one of the first and up to now the most developed application of metallic particles. But beside this application, a very new generation of biosensors based on the optical properties of colloidal gold and fluorescent nanocrystals, called quantum dots seems to be ready to be implemented in diagnosis and medical imaging. Concerning therapeutic applications, the potentialities of metal nanoparticles to help fulfilling the need of time and space controlled release of drugs has been intuited for a long time. Nowadays, magnetically guided carriers or thermal responsive matrices, in which drug release is triggered by the heating of metal nanoparticles, are effective examples of their application in drug delivery, while more recently efforts to develop metallic nanoobjects to be used as vectors of nucleic acids for vaccination and transfection have been multiplied. In the future, one of the most interesting challenges is certainly the use of metallic nanoparticles for an innovating, effective and selective physical treatment of solid tumors via targeted intracellular hyperthermia.

Animals↗

[The correction of free-radical oxidation processes in patients with chronic cholecystitis subjected to ionizing radiation exposure].

An activation was found of lipid peroxidation system as well as suppression of antioxidant defence tending to be more profound in blood erythrocytes, in 47 patients with chronic cholecystitis having been in the zone of abnormal radiation. Correction of the above alterations revealed unithiol, clinical and biochemical effects to be pronounced compare with those or tocopherol. Direct antioxidant effect or unithiol, its capability of serving as an antidote of heavy of heavy metals are believed to account for the above observation.

Adult↗

Radiolabeled alpha-melanocyte-stimulating hormone analogs for receptor-mediated targeting of melanoma: from tritium to indium.

Following the first synthesis of tritiated alpha-melanocyte-stimulating hormone (alpha-MSH, alpha-melanotropin) in 1974 by Medzihradszky et al., several alpha-MSH analogs were designed containing between 2 and 12 tritium atoms, the latter of which displayed a specific radioactivity of 12.21 GBq/micromol (330 Ci/mmol). Similarly, radioiodinated alpha-MSH analogs of high purity, full biological activity and a specific radioactivity of approximately 140 GBq/micromol were obtained. Although tritiated and radioiodinated alpha-MSH became indispensable tools as tracer molecules for numerous in vitro and in vivo studies, above all for receptor identification and characterization as well as for structure-activity studies, they did not fulfill the criteria required for therapeutic in vivo targeting of metastatic melanoma. Therefore, we recently developed alpha-MSH analogs containing the universal metal chelator 1,4,7,10-tetraazacyclododecane-1,4,7,10-tetraacetic acid (DOTA) in different positions of the molecule. As DOTA can equally well incorporate diagnostic (e.g. (111)In, (67,68)Ga) and therapeutic (e.g. (90)Y, (67)Cu) radionuclides, DOTA-MSH compounds may serve for both melanoma scintigraphy and therapy. The analog DOTA-[betaAla(3), Nle(4), Asp(5), D-Phe(7), Lys(10)]-alpha-MSH(3-10) (DOTA-MSH(OCT)), which contains the metal chelator at its N-terminal end, displayed good in vitro MC1R affinity (IC(50) 9.21 nm). In vivo, [(111)In]DOTA-MSH(OCT) exhibited a favorable biodistribution profile after injection in B16-F1 tumor-bearing mice. The radiopeptide was rapidly cleared from blood through the kidneys and, most importantly, accumulated preferentially in the melanoma lesions. Lung and liver melanoma metastases could be clearly imaged on tissue section autoradiographs 4 h after injection of [(111)In]DOTA-MSH(OCT). A comparative study of [(111)In]DOTA-MSH(OCT) with [(111)In]DOTA-[Nle(4), D-Phe(7)]-alpha-MSH ([(111)In]DOTA-NDP-MSH) demonstrated the superiority of the DOTA-MSH(OCT) peptide, particularly with respect to the amount of radioactivity taken up by non-malignant organs, including bone, the most radiosensitive tissue. These results demonstrate that [(111)In]DOTA-MSH(OCT) specifically targets melanoma metastases and represents a lead compound for the development of therapeutic DOTA-MSH analogs.

Animals↗

Different behaviour of 63Ni and 59Fe during absorption in iron-deficient and iron-adequate jejunal rat segments ex vivo.

