The interactions of99mTc phosphorus radiopharmaceuticals and human serum proteins (original) (raw)
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The stability of99mTc phosphorus compounds in plasma both in vivo and in vitro
Journal of Radioanalytical Chemistry, 1980
The in vivo and in vitro stability of 99 mTc hydroxyethlylidene diphosphonate, 99mTc methylenediphosphonate and 99 mTc pyrophosphate in plasma has been studied using paper chromatographic technique as the analytical tool. The results indicate that the amounts of 99 rote activity found both at the origin and Rf range of ~ 9 mTcO-* for in vivo experiments are slightly greater than those for either in vitro or control experiments. However, this amount of 99 mTc activity represents about 0.16-0.4% of the injected dose. Therefore, it is suggested that 99mTc phosphorus radiopharmaoeuticals are stable in vivo and neither oxidation nor hydrolysis of these bone imaging agents occurs in the blood.
Radiopharmaceuticals for renal studies: Evaluation of protein binding
Journal of Radioanalytical and Nuclear Chemistry, 1989
Determination of total in vitro protein binding was evaluated for the following radiopharmaceuticals:99mTc-diethylenetriaminepentaacetic acid (DTPA),99mTc-dimercaptosuccinic acid (DMSA),99mTc-glucoheptonate (GH) and99mTc-fosfomycin (PHO). For that they were incubated wtih human serum at 37°C. After three and sixty minutes of incubation, the bound fraction was evaluated by two different methods: gel filtration and precipitation with trichloroacetic acid (TCA). The percentage of the99mTc-kidney agents bound
Nuclear Medicine and Biology, 1997
Technetium-99m-labeled alendronate is a new radiopharmaceutical for bone scanning developed under strict quality control at the INNSZ. The purpose of this work was to compare the radiopharmacokinetic data and the dosimetry of 99mTc-ABP and 99mTc-MDP in 10 volunteers, after it was tested in laboratory animals. 99"Tc-ABP has shorter mean residence time (MRT) and t'lz p; is less protein bound; has a higher renal clearance; smaller Vdss, and similar bone uptake at 1 and 2 h. 99"Tc-ABP gives less radiation exposure to the patient with a 740 MBq dose, and the quality of the bone scan is excellent. 99"Tc-ABP is a better radiopharmaceutical than 99"Tc-MDP for bone scanning. Copyighr 0 19%' Elsevier Science Inc. NUCL MEL) BIOL 24;1:27-33, 1997.
Interaction of 99mTc-radiopharmaceuticals with transport proteins in human blood
Nuclear Medicine and Biology, 1993
Interaction of a series of 99"Tc-radiopharmaceuticals with human blood proteins was investigated from two aspects: total protein binding, and specificity of binding to certain classes of proteins. After in vitro labelling of human sera with %Tcradiopharmaceuticals, total protein binding was determined for thirteen 99"Tc-compounds
The Yale Journal of Biology and Medicine, 1996
Secure determination of the binding of 99mTc-radiopharmaceuticals to plasma (P) and blood cell (BC) constituents can help to understand the biodistribution of radiophamaceuticals. The reported precipitation studies of blood with radiopharmaceuticals have shown that the results can not be easily compared between studies. We decided to determine the "gold standard" concentration of trichloroacetic acid (TCA) to evaluate the binding to blood elements for several radiopharmaceuticals used in routine nuclear medicine. We have studied phytic (99mTc-PHY), diethylenetriaminepentaacetic (99mTc-DTPA), glucoheptonic (99mTc-GHA) and dimercaptosuccinic (99mTc-DMSA) acids. Blood was incubated with radiopharmaceuticals, centrifuged and P and BC separated. Samples of P and BC were also precipitated with TCA concentrations (20.0, 10.0, 5.0, 1.0, 0.5 and 0.1 percent) and soluble (SF) and insoluble fractions (IF) were isolated. The percent radioactivity (percent rad) in IF-P depends on TCA c...
Radiochimica Acta, 2011
99mTc-phosphonate structures are well established tracers for bone tumour imaging. Our objective was to investigate different 68Ga-labelled phosphonate ligands concerning labelling kinetics, binding to hydroxyapatite and bone imaging using μ-PET. Seven macrocyclic phosphorus-containing ligands and EDTMP were labelled in nanomolar scale with n.c.a. 68Ga in Na-HEPES buffer at pH∼4. Except for DOTP, all ligands were labelled with >92% yield. Binding of the 68Ga-ligand complexes on hydroxyapatite was analysed to evaluate the effect of the number of the phosphorus acid groups on adsorption parameters. Adsorption of 68Ga-EDTMP and 68Ga-DOTP was >83%. For the 68Ga-NOTA-phosphonates an increasing binding with increasing number of phosphonate groups was observed but was still lower than 68Ga-DOTP and 68Ga-EDTMP. μ-PET studies in vivo were performed with 68Ga-EDTMP and 68Ga-DOTP with Wistar rats. While 68Ga-EDTMP-PET showed uptake on bone structures, an excess amount of the ligand (>...
Bone, 2005
Introduction: Although the first polyphosphonates (PP) were introduced to nuclear medicine as bone imagers in the early 70s, mechanisms involved in uptake still remain speculative. Controversies range from adsorption onto the mineral phase with disputed binding to the organic phase, over incorporation into the mineralisation process to a combination of both mechanisms. Other factors such as solubility of the complex, concentration of ligand or effects of the radionuclide have also been discussed as possible parameters influencing bone uptake. Therefore, the present work aimed to verify the recently presented pre vivo model which was developed to rate the influence of various factors on the binding of differently radiolabelled PP and [ 18 F]-fluoride on synthetic bone matrix. Methods: Radiolabelled polyphosphonates and [ 18 F]-fluoride were added to a vial containing lyophilised and milled spongiosa (Sp) or cortical bone (Co) in Hank's Balanced Salt Solution. After incubation, the radioactivity was measured in the gamma-counter before and after filtration. The percentage of irreversibly bound radioactivity was calculated. Same experiments were performed after decalcification of Sp and Co with hydrochloric acid. Results: Descriptively, [ 111 In] increases the uptake of EDTMP in each case compared to similarly prepared [
Journal of Saudi Chemical Society, 2010
Protein binding affects tissue distribution, plasma clearance and uptake of renal radiopharmaceuticals. The 99m Tc bound to plasma protein after incubation 99m Tc-Gluco-ene-diolate (99m Tc-Sn-Gluco) agent or 99m Tc-prylidinomethyl-tetracycline (99m Tc-Sn-PMT) agent with plasma protein. It was observed that the protein bound to 99m Tc is lesser extent with (99m Tc-Sn-Gluco) agent than with the 99m Tc-PMT agent. 99m Tc-Sn-PMT is excreted more rapidly than 99m Tc-Sn-Gluco. On the other hand the percentage binding to protein seems to depend on the origin of the protein and or the type of protein (human or animal). However lower human protein binding or higher protein binding were observed with 99m Tc-Sn-Gluco or with 99m Tc-Sn-PMT, respectively compared with the binding to rat protein. The unbroken down of the chemical form of the origin of these two agents and the highest of 99m Tc-Sn-Gluco remained as origin in urine indicate that 99m Tc-Sn-Gluco are more stable than 99m Tc-Sn-PMT. Concerning the type of protein binding to 99m Tc-Sn-PMT or to 99m Tc-Sn-Gluco, it was observed that Human Plasma Protein is greater binding than Human serum protein or than IgG.