Uptake and conversion of radioactive iodine (I131) by thyroid gland in vivo and in vitro in tourniquet shock in rats.
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Animals↗
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Results for “IODINE AND COMPOUNDS RADIOACTIVE”
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The radioactive labeling of polypeptide hormones with myeloperoxidase in solid state comparison with chloramine T method.
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Chloramines↗
A novel [125I]iodinated carboxypeptidase A substrate detects a metallopeptidase activity distinct from carboxypeptidase A in brain.
We have designed two radioactive substrates, hippuryl-L-[3H]phenylalanine and 3-(p-hydroxy, m-[125I]phenyl)propionic acid ([125I]Bolton reagent) derivative of L-arginyl-L-phenylalanine, i.e. [125I]BRF, for a highly sensitive assay of carboxypeptidase A (CPA) activity. After cleavage of the C-terminal phenylalanine residue by CPA, the radioactive product of the reaction was conveniently separated by polystyrene bead chromatography. Using [125I]BRF, typical CPA activity inhibited by 1 microM 2-benzyl-3-mercaptopropanoic acid was detected in extracts from rat pancreas or intestine. In brain and some other tissues, however, [125I]BRF-hydrolyzing activity was only inhibited by this compound in 1000-fold higher concentration, suggesting the participation of a metallopeptidase distinct from CPA.
Animals↗
A facile method for post-conjugation prosthetic radioiodination of "mini-peptides".
Prosthetic radioiodination methods were developed to facilitate the labeling of proteins devoid of tyrosine(s) or when these moieties are crucial for biological activity. This method involves the use of the so-called Bolton-Hunter-type reagents. However, the in vivo instability of the label prompted the search for more stable groups. Although these second generation reagents have worked well with proteins and peptides, the current reaction scheme takes a long time to perform. A simplified method may be more appropriate especially from radiation safety point of view. More importantly, for short-lived halogens, advantage may be gained utilizing a shorter reaction time. Recently we reported on the radioiodination of interleukin-8 (IL-8) using the pyridine carboxylate-derived activated ester. We have successfully conjugated this prosthetic group to tri- and tetrapeptides harboring the somatostatin (SST) receptor recognition units and characterized by HPLC and MS. The radioiodination was accomplished using the Iodogen method in a reasonable yield (mean=60%). The total synthesis time was approximately 60 min, which was 3-4 times shorter than the classical two-step method. Preliminary biodistribution of the radiolabeled peptide showed uptake in some of the organs known to express SST receptors. Injection of a low specific activity tracer significantly decreased the retention of radioactivity in these organs.
Animals↗
Striatal and extrastriatal imaging of dopamine D2 receptors in the living human brain with [123I]epidepride single-photon emission tomography.
The iodine-123 labelled ligand benzamide epidepride was evaluated as a probe for in vivo imaging of striatal and extrastriatal dopamine D2 receptor sites in the human brain. Four healthy males were imaged with a high-resolution single-photon emission tomography scanner. Striatal radioactivity peaked at 3 h after injection. The specific binding in the striatum was 0.91+/-0.03 at 3 h and this ratio steadily increased with time. Extrastriatal radioactivity was highest in the thalamus, in the midbrain and in the temporal cortex, and peaked at 45-60 min after injection of tracer. A smaller amount of radioactivity was found in the parietal, frontal and occipital cortices. Two radioactive metabolites were observed, of which one was more lipophilic than the parent compound. The radiation burden to the patient was 0.035 mSv/MBq (effective dose equivalent). The preliminary results showed that [123I]epidepride can be used for imaging striatal and extrastriatal dopamine D2 receptor sites in the living human brain.
Adult↗
Degradation of tetraphenylphosphonium bromide at high pH and its effect on radionuclide solubility.
Recently, tetraphenylphosphonium bromide (TPPB) has been used to remove technetium from some radioactive waste streams. However, before TPPB could be approved for use it was necessary to show that TPPB and its degradation products would not have a significant detrimental effect on post-closure performance of a radioactive waste repository. TPPB is known to be stable at neutral pH, however, under alkaline conditions it degrades by an alkaline hydrolysis mechanism to triphenylphosphonium oxide (TPPO). Degradation can also occur by radiolysis to produce triphenylphosphine (TPP). The kinetics of the alkaline hydrolysis degradation of TPPB is described and the solubility of europium, iodine, nickel, technetium(VII) and uranium(VI) in aqueous solutions of TPPB and its degradation products is reported. These results were used to support the use of TPPB in removing technetium from some waste streams.