Nickel exhibits low oral toxicity. It shares the absorptive pathways for iron, though there are substantial quantitative differences in handling of both metals. To analyse these differences more closely, jejunal segments from iron-deficient and iron-adequate rats were luminally perfused ex vivo with 59Fe and 63Ni at six different concentrations (1-500 micromo1/l) under steady state conditions. 59Fe over-all absorption increased 2.0-4.6-fold in iron-deficiency at luminal concentrations between 1 and 100 micromol/l, while 63Ni absorption increased to a much lower extent (2.6-fold at 1 micromol/l and 1.5-fold at higher luminal concentrations). Moreover, there was a 5-7-fold higher concentration for 63Ni in the jejunal tissue than in the absorbate at luminal concentrations above 50 micromol/l which was not observed at 1 micromol 63Ni/l and not for 59Fe. 63Ni tissue load showed a linear and a saturable fraction. In iron-deficiency the saturable 63Ni fraction increased 4-fold as compared to only 1.5-fold increments for 59Fe. Moreover, a substantially higher share of 63Ni was retained in the jejunal tissue at high as compare to low luminal concentrations after perfusion had been continued without luminal radioactivity. This was not found for 59Fe and suggests a concentration-dependent block of 63Ni export across the enterocytes' basolateral membrane. To explain these results one may speculate that 63Ni may bind more tightly to tissue ligands than 59Fe due to the higher thermodynamic and kinetic stability of nickel complexes. In particular, nickel may bind to a basolateral population of metal carriers and block its own basolateral transfer in a concentration-dependent manner. Tight 63Ni binding to non-specific jejunal ligands is responsible for the unaltered high linear fraction of jejunal 63Ni load in iron-deficient and iron-adequate segments. Binding of 63Ni to food and tissue ligands in the small intestine may, thus, be a likely explanation for the low oral nickel toxicity.

Animals↗

STUDIES ON INHIBITION OF INTESTINAL ABSORPTION OF RADIOACTIVE STRONTIUM. I. PREVENTION OF ABSORPTION FROM LIGATED INTESTINAL SEGMENTS.

A method is reported which permits selective suppression of absorption of radioactive strontium from ingested food material, permitting the calcium to be available to the body. Studies were carried out in vivo by injection of Sr(89) and Ca(45) in the presence of inert carrier into ligated intestinal segments in rats, and the amount of absorption was measured by standard monitoring techniques. The pattern of absorption of both ions is very similar but the rate of absorption is different. It was found that the polyelectrolyte, sodium alginate, obtained from brown algae (Phaeophyceae), injected simultaneously with radiostrontium effectively reduces the absortion of Sr(89) from all segments of the intestine by as much as 50-80% of the control values. No significant reduction in absorption of Ca(45) was observed in equivalent concentrations. The reduction in blood levels of Sr(89) and in bone uptake corresponded to the absorption pattern. The difference in the effect on strontium and calcium absorption may be due to differences in the binding capacity of sodium alginate from the two metal ions under the conditions present in vivo.

Absorption↗

Application of nonlinear analysis methods for identifying relationships between microbial community structure and groundwater geochemistry.

The relationship between groundwater geochemistry and microbial community structure can be complex and difficult to assess. We applied nonlinear and generalized linear data analysis methods to relate microbial biomarkers (phospholipids fatty acids, PLFA) to groundwater geochemical characteristics at the Shiprock uranium mill tailings disposal site that is primarily contaminated by uranium, sulfate, and nitrate. First, predictive models were constructed using feedforward artificial neural networks (NN) to predict PLFA classes from geochemistry. To reduce the danger of overfitting, parsimonious NN architectures were selected based on pruning of hidden nodes and elimination of redundant predictor (geochemical) variables. The resulting NN models greatly outperformed the generalized linear models. Sensitivity analysis indicated that tritium, which was indicative of riverine influences, and uranium were important in predicting the distributions of the PLFA classes. In contrast, nitrate concentration and inorganic carbon were least important, and total ionic strength was of intermediate importance. Second, nonlinear principal components (NPC) were extracted from the PLFA data using a variant of the feedforward NN. The NPC grouped the samples according to similar geochemistry. PLFA indicators of Gram-negative bacteria and eukaryotes were associated with the groups of wells with lower levels of contamination. The more contaminated samples contained microbial communities that were predominated by terminally branched saturates and branched monounsaturates that are indicative of metal reducers, actinomycetes, and Gram-positive bacteria. These results indicate that the microbial community at the site is coupled to the geochemistry and knowledge of the geochemistry allows prediction of the community composition.

