SEARCH · PubMed Health

Results for “IODINE AND COMPOUNDS RADIOACTIVE”

Explore indexed PubMed citations for clinical trials, systematic reviews and public health research. Read source abstracts and follow each citation to its original PubMed record.

Quote a phrase for an exact phrase match. Source license links do not imply unrestricted reuse.

At least 541 records · Page 30Linked to original sources

PubMed1996

Radiation safety in the central radiopharmacy.

The currently increasing number of new radiopharmaceuticals and the increase in individual patient-dose activity, particularly for single photon emission computer tomography imaging, coupled with the switch toward unit doses probably contribute to an increase in the radiation burden to radiopharmacy personnel. To meet this increased need of the nuclear medicine community, a medium-sized radiopharmacy may order seven to eight 3-Ci molybdenum-99/technetium-99M generators per week and may perform 10 to 15 elutions per day. The maximum radiation exposure to radiopharmacy personnel occurs during the generator elutions, compounding (kit preparation), and unit-dose dispensing. Additional sources of radiation exposure can occur during receipt of radioactive packages, transport of prepared doses, and the process of storage and disposal of radioactive waste. Recent reports have shown extremity radiation doses to the fingers and hands at 14 to 21 rem/year. Radiation exposure can be monitored by film badges, thermoluminescent detectors, or one of the analog or digital self-reading dosimeters. Each monitoring device has advantages and the choice depends upon the personnel involved (eg, visitors) and the particular needs of the radiopharmacy. Extremity dose reductions during radiopharmacy procedures can be achieved by a number of techniques, some as simple as the use of 8- to 9-inch forceps during transfers of radioactive vials and syringes and the use of a dose-drawing syringe shield during unit-dose dispensing procedures. In preparation of unsealed doses or capsules of radioactive iodine, there is a potential for a high internal dose because of inhalation of the volitile solution. Frequent monitoring in the form of bioassays and the use of strict threshold levels will ensure early detection of exposure to radioactive iodine and quick corrective action. In pharmacies and nuclear medicine departments handling fluorine-18 for use with Anger gamma cameras, the high levels of both beta and gamma radiation present an additional set of radiation safety problems.

Equipment Design↗

PubMed1979

Hepatic handling of a gamma-emitting bile salt derivative, 123I-cholylglycylhistamine, in the dog.

The hepatic handling of the bile salt derivative 123I-cholylglycylhistamine has been compared with that of the physiologic bile salt taurocholate in boxer dogs equipped with a Thomas duodenal cannula. After intravenous injection of trace amounts, 123I-cholylglycylhistamine and 14C-taurocholate disappeared from plasma with nearly identical disappearance rate constants. Excellent scintiscans of the liver were obtained with the Anger camera after injection of 3 mCi of 123I-cholylglycylhistamine. Monitoring of radioactivity over a hepatic region of interest revealed rapid uptake of 123I-cholylglycylhistamine by the liver, which reached a maximum 5.7 +/- 0.4 min after injection. The biliary excretion rates of the compounds closely paralleled each other, reaching their maximum within 15 min after injection. Cumulative biliary excretion within 45 min was 58.5 +/- 2.9% and 61.4 +/- 5.0% of the dose for 123I-cholylglycylhistamine and 14C-taurocholate, respectively. Modification of the side chain and gamma-labelling of bile salts may provide scintigraphic agents for the study of the biliary system, which in the behaviour closely resemble the physiologic parent compounds.

Animals↗

PubMed2006

In SCID mice with transplanted joint tissues from rheumatism patients, a model mice of human rheumatoid arthritis, anti-human fas antibody (R-125224) distributes specifically to human synovium.

PURPOSE: We investigated the tissue distribution of a humanized anti-human Fas monoclonal antibody, R-125224, in SCID mice transplanted with synovial tissues from patients with rheumatoid arthritis (SCID-HuRAg mice). The binding kinetics of R-125224 was also determined, using isolated human synovial cells. MATERIALS AND METHODS: Tissue distribution was assessed at 1, 24 and 168 h after intravenous administration of (125)I-R-125224 to SCID-HuRAg mice (0.4 mg/kg). The in vitro binding of (125)I-R-125224 to isolated human synovial cells was investigated. RESULTS: After intravenous administration of (125)I-R-125224 to SCID-HuRAg mice, the radioactivity distributed to various tissues at 1 h. Thereafter, the radioactivity in the tissues gradually decreased except for the transplanted synovial tissues, in which the radioactivity increased in a time-dependent manner, and at 168 h, the tissue/plasma concentration ratio was about 1. The in vitro binding affinity of (125)I-R-125224 to human synovial cells was high with a dissociation constant of 1.32 +/- 0.62 nM and the binding was inhibited by non-labeled R-125224 in a concentration-dependent manner. CONCLUSION: R-125224, a candidate compound for treating rheumatoid arthritis, specifically distributed to the pharmacological target site, human synovium transplanted in SCID mice, with high affinity.

Animals↗

PubMed2006

Crosslinked chitosan implants as potential degradable devices for brachytherapy: in vitro and in vivo analysis.

Compared with conventional external beam radiation, brachytherapy offers a superior therapeutic regimen. However, some major constraints are associated with its implementation, including the need of complicated procedures for device placement and removal. The purpose of this study was to examine whether crosslinked chitosan (Ct) implants could serve as potential biodegradable devices for brachytherapy. Ct was reacted with increasing amounts of glutaraldehyde to obtain hydrogels with different crosslinking densities, which were characterized chemically, thermally and mechanically. The effect of the dialysis medium conditions (ionic strength, osmolarity and pH) on the gel hydration and in vivo degradation was assessed. Two types of implants, slow and fast degrading gel (SDG and FDG, respectively), were prepared and implanted with or without Sudan Black (SB) in the rat. While SDG withstood for over a month, the FDG degraded within two weeks after implantation. The release kinetics of SB from the hydrogels verified their in vivo degradation properties. The incorporation of the radioactive compound (131)I-norcholesterol ((131)I-NC) into the SDG altered the degradation kinetics of the gel as reflected by the release kinetics of the radioactive marker. Eighty percent of (131)I-NC was released within a month after implantation, after which time, radioactivity was detected in the regional lymph nodes. Histological examination of the tissues surrounding the implants demonstrated negligible tissue response to the implants, when compared to biodegradable surgical sutures. It is concluded that hydrogels made of crosslinked Ct are potential novel, safe, degradable devices for brachytherapy.

19-Iodocholesterol↗

PubMedDate not supplied

Antibody labeling with copper-67 using the bifunctional macrocycle 4-[(1,4,8,11-tetraazacyclotetradec-1-yl)methyl]benzoic acid.

The high kinetic stability of the Cu2+ complex of the chelator 4-[(1,4,8,11-tetraazacyclotetradec-1-yl)-methyl]benzoic acid was demonstrated at physiological pH as well as under acidic conditions. The chelating agent was conjugated to AB35, a monoclonal antibody directed against CEA, without a significant loss of immunoreactivity. The conjugate could, under optimal labeling conditions, be labeled with 67Cu in acetate buffer with a full occupancy of ligands within 20 min. This radiolabeled conjugate showed no transfer of radiocopper to serum proteins in human serum over 7 days. The biodistribution in tumor-bearing mice was measured and compared to that of iodinated AB35. Tumor uptake was high with 15 +/- 3% ID (injected dose)/g after 24 h and 32 +/- 7% ID/g after 96 h for the 67Cu-labeled antibody and 13 +/- 4% ID/g after 24 h and 14 +/- 2% ID/g after 96 h for the 125I-labeled antibody. Whereas radioactivity in normal organs decreased with time after 24 h, increased residence time was shown up to 4 days with the 67Cu-labeled AB35.