Hydrolysis↗
[Incineration system for the disposal of 125I-radioimmunoassay test tube wastes--confirmation of 125I decay in wastes].
Before incineration of disposed RIA test tubes, residual 125I radioactivity should be measured for the purpose of radiation safety. This confirmation method has been carried out according to the followings: Residual 125I radioactivity of test tubes in the plastic bag was measured from outside with the low-energy gamma-ray survey meter (S1371, Ohyo Kohken CO., Ltd.) newly developed by one of the authors. Gaseous 125I released from the residual 125I-compounds in test tubes by radiation self decomposition was adsorbed by the activated carbon fiber filter (ACFF), and was measured. From the above 2 methods, the minimum detectable concentration of residual 125I in waste tubes would be reached under a level of about 100 mBq/g (2.8 X 10(-6) muCi/g).
Iodine Radioisotopes↗
Uptake and release of iodine-labelled m-iodobenzylguanidine in a neuroblastoma cell culture system and its importance in neuroblastoma therapy.
A neuroblastoma cell line was established from bone marrow of a patient in stage IV of the disease and used as a model system in order to elaborate experimental data of importance in neuroblastoma therapy, such as cell-drug interactions, the mode of uptake and conditions for storage and release. m-Iodo benzylguanidine (MIBG) is rapidly taken up from culture medium, giving high concentrations of cell-bound radioactivity reaching a maximum level 4 h after the addition of the compound. A removal of the radiopharmacon from the culture medium causes a dramatic loss of cell-associated radioactivity, suggesting that neuroblastoma cells are not able to retain MIBG in a drug-free environment. Replacement of labelled by unlabelled MIBG prevents a similar release and maintains high levels of cellular radioactivity. Variations of cell culture conditions only result in minor changes of uptake rates, whereas a pretreatment with drugs used in neuroblastoma chemotherapy harms the cells extensively: even after a short-term exposure the cells lose the capacity for MIGB uptake and fail to recover within a long period of incubation in growth medium. The importance of our results is discussed, leading to the following suggestions: 1. The performance of radiotherapy with labelled MIBG is recommended prior to the chemotherapy protocols. 2. Therapeutically effective radioactivity in tumor tissues may be maintained by the additional infusion of unlabelled MIGB.
3-Iodobenzylguanidine↗
Intrinsic proteins of the intestinal microvillus membrane. Iodonaphthylazide labeling studies.
Isolated brush border membranes of the intestinal epithelial cell were labeled with a hydrophobic photoactive compound [125U]iodonaphthylazide. High incorporation of the radioactive naphthylazide was noted for molecular weight bands of 99 000, 86 000, 65 000, 54 000 and 30 000. Minimal labeling occurred in the higher bands of 300 000, 135 000, 125 000 and 17 000. The iodonaphthylazide label was not removed by extensive papain digestion whereas chloramine T iodinated membranes released radioactivity under the same conditions. Neither enzymatic nor transport activities were inhibited by the presence of iodonaphthylazide or the irradiation process. On the basis of the presented data it is concluded that the iodonaphthylazide unspecifically labels those portions of membrane proteins which are inserted into the lipid bilayer matrix.
Alkaline Phosphatase↗
[Analysis of iodine compounds in young rat skin in the period of suckling and in the adult. Effect of perchlorate].
In the suckling and adult rats equilibrated or no by 125I, cutaneous iodine analysed by dialysis and chromatography techniques (Dowex and Sephadex) was the purpose of this study. Dialysis studies had shown that most of steady or labelled skin iodine had an iodide form (90 to 95% of the total iodine). There were at least two intracellular iodide pools: the first one was quickly dialysable, in fact about 60 percent of initial radioactivity represented the intracellular iodide equilibrated with extracellular fluid. The other one wasn't or was little dialysable representing probably the cutaneous iodide storage compartment. Chromatography studies (Dowex or Sephadex) demonstrated that the skin of the young and adult rat contained T4 and T3 hormones in a small percentage. The iodide represented a value more than 90% of initial total radioactivity. Results concerning kinetic skin iodine, eight and twenty four hours after LT4(125)I injected to adults and to control and iodine deficient ten day old rats, confirmed those obtained here by Dowex chromatography and previous ones. Triiodothyronine (T3) might have an origin either in thyroid synthesis or in deiodination of T4. Consequently we may say that the skin of the 10 day and 14 day old rats presented a great accumulation of iodide. The perchlorate inhibited this storage. Indeed, in young deficient iodine rats at birth, cutaneous iodide concentrations were reduced whereas those of T4 and T3 as well as the ratio T3/T4 haven't been modified. Therefore the iodine deficiency seemed to have a few effects on the skin deiodinating activity. Indeed the skin of iodine deficient immature rat became unable to accumulate iodide. The main effect of the skin iodine deficiency was the inhibition of iodide transport from the extracellular fluid to the intracellular one, but not inside cellular structures.
Animals↗
Distribution behaviour of 131-iodine labelled trans-N,N'-bis-(ethoxy-carbonyl)-N-[4-(3-iodo-4-methoxyphenyl)butyl]-N' -5- phenylpentyl)-1,4-cyclohexanedimethanamine.
The title compound 9, which is a prodrug, and its active metabolite 7 were labelled with 131I (7*/9*) to investigate their pharmacokinetic behaviour, including the distribution between stomach, gut, muscle, blood, lung, liver, kidney, adrenal gland, heart, and spleen. Four hours after oral administration of 7* to mice only 3% of the dose had been absorbed from the g.i. tract. After 24 h 54% of the radioactivity still is found the gut, predominantly in the small intestine. These results explain why 7, which is a potent antiplatelet drug in vitro, shows no antithrombotic effect in vivo. In contrast, the produg 9/9* is absorbed considerably, i.e. up to 50% in 4 h from the g.i. tract depending on the dose applied and the vehicle used. At doses in the micromolar range the absorption appears to be diffusion limited. The highest concentrations are found in the liver and the kidneys suggesting a first pass effect of 7 followed by renal excretion. From the blood levels achieved, the dose necessary for an antithrombotic effect has been calculated to be about 100 mg/kg. In summary, the N-ethoxycarbonyl derivatives of oligoamines appear to be suitable prodrugs for oral administration of oligoamines.
Animals↗
Imaging expression of adenoviral HSV1-tk suicide gene transfer using the nucleoside analogue FIRU.
Substrates for monitoring HSV1-tk gene expression include uracil and acycloguanosine derivatives. The most commonly used uracil derivative to monitor HSV1-tk gene transfer is 1-(2-fluoro-2-deoxy--D-arabinofuranosyl)-5-[*I]iodouracil (fialuridine; I*-FIAU), where the asterisk denotes any of the radioactive iodine isotopes that can be used. We have previously studied other nucleosides with imaging properties as good as or better than FIAU, including 1-(2-fluoro-2-deoxy--D-ribofuranosyl)-5-[*I]iodouracil (FIRU). The first aim of this study was to extend the biodistribution data of 123I-labelled FIRU. Secondly, we assessed the feasibility of detecting differences in HSV1-tk gene expression levels following adenoviral gene transfer in vivo with 123I-FIRU. 9L rat gliosarcoma cells were stably transfected with the HSV1-tk gene (9L-tk+). 123I-FIRU was prepared by radioiodination of 1-(2-fluoro-2-deoxy--D-ribofuranosyl)-5-tributylstannyl uracil (FTMRSU; precursor compound) and purified using an activated Sep-Pak column. Incubation of 9L-tk+ cells and the parental 9L cells with 123I-FIRU resulted in a 100-fold higher accumulation of radioactivity in the 9L-tk+ cells after an optimum incubation time of 4 h. NIH-bg-nu-xid mice were then inoculated subcutaneously with HSV1-tk (-) 9L cells or HSV1-tk (+) 9L-tk+ cells into both flanks. Biodistribution studies and gamma camera imaging were performed at 15 min and 1, 2, 4 and 24 h p.i. At 15 min, the tumour/muscle, tumour/blood and tumour/brain ratios were 5.2, 1.0 and 30.3 respectively. Rapid renal clearance of the tracer from the body resulted in increasing tumour/muscle, tumour/blood and tumour/brain ratios, reaching values of 32.2, 12.5 and 171.6 at 4 h p.i. A maximum specific activity of 22%ID/g tissue was reached in the 9L-tk+ tumours 4 h after 123I-FIRU injection. Two Ad5-based adenoviral vectors containing the HSV1-tk gene were constructed: a replication-incompetent vector with the transgene in the former E1 region, driven by a modified CMV promoter, and a novel replication-competent vector with the HSV1-tk gene in E3 driven by the natural E3 promoter. The human glioma cell lines U87MG and T98G were infected with a multiplicity of infection (m.o.i.) of 10. Forty-eight hours later the cells were incubated with 123I-FIRU and radioactivity was measured in a gamma counter. We found significantly higher levels of radioactivity in both cell lines following infection with the replication-competent vector (P<0.001). NIH-bg-nu-xid mice were then inoculated subcutaneously with U87MG cells. Tumours (approximately 1,000 mm3) were injected with 108 and 109 Infectious Units (I.U.) of either vector. After 48 h, the tracer was injected, followed by gamma camera imaging and direct measurement of radioactivity in the tumours at 4 h p.i. Images and direct measurements indicated increased uptake of tracer with higher I.U. and also demonstrated increased accumulation of tracer in the tumours treated with the replication-competent adenoviral vector (P=0.03). These results demonstrate that 123I-FIRU in combination with HSV1-tk is a valuable tracer for in vivo monitoring of adenoviral gene transfer.
Adenoviridae↗
A micromethod for the determination of an unbound radioactive iodine in radiolabeled glycoproteins by means of uranyl acetate.
A method for determination of an unbound radioactive iodine in radiolabeled glycoproteins is based on coprecipitation of these macromolecules with uranyl and phosphate ions. Under these conditions unbound 125I is not precipitated. The method is simple, rapid, and very sensitive.
Glycoproteins↗
High-performance liquid chromatographic separation of biotinylamide analogues used as substrates in biotinidase radioassays.
A simple, one-step protocol for synthesizing biotinylmono[125I]iodotyramine and biotinyldi[125I]iodotyramine, which are used as tracer substrates in biotinidase radioassays, is presented. This synthetic protocol uses reversed-phase HPLC for the isolation of the biotinylamide analogues from the reaction mixture. The HPLC method developed can potentially be applied to a scaled-up synthetic protocol for non-radioactive biotinylmono- and diiodotyramine. In addition, it can be used for the identification of the above-mentioned compounds.
Amidohydrolases↗
High-speed electron microscope autoradiographic studies of diffusible compounds.
Three important factors are necessary for successful electron microscope autoradiography (EM-ARG): good resolution, proper preparation of the radioactive isotope (RI) labeled diffusible compounds, and shortened exposure time for ARG. The resolution problem is fundamental to EM-ARG. However, unless the diffusible RI compounds have been fixed correctly in the tissues during preparation, good resolution is useless. It is also necessary to shorten the exposure time for ARG. As yet, a high-speed ARG method fol electron microscopy has not been reported, although scintillation ARG methods have been applied to macro- and micro-ARG since 1960. High specific activity, a large amount of radioactivity per unit exposure for radio incorporation (incubation), and careful selection of labeled compounds that concentrate in the DNA or RNA of cell organelles may increase the sensitivity of the emulsion and shorten the exposure time for ARG. For example, labeled thymidine accumulates in nuclear DNA, 3H-SPG (Schizophyllan-produced polyglucan) is incorporated into lysosomal granules, and labeled iodine concentrates in thyroid follicles, often increasing the sensitivity of the emulsion and shortening the exposure time, but high-resolution ARG continues to be necessary, even though it requires 4 weeks or more of exposure time. Scintillation autoradiography using tritium seems unstable. We propose a new way to shorten exposure time for EM-ARG, by combining overdevelopment with coating both sides of the grid with emulsion. This method is approximately 100 times more sensitive than the conventional method, and only 4 days of exposure time are required, in contrast to the 1 month usually needed.
Amino Acids↗
Tumor model studies of 131I-tetracycline and other compounds.