Bacteria↗

Delivery of salbutamol pressurized metered-dose inhaler administered via small-volume spacer devices in intubated, spontaneously breathing rabbits.

Little is known about the ability of small-volume valved spacer devices to deliver a significant amount of an aerosolized drug to the lungs of babies. This study compared the in vitro delivery of salbutamol administered via Aerochamber-Infant (145 mL), Babyhaler (350 mL), and metallic NES-spacer (250 mL), as well as the in vivo delivery using an animal model. The lung deposition study of technetium-99m-labeled salbutamol was conducted in six anesthetized, intubated (3.0-mm endotracheal tube simulating oropharyngeal deposition), spontaneously breathing New Zealand White rabbits, a model for 3-kg babies. Each rabbit was studied on three separate occasions, once with each spacer device. The amount of radioactivity deposited in the spacer device, the endotracheal tube, the lungs, or the body was measured by a gamma camera and expressed as a percentage of the emitted labeled dose. The emitted dose and particle size distribution of salbutamol via the three spacer devices were measured using unit dose sampling tubes and an eight-stage Anderson cascade impactor, respectively. The results were compared by ANOVA or Student-Newman-Keuls test when indicated. In vitro, the NES-spacer and Babyhaler were equivalent for delivering particles <5.8 microm in diameter (NES-spacer = Babyhaler > Aerochamber-Infant; p < 0.05). In vivo, the lung and body deposition was low with all spacer devices (range: 0.52-5.40% of the delivered dose) but greater with the NES-spacer than with the Aerochamber-Infant or the Babyhaler (5.40 +/- 2.40%, 2.91 +/- 0.86%, 0.52 +/- 0.46%, respectively; p = 0.002). These results suggest the metal-valved spacer device may be preferable for delivering pressurized aerosols to spontaneously breathing infants.

Administration, Inhalation↗

Targeting radiopharmaceuticals--II. Evaluation of new trivalent metal complexes with different overall charges.

Three new multidentate ligands designed to have high affinity for Ga3+, In3+ and Fe3+ have been synthesized. N-(2-hydroxybenzyl)-N'-pyridoxylethylenediamine-N,N'-diacetic acid (HBPLED), N-(2-hydroxy-3,5-dimethylbenzyl)-N'-(3-hydroxy-1,2,5-trimethyl-4- pyridylmethyl)ethylenediamine-N,N'-diacetic acid (Me4HBPLED) and N,N'-bis(3-hydroxy-1,2,5-trimethyl-4-pyridylmethyl) ethylenediamine-N,N'-diacetic acid (DMPLED). These ligands give metal-ligand (M-L) complexes with (M = Ga3+, In3+, Fe3+) overall charges of -1.0 and +1, respectively. The 67Ga, 68Ga and 111In complexes of each of the three ligands and the 59Fe complex of Me4HBPLED were prepared, characterized and their biodistributions determined in rats after intravenous injection. Despite the differences in overall charge, the biological behavior of all three 111In complexes were similar, in that the radioactivity cleared rapidly via the kidney. The biodistributions of the 68Ga and 67Ga complexes were comparable to that of the 111In complex counterpart. Also, the 59Fe-Me4HBPLED biodistribution was not significantly different from those of the 68Ga- and 111In-Me4HBPLED. The renal clearance rate seems insensitive to the overall M-L charge; suggesting that the hydrophilic periphery of the ligand rather than the overall molecular charge determines the biological fate (with respect to renal clearance).

Animals↗

Microscale preparation of natural and labeled oxysterols.

The preparation of cholesterol and radiocholesterol oxidation products on a microscale is difficult. Cholesterol generally resists oxidation unless it is well dispersed under controlled conditions. A method was developed to reliably produce 7 alpha- and 7 beta-hydroxycholesterol and 7-ketocholesterol. Small changes in pH, metal ions present, or in the colloidal dispersion, resulted in production of completely different oxysterols. Attempts to oxidize aged radiocholesterol were not successful even after purification by several thin-layer chromatographic steps, and this appeared to be due to a time-related change in the radioactive material. Fresh radiocholesterol oxidized readily.

Carbon Radioisotopes↗

A novel 111In-labeled antisense DNA probe with multi-chelating sites (MCS-probe) showing high specific radioactivity and labeling efficiency.

A multi-aminolinked oligodeoxynucleotide (ODN) was synthesized by substitution of dT with aminolinked dU in the sequence, following conjugation with isothiocyanobenzyl-EDTA (IBE) for 111In labeling. As a model target gene, the c-erbB-2 protooncogene was used. The probability of the number of aminolinked dU in the 20mer ODN was 5, but there were actually 3 and 4 in the selected antisense and sense ODNs, respectively. The IBE/ODN conjugation levels of probes with multi-chelating sites (MCS-probe) were 1.6 (antisense) and 2.4 (sense), more than 50 times higher than those of our previous studies using 5'-end aminolinked ODNs (IBE/ODN = 0.03). Labeling studies using the MCS-probe and 111In indicated that specific radioactivity as high as 48 MBq/nmol could be obtained with a labeling efficiency of over 90%. The 111In-antisense-MCS-probe could bound to sense ODN under physiological conditions, but the 111In-sense-MCA-probe could not. Thus, side-chain modification of ODN for metal labeling is considered to be useful for antisense techniques.

Antisense Elements (Genetics)↗

Zinc ions inhibit the QP center of bovine heart mitochondrial bc1 complex by blocking a protonatable group.

Bovine heart bc1 complex is reversibly inhibited by zinc ions with an inhibition constant KI of 10(-7) M at pH > or = 7.0. Binding of zinc is at least a factor of 10 tighter than binding of any other metal ion tested. Essentially complete inhibition of ubihydroquinone:cytochrome c oxidoreductase activity is observed at concentrations of [Zn2+] > 5 microM. Zinc does not affect the Km for the substrates, ubihydroquinone or cytochrome c, but zinc inhibits reduction of the cytochromes by ubihydroquinone through the QP center. A radioactive binding assay using 65Zn revealed one high affinity binding site per bc1 complex with KD < or = 10(-7) M at pH = 7.0 and 3-4 additional low affinity binding sites (KD > 2 x 10(-6) M). Zinc binding does not depend on the redox state of the high potential chain (iron-sulfur protein and cytochrome c1). Zinc binds 3 times tighter to Fe-S-depleted bc1 complex indicating that the zinc binding site is not on the "Rieske" iron-sulfur protein in contrast to a recent report by Lorusso et al. (Lorusso, M., Cocco, T., Sardanella, A.M., Minuto, M., Bonomi, F., and Papa, S. (1991) Eur. J. Biochem. 197, 555-561). Zinc binds to a site which has the same affinity for zinc as for protons. We conclude that the zinc binding site is close to a protonatable group of the bc1 complex with pKa = 7.2 which has not been identified previously. We propose that this group is part of the proton channel at the hydroquinone oxidation center of the bc1 complex.

Animals↗

Wire or coated balloon? Searching for an optimal source for intravascular brachytherapy with beta emitters using (32)P as an example.

This study identifies basic dosimetric differences between two designs for intravascular brachytherapy (IVBT) in current clinical practice and ongoing trials and their clinical implications within beta emitting systems using P-32 as an example. The two designs are (i) the wire-type source, where the radioactive source material is confined to a wirelike structure within the vessel lumen, and (ii) the balloon-surface source, where the radioactive source material is distributed over a surface area (balloon-wall) which is brought in close proximity with the vessel wall. Using Monte Carlo simulations with the EGS4 code, the target coverage, the influence of centering errors, and the perturbation of the dose distribution caused by metallic stents have been compared. The radial dose fall-off in the target region was found to be steeper for balloon surface systems compared with wire systems. The inner lumen wall dose for a balloon surface source was 25% higher than that for a wirelike source (2.5 mm vessel diameter). However, the comparably shallower fall-off from wire-type systems is very sensitive to centering uncertainties. A 0.5 mm displacement, for example, will cause the dose to change by a factor of 2 at the inner vessel wall and by a factor of 1.8 at the prescription point. It is shown that the interference from metallic stents is more significant for wire-type systems than it is for balloon-surface-type systems, where double the dose variation beyond the stent at the radial prescription distance may occur. Centering uncertainties dominate the dose perturbation effects for wire-type systems. Balloon-surface-type designs show a more predictable dose distribution that features, however, a higher inner vessel surface dose. Since a direct clinical comparison of systems of both types is not likely, these findings should be considered when interpreting clinical results from treatments with either type of source and, possibly, for future source design.