Animals↗

PubMed1995

A radioactive assay for the degradation of neuropeptide Y.

Neuropeptide Y (NPY) is one of the most abundant neuropeptides in the mammalian central nervous system. Like other neuropeptides, NPY is inactivated by specialized neuropeptidases. To trace the degradation of NPY, an assay was established using biotinylated NPY. Biotinyl-NPY was radiolabeled with Na125l by the chloramine-T method and bound to a streptavidin-agarose matrix. The amount of radiolabeling was analyzed by reverse-phase HPLC. The assay was carried out with five peptidases and inhibitors to demonstrate different specific activity. Measurable amounts of radioactivity were released by treatment with endopeptidase-24.18, plasmin, and trypsin, whereas dipeptidylpeptidase IV (DPPIV) and angiotensin-converting enzyme (ACE) showed no activity in this assay. In the case of DPPIV this is due to a resistance of the assay to aminopeptidase attack. The assay is useful to study the specific degradation of NPY particularly by endopeptidases in all kinds of biological samples.

Amino Acid Sequence↗

PubMed1990

Synthesis of affinity ligands and radioactive probes for isolation and study of myo-inositol 1,4,5-trisphosphate binding proteins.

To synthesize an affinity matrix for isolation of D-myo-inositol 1,4,5-trisphosphate binding proteins, racemic 3-cyclohexene-1-carboxaldehyde was oxidized and converted to a mixture of trans-3,4-di-hydroxycyclohexane-1-carboxylic acid methyl ester isomers, which was phosphorylated and separated into (+-)-(1R,3R,4R)- and (+-)-(1R,3S,4S)-trans-3,4-bis[(diphenoxyphosphoryl)oxy]cyclohex an e-1- carboxylic acid methyl esters. Each of these racemic compounds was hydrogenolyzed and reacted with ethylenediamine to give a monoamide, N-(2-aminoethyl)-bis(phosphonyloxy)cyclohexane-1-carboxamide, that was coupled to cyanogen bromide activated Sepharose 4B to provide the desired affinity matrices. The intermediate trans-3,4-bis[(diphenoxyphosphoryl)oxy]cyclohexane-1-carboxylic acid methyl ester was also reduced with lithium borotritide to give the (hydroxy[3H]methyl)cyclohexane derivative, which was phosphorylated and hydrogenolyzed to yield trans-3,4-bis(phosphonyloxy)-1-[(phosphonyloxy)[3H]methyl]cy clohexane, a radiolabeled analogue of inositol 1,4,5-trisphosphate. The carboxamide was also coupled to 4-azidosalicylic acid, and the product was iodinated to provide a 125I-radiolabeled photoactivatable cross-linking derivative of cyclohexanediol bisphosphate.

Calcium Channels↗

PubMedDate not supplied

Radionuclide imaging of tumor xenografts in mice using a gelatinase-targeting peptide.

Tumors express MMP-2 and MMP-9 gelatinases, which are involved in the formation of tumor vasculature. This suggests that a tumor and its surrounding neovasculature can be visualized by a sensitive gelatinase recognition method. We have studied tumor radioimaging using a gelatinase inhibitory peptide CTTHWGFTLC (CTT), which in a mouse model targets the tumor site following an intravenous injection. We determined a solution NMR structure of CTT and its retro-inversion peptide, and prepared 125I and 99mTc-labelled CTT peptide derivatives. Radiolabelled CTT inhibited gelatinases in vitro, and homed to a tumor xenograft in mice. In normal mice, CTT was instead rapidly cleared from the circulation mainly through the kidney and, after 24 h, no significant radioactivity was accumulated in healthy tissues. Gamma camera imaging of a primary tumor in live mice was obtained with double-labelled liposomes, which were coated with 99mTc-CTT and encapsulated with 125I albumin. CTT also targeted liposomes to the lungs of tumor-bearing mice, which may indicate the existence of non-visible lung micrometastases. Our studies suggest that selective gelatinase-targeting compounds could be useful in the early detection and imaging of primary tumors and metastases.

Animals↗

PubMed1991

Analyses of microvascular permeability in response to mediators of immediate hypersensitivity.

Mediator-induced changes in microvascular permeability were studied in rodent skin. To monitor these changes, Evan's blue dye, iodinated rat albumin and IgG, and tritiated neutral dextran molecules having different molecular radii were used. After intradermal injections of serotonin, histamine, and bradykinin, the degree of radiolabeled tracer efflux was determined by measuring the extent of blueing and the level of radioactivity in skin biopsy specimens. Although the mediators varied in potency on a molar basis (serotonin greater than bradykinin greater than histamine), the efflux resulting from each was similar. Furthermore, kinetic studies revealed that each of these vasoactive agents caused a marked but transient increase in macromolecular permeability that lasted less than 30 minutes. To determine the pore size created and the effect of charge on the transudation of macromolecules into the interstitium, fractions of neutral [3H]dextrans with a known molecular size (average radii, 12 and 4.4 nm, respectively) were infused either singly or in combination with 125I-labeled rat albumin and/or IgG before intradermal injection of serotonin, histamine, bradykinin, or compound 48/80. Regardless of the mediator used, no differences could be demonstrated in macromolecular efflux, as indicated by either the molecular size of the charge of the tracer used. Thus, all mediators of immediate hypersensitivity reactions that were studied produce venular gaps greater than 12 nm in addition to displaying similar vasopermeable characteristics.

Animals↗

PubMed1994

Biodistribution and preclinical radioimmunotherapy studies using radiolanthanide-labeled immunoconjugates.

Lutetium-177 (177Lu), samarium-153 (153Sm), and yttrium-90 (90Y) are members of the family of elements known as lanthanides or rare earths. Monoclonal antibody CC49, a murine immunoglobulin (Ig) G1, which is reactive with the tumor-associated antigen TAG-72, previously has been shown to react with a wide range of human carcinomas. The authors review here the comparative biodistributions of CC49 IgG and F(ab')2 fragments labeled with 177Lu, 153Sm, and 90Y using the bifunctional chelating agent PA-DOTA. The authors also review the results of a biodistribution study comparing iodine-125-labeled and 177Lu-labeled CC49 sFv, and the use of 177Lu-CC+9 IgG in an experimental therapy model. Chelation and conjugations gave similar yields, and the labeled proteins showed similar retention of immunoreactivity regardless of the isotope used for both IgG and F(ab')2. Biodistribution data obtained in athymic mice bearing LS-174T human colon carcinoma xenografts likewise showed no differences among the three radioisotopes for both IgG and F(ab')2. Femur uptake of radioactivity was lower than previously reported for other radiolanthanide immunoconjugates. Different metabolic patterns were observed for radioiodinated versus radiometal-labeled sFv, particularly in the kidney, where localization of the latter was increased dramatically. 177Lu-CC49 was found to delay the growth of established LS-174T human colon carcinomas in athymic mice at a single dose of 50 microCi. Elimination of established tumors was demonstrated over the observation period (77 days) using single administrations of 200 or 350 microCi. Dose fractionation experiments revealed that the mice tolerated 750 microCi (3 x 250 microCi, given weekly), whereas > 50% of the mice died after receiving a single administration of approximately 500 microCi. In isotype-matched control experiments, a large differential in the therapeutic effects was observed between 177Lu-labeled control antibody and CC49.

Aniline Compounds↗

PubMed1981

Experiences using chloramine-T and 1, 3, 4, 6-tetrachloro-3 alpha, 6 alpha-diphenylglycoluril (Iodogen) for radioiodination of materials for radioimmunoassay.

A comparison of labelling compounds with chloramine-T and with 1, 3, 4, 6-tetrachloro-3 alpha, 6 alpha-diphenylglycoluril (Iodogen) has been carried out. For human transferrin, human calcitonin, 1-84 bovine parathyrin, fibrinopeptide-A, human thyrotropin and F-CB3, a cyanogen bromide cleavage peptide of human fibrinogen, the quality of tracer produced by the Iodogen method was better. For rat lutropin, human growth hormone and human prolactin, labelling with Iodogen produced a tracer of unsatisfactory quality. For a further 13 peptides, the results from both methods were comparable. Optimal reaction times using Iodogen were of the magnitude of two to three times longer than when using chloramine-T. Reduction of the volume of radioactive waste by up to 90% could be achieved when the Iodogen method was coupled with a short cation-exchange column to separate unreacted iodide from the labelled compound. Data is presented on the quality of tracer, expressed in terms of elution profiles and radioimmunoassay standard curves. A novel "combi-method" of labelling proteins without tyrosine or histidine moieties is presented where N-succinimidyl-3-(4-hydroxyphenyl)-propionate is labelled at pH 7.5 using Iodogen to give "Bolton-Hunter" reagent, which is then transferred to a vessel containing the peptide to be labelled at ph 8.6.

Animals↗

PubMed1990

Comparison of specific radioactivities of human alpha-lactalbumin iodinated by three different methods.

Radioiodination provides an extremely sensitive method for the detection of low levels of proteins. In the development of a sensitive radioimmunoassay for human alpha-lactalbumin (alpha-LA), the protein was labeled to high specific activity (approaching 2000 Ci/mmol) with lactoperoxidase, chloramine-T, and Iodogen. Despite high specific activities of the labeled protein by each method, there was a considerable difference in their binding affinity with monoclonal anti-human alpha-LA antibodies due to varying degrees of protein damage. Iodination of human alpha-LA with Iodogen resulted in labels of the highest specific activity and immunoreactivity with the monoclonal antibodies used.

Antibodies, Monoclonal↗

PubMed2006

Labeling of acetaminophen with I-131 and biodistribution in rats.

The aim of the present study was to label acetaminophen (APAP) with I-131 and to determine its radiopharmaceutical potential in rats. Acetaminophen was labeled with I-131 using the iodogen method. The radiochemical purity of (131)I-APAP was determined by RTLC and paper electrophoresis. The labeling yield was 94 +/- 4%. The biodistribution studies of the labeled compound (specific activity; 56.60 GBq/mmol) were performed in male Albino Wistar rats. The uptake of (131)I-APAP in some organs were determined at different time after injection to the rats. The radioactivity in each organ was counted and the percentage of injected activity per gram of tissue weight (%ID/g) for each organ and blood was calculated. (131)I-APAP uptake in the lung, liver, kidneys, pancreas, blood, stomach and some brain region, were observed. Thus, (131)I-APAP may be radiopharmaceutical for the imaging of the brain.

Acetaminophen↗

PubMed1988

Cytotoxic effects of m-[131I]- and m-[125I]iodobenzylguanidine on the human neuroblastoma cell lines SK-N-SH and SK-N-LO.

As we have reported recently, the human neuroblastoma cell line SK-N-SH is able to take up and store m-iodobenzylguanidine (mIBG). This is in contrast to several other neuroblastoma cell lines, among which are SK-N-LO cells. Both cell lines were used in cell killing experiments with unlabeled and radioactive-labeled mIBG. Using 1-200 microCi m-[131I]IBG (1 h incubation time), only SK-N-SH cells could to a large extent be destroyed in a dose-dependent manner. This effect is completely caused by the radioactive labeling of the molecule, because unlabeled mIBG proved not to be toxic in the concentration range used in experiments with radiolabeled mIBG (30 nM-3 microM). The killing effect was strongly reduced when m-[131I]IBG with low specific activity (0.2-0.3 mCi/mg) was used instead of 20-30 mCi/mg. Similar effects in both cell lines were obtained using m-[131I]-and m-[125I]IBG. SK-N-SH cells that survived a first treatment with m-[131I]IBG were less sensitive to a second treatment. SK-N-LO cells were more sensitive against m-[131I]- and m-[125I]IBG than SK-N-SH cells if both cell lines are exposed to these radioactive compounds over a long period of time (24 h). The reason that only SK-N-SH cells could be destroyed in short-term incubation experiments is that mIBG is stored for approximately 7 days in these cells only. SK-N-LO cells could only be destroyed to a significant degree if m-[131I]IBG was permanently present in the test system. Bone marrow stem cells (CFU-c) also proved to be sensitive against m-[131I]IBG, although the effects were less pronounced than on SK-N-SH cells.

3-Iodobenzylguanidine↗

PubMed2000

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↗

PubMed1994

Studies on the iodination of a ras protein and the detection of ras polymers.

Several methods for the iodination of recombinant v-H-ras protein were compared. The Iodobead method gave greatest incorporation of radioactivity with minimal modification of the ras protein. Upon treatment of the ras protein with [125I] Nal and an Iodobead, radioactivity was initially incorporated into a 22 kDa species with a pl of 5.2, then predominantly into a 23 kDa species with a pl of 5.4. The specific activity of [125I]ras was 6 x 10(6) cpm/pmol total ras protein. Iondination did not alter the biological activity of the ras protein as judged by its ability to bind GTP gamma S and induce maturation of Xenopus laevis oocytes. It is concluded that while iodination alters the apparent molecular weight and pI of ras, presumably by the oxidation of one or more classes of amino acids, this does not affect the biological function of the protein. The ras protein, radioactively-labelled with iodine using the Iodobead method, should be suitable for studies of protein-protein interactions involving ras. Treatment of iodinated ras with the chemical cross-linking agent disuccinimidyl suberate revealed the presence of several minor high molecular weight protein species. This result shows that, in a dilute solution of purified ras protein, the monomeric form is in equilibrium with small amounts of polymeric forms.

Animals↗

PubMed1998

The synthesis, radioiodination and preliminary biological study of the new carboxylic derivatives of dithizone.

Synthesis, characteristics and radioiodination of the new carboxylic derivatives of dithizone are described in this paper. We have applied the carboxy dithizones for preparation of radioactive compounds by coupling with [131I]-histamine. Preliminary biological studies of the new radiodithizone were done in rats after two different application routs: peripheral i.v. injection and direct injection to splenic artery. Biodistribution of the carboxy dithizone-[131I]-histamine conjugate (i.v. injection) was quite different than that for free [131I]-histamine. However, uptake of activity in pancreas was low (0.81% g-1 of tissue). Direct application of the conjugate to splenic artery resulted in high activity retention in pancreas after 30 and 45 min post injection (respectively 8.8 and 12.4% g-1 of tissue) indicating potential usefulness of the new radiodithizone for in vivo monitoring of pancreas.

Animals↗

PubMedDate not supplied

Clinical value of deconvolution analysis in radionuclide renal study.

Deconvolution analysis was applied to radionuclide renal study. The purpose of this study was to clarify the underlying renal physiology that determines the shape and values of the transfer function. Analysis of the renal models revealed that the initial height of the transfer function is the ratio of the radioactivity extracted by the kidney to that in the input function. In addition, the shape of the transfer function displayed the distribution of the transit times and enabled us to evaluate the percentage of nephrons having a particular transit time. Based on the relation between the input and output function, a new method for measuring GFR or ERPF was developed in which the input function was corrected by the plasma radioactivity at 5 min after injection of the tracer. As one of the advantages of the transfer function, it was proved clinically that the contribution of the blood background is automatically eliminated from the amplitude of the transfer function. From these findings, our method for the measurement of GFR was considered superior to that proposed by Gates and highly useful for routine radionuclide renal study.

Glomerular Filtration Rate↗