Iodine-131-tetracycline (131I-TET) was prepared by allowing tetracycline hydrochloride to react with radioiodide in acidic methanol (labeling efficiency greater than 85%). This preparation was found to be stable at--4 degrees C for at least 72 hr. Some minimal in vivo breakdown did occur. The 131I-TET, 67Ga, and several 99mTc compounds were studied in a rat hepatoma model. The incorporation of the radiopharmaceuticals into the tumor occurred rapidly, with peak levels at 0.5 and 24 hr after injection for 131I-TET and 67Ga, respectively. The clearnace of the radiopharmaceutical from nonviable tumor was slower than for viable tumor, and by 72 hr after injection the greatest concentration of radioactivity appeared in the nonviable fraction. All normal tissues showed faster clearance than did tumor tissue, regardless of viability. Decreasing the quantity of 131I-TET injected increased the percent of uptake in the nonviable tumor tissue but had no effect on the viable tumor uptake. Of the 99mTc compounds studied, the phosphates developed the highest tumor-to-background ratios. Unfortunately these ratios were not as high as those achieved for 67Ga or 131I-TET.
Animals↗
In vivo and in vitro studies with omega-[rho-123I-phenyl]-pentadecanoic acid in rats.
Biodistribution, plasma clearance and urinary excretion of omega-[p-123I-phenyl]-pentadecanoic acid were investigated in rats. The affinity of this radiopharmaceutical to red blood cells and to the plasma proteins was determined in vitro. Various radioactive metabolites were analysed by paper electrophoresis both in blood and urine at various intervals after administration of the compound. Protein-binding in plasma was determined by both electrophoresis and TCA precipitation. In vitro studies showed 30% uptake by red blood cells at equilibrium (30 min post-injection). 48% of the activity in the red cells could be removed after repeated washing with saline. The maximum uptake by myocardium occurred at 1 min and the maximal heart-to-blood ratios at 3 min. Although in vitro protein-binding was high, in vivo studies showed a very rapid plasma clearance (94% in 3 min) which indicated a weak binding. The amount of free iodine in plasma was less than 1% at any time after injection, thus not presenting a background problem or unnecessary radiation dose to thyroid and whole body. The major radioactive metabolites were 123I-p-hippuric acid and 123I-p-benzoic acid. In urine 123I-p-hippuric acid was excreted almost quantitatively. The metabolism was very fast, even 3 min post-injection the first metabolites could be found in the blood stream. Urinary excretion did not reach a plateau until 48 h. The total amount of radioactivity excreted was 56% within 48 h.
Animals↗
Substituted halogenated arylsulfonamides: a new class of sigma receptor binding tumor imaging agents.
The discovery of a series of novel halogenated arylsulfonamides (HAS) as new sigma receptor binding tumor imaging agents is described. Several substituted halogenated sulfonamides have been prepared and characterized. Target compounds were examined for their affinity for sigma1 and sigma2 receptor subtypes using guinea pig brain membranes and rat liver membranes, respectively. A number of substituted halogenated sulfonamides displayed subnanomolar affinities for sigma1 sites and low nanomolar affinities for sigma2 subtype receptors. A limited structure-activity relationship study of this chemical series is discussed. The radioiodination (I-125) of one congener member (4-[125I]iodo-N-[2-(1'-piperidinyl)ethyl]benzenesulfonamide, 4-[125I]IPBS) was accomplished in high yields. The in vitro competition binding studies of 4-[125I]IPBS in guinea pig brain membranes with sigma receptor binding ligands confirmed its sigma pharmacology. The rank order of potency was BD1008 (N-[2-(3, 4-dichlorophenyl)ethyl]-N-methyl-2-(1-pyrrolidinyl)ethylamine) > 4-IPBS > haloperidol > (+)-pentazocine > DTG (1, 3-di-o-tolylguanidine) > (-)-pentazocine. The inhibition constants (IC50) were 0.70, 1.46, 6.28, 10.4, 87.2, and 152 nM, respectively, and are consistent with labeling of sigma1 receptors. The tumor imaging potential of 4-[125I]IPBS was studied in C57 black mice bearing B16 melanoma xenograft. A high tumor uptake of 4-[125I]IPBS was observed (7.40% ID/g) at 1 h postinjection. The wash out of activity from the tumor was slow at 6 h postinjection (7.22% ID/g). The tumor also had the highest amount of radioactivity (1.54% ID/g) at 24 h postinjection. These results demonstrate that radiohalogenated benzenesulfonamides could be a potentially useful class of compounds in nuclear oncologic scintigraphy.
Animals↗