Beta Particles↗

A new tool for laboratory studies on volatilization: extension of applicability of the photovolatility chamber.

Volatilization from soil and plant surfaces after application is an important source of pesticide residues to the atmosphere. The laboratory photovolatility chamber allows the simultaneous measurement of volatilization and photodegradation of 14C-labeled pesticides under controlled climatic conditions. Both continuous air sampling, which quantifies volatile organic compounds and 14CO2 separately, and the detection of surface-located residues allow for a mass balance of radioactivity. The setup of the photovolatility chamber was optimized, and additional sensors were installed to characterize the influence of soil moisture, soil temperature, and evaporation on volatilization. The modified flow profile in the glass dome of the chamber arising from the use of a high-performance metal bellows pump was measured. Diminished air velocity near the soil surface and a wind velocity of 0.2 m/s in 3 cm height allowed the requirements of the German guideline on assessing pesticide volatilization for registration purposes to be fulfilled. Determination of soil moisture profiles of the upper soil layer illustrated that defined water content in the soil up to a depth of 4 cm could be achieved by water saturation of air. Cumulative volatilization of [phenyl-UL-14C]parathion-methyl ranged from 2.4% under dry conditions to 32.9% under moist conditions and revealed the clear dependence of volatilization on the water content in the top layer.

Air↗

X-ray attenuation coefficients of high-atomic-number, hexanuclear transition metal cluster compounds: a new paradigm for radiographic contrast agents.

RATIONALE AND OBJECTIVES: The purpose of this study was to examine the radiologic attenuation properties of the parent cluster compounds, particularly attenuation as a function of discrete photon energy, before investigating ligand substitutions, which are necessary to improve cluster biocompatibility and to impart desirable physicochemical properties. MATERIALS AND METHODS: The linear attenuation coefficients for solutions of the cluster compounds Ta6Br14, K8Ta6O19, and (H3O)2W6Cl14 were determined at 60, 80, 103, 122, and 140 keV from gamma-ray transmission measurements with americium-241, xenon-133, gadolinium-153, cobalt-57, and technetium-99m radioactive sources. Transmission measurements were obtained for a fixed time interval that ensured a statistically accurate count distribution exceeding 20,000 counts through the sample for each trial. RESULTS: On a strictly mole per liter basis, a 0.075 mol/L aqueous solution of K8Ta6O19 showed 1.08 times the attenuation of 0.063 mol/L aqueous iohexol at 60 keV and 3.30 times the attenuation at 80 keV. Similarly, a 0.05 mol/L methanolic solution of (H3O)2W6Cl4 showed 0.96 times (96%) the attenuation of 0.063 mol/L aqueous iohexol at 60 keV but 3.09 times the attenuation of the iohexol solution at 80 keV. Attenuations of 0.063 mol/L aqueous iohexol and 0.0125 mol/L Ta6Br14 (ie, at approximately one-fifth the iohexol concentration) were comparable at greater than 60 keV. CONCLUSION: These results confirm the theoretic potential for use of early transition metal cluster compounds as radiographic contrast agents. At higher x-ray energies, cluster compounds demonstrate multiplied x-ray attenuation relative to iodinated contrast agents.

Contrast Media↗

Synthesis, tissue distribution and tumor uptake of 99mTc- and 67Ga-tetrasulfophthalocyanine.

Complexes of tetrasulfophthalocyanine with 99mTc, 69Ga and 67Ga were prepared by the condensation of sulfophthalic acid with the appropriate metal-species. The Ga-complex was also obtained by exchange of the central hydrogens of the empty tetrasulfophthalocyanine. The labeled complexes were purified by thin layer chromatography and characterized by their chromatographic properties. Their biodistribution in rabbits and tumor-bearing rats revealed that most of the radioactivity accumulated in the kidneys, liver, ovaries, adrenals and spleen. Comparison of these distribution pattern with those of [99mTc]pertechnetate and 67Ga-citrate confirmed the in vivo stability of the labeled complexes. The 67Ga-complex reached better tumor-to-blood and tumor-to-muscle ratios than 67Ga-citrate.

Adenocarcinoma↗