共查询到20条相似文献,搜索用时 15 毫秒
1.
Fan Caiyun Jia Hongmei Deuther-Conrad Winnie Brust Peter Steinbach J?rg Liu Boli 《中国科学B辑(英文版)》2006,49(2):169-176
A novel 99mTc labeled complex, [N-[2-((2-oxo-2-(4-(3-phenylpropyl)piperazin-1-yl)ethyl) (2-mercaptoethyl)amino)acetyl]-2-aminoethanethiolato]Technetium(V)
oxide (PPPE-MAMA’-99mTcO) ([
99m
Tc]-2) has been designed and prepared based on the integrated approach. The corresponding rhenium complex (PPPE-MAMA’-ReO)(Re-2) has been prepared and characterized. In vitro competition binding assays show moderate affinity of Re-2 towards σ1 and σ2 receptors with K
i values of 8.67 ± 0.07 and 5.71 ± 1.88 μmol, respectively. Planar images obtained at 0.5 h, 4 h, 20 h after i.v. injection
indicate the accumulation of [
99m
Tc]-2 in MCF-7 human breast tumor bearing mice at 20 h. Furthermore, the accumulation of [
99m
Tc]-2 has been inhibited at 20 h after co-injection of [
99m
Tc]-2 plus haloperidol (1 mg/kg). Biodistribution studies of [
99m
Tc]-2 display an in vivo tumor uptake of 0.14% ± 0.01% ID/g at 24 h post i.v. injection with a tumor/muscle ratio of 6.02 ± 0.87. The above results
suggest that [
99m
Tc]-2, derived from a previously published lead compound, retains certain tumor uptake and affinity for σ receptors. [
99m
Tc]-2 may be used as a basis for further structural modifications to develop tumor imaging agents with high affinity for σ receptors. 相似文献
2.
C. Acar S. Teksoz P. ünak F. Z. Biber Müftüler E. I. Medine 《Journal of Radioanalytical and Nuclear Chemistry》2009,280(2):375-380
The aim of this study is to investigate stereoisomeric behavior of penicillamine and the effect of temperature on labeling.
In addition, it was explored how stereoisomerism affected biological behavior of them. In the present work, D- and L-enantiomers
of penicillamine(D-PA, L-PA) were labeled with 99mTc using SnCl2 as reducing agent and their radiopharmaceutical potentials were investigated. Quality control procedures were carried out
using thin layer radiochromatography (TLRC), electrophoresis and high performance liquid radiochromatography (HPLRC). HPRLC
chromatograms showed two peaks for 99mTc-D-PA, while a single peak was observed for 99mTc-L-PA at room temperature. However, the single peak was observed at 90 °C for both isomers. Labeling yields of each isomer
were found to be over 98%. Biological activity of these complexes was determined on male Albino Wistar rats by biodistribution
studies. While the biodistribution result of 99mTc-D-PA showed high uptake in the liver, maximum uptake of 99mTc-L-PA was observed in the kidneys. Both two complexes were cleared rapidly from the blood, mainly by the renal system. Since
the activity concentration of 99mTc-D-PA at the 30th minute in the kidneys and the liver reached a maximum value and at the 120th minute, it was removed by
renal and hepatobiliary excretion. As a result, it can be concluded that stereoisomerism affect not only the chemical behavior,
but also differs their biological behavior of these compounds. 相似文献
3.
叶酸受体在许多源于上皮组织的恶性肿瘤中高度表达,是目前肿瘤放射性显像研究的一个新的靶点。由于叶酸对于叶酸受体具有很高的亲和性,作为重要的特异性靶向介导分子,99mTc标记叶酸肿瘤显像剂已成为当前放射性药物的研究热点之一。本文对不同类型的99mTc标记的叶酸类放射性肿瘤显像剂的研究进展、应用情况和存在的问题进行了评述,探讨了99mTc标记叶酸显像剂的一般设计方法,并对其未来发展方向进行了展望。 相似文献
4.
Drishty Satpati Archana Mukherjee Meera Venkatesh Sharmila Banerjee 《Journal of Radioanalytical and Nuclear Chemistry》2011,290(1):89-93
The over-expression of folate receptors in variety of neoplastic tissues makes radiolabeled folate conjugates potential agents
for imaging and therapy of such cancers. With the aim of preparing an imaging agent for targeting folate receptors, folic
acid has been conjugated with homocysteine for complexation with [99mTc(CO)3(H2O)3]+ core. The radiolabeled complex of the homocysteine-folate could be obtained in >95% radiochemical yield as observed by HPLC.
Stability of complex in saline was studied and challenge studies with histidine and cysteine revealed kinetic stability of
the complex. Lipophilicity of the radiolabeled complex (log P) was found to be 0.45. In vitro uptake of 99mTc(CO)3-labeled folic acid derivative was studied in KB cells and inhibition studies were carried out using 3H-folic acid and cold homocysteine–folate conjugate. The in vitro studies indicated loss of binding affinity of the derivative
towards folate receptors. 相似文献
5.
JunBo Zhang XueBin Wang ChunJun Tian 《Journal of Radioanalytical and Nuclear Chemistry》2007,273(1):15-17
The bis(N-butyl dithiocarbamato) nitrido 99mTc complex [99mTcN(BDTC)2] (BDTC: N-butyl dithiocarbamato) has been synthesized through a ligand-exchange reaction. The two-step procedure consisted
of an initial reaction of 99mTcO4
− with succinic dihydrazide (SDH) in the presence of stannous chloride as reducing agent and propylenediamine tetraacetic acid
(PDTA) as complexing agent, and subsequent addition of sodium salt of N-butyl dithiocarbamate. The radiochemical purity of
the complex was over 90%, as measured by thin layer chromatography. No decomposition of the complex at room temperature was
observed over a period of 6 hours. Its partition coefficient indicated that it was a lipophilic complex. The electrophoresis
results showed the complex was neutral. Biodistribution in mice showed that the complex accumulated in the brain with high
uptake. The brain/blood ratio was 1.58, 1.67 and 1.20 at 5, 30 and 60-minute post-injection, respectively, suggesting this
compound would be a potential cerebral imaging agent. 相似文献
6.
Adsorption behavior of molybdate on acidic alumina was studied at boiling water bath temperature (~100 °C). Various parameters
affecting the adsorption of molybdenum, such as pH, amount of molybdenum, incubation period, etc., were determined. A 99mTc generator was prepared by adsorbing low specific activity 99Mo (150 mg) on 1 g alumina. Elutions were carried out with saline. Performance of the generator such as 99Mo breakthrough, aluminum contents, pH, elution profile, radiochemical purity, and labeling efficiency of kits were checked. 相似文献
7.
<正>The chemokine CXCR4 receptor is over-expressed in a wide variety of tumors.In this study,AMD3100,which was a prototype non-peptide antagonist of CXCR4 receptor,was labeled with ~(99m)Tc.~(99m)Tc-AMD3100 was verified by thin layer radio chromatography(TLRC).The tumor-localizing properties of ~(99m)Tc-AMD3100 were evaluated and proved in mice bearing Hep-G2 tumor xenograft.~(99m)Tc-AMD3100 was a promising,novel receptor-specific radiopharmaceutical with potential application in the imaging of human tumors. 相似文献
8.
9.
N. Sadeghzadeh M. Ahmadzadeh M. Erfani 《Journal of Radioanalytical and Nuclear Chemistry》2013,298(1):287-293
Gastrin-releasing peptide (GRP) receptors are over-expressed in various human tumor including breast and prostate which can be targeted with bombesin for diagnosis and targeted therapy. High abdominal accumulation and the poor in vivo stability of radiolabeled bombesin analogues may represent a limitation for diagnostic imaging and targeted therapy. In this study a new bombesin derivative was labeled with 99mTc via HYNIC and tricine as a coligand and investigated further. The peptide HYNIC conjugate was synthesized on a solid phase using Fmoc strategy. Labeling with 99mTc was performed at 100 °C for 10 min and radiochemical analysis involved ITLC and HPLC methods. The stability of radiopeptide was checked in the presence of human serum at 37 °C up to 24 h. Internalization was studied with the human GRP receptor cell line PC-3. The Biodistribution was studied in mice. Labeling yield of >98 % was obtained to correspond a specific activity of ~80.9 GBq/μmol. Radioconjugate internalization into PC-3 cells was high and specific (15.6 ± 1.9 % at 4 h). A high and specific uptake in GRP-receptor-positive organs such as mouse tumor and pancreas (2.11 ± 0.18 and 1.78 ± 0.09 % ID/g after 1 h respectively) was also determined. 相似文献
10.
Synthesis, biodistribution and evaluation of 99mTc-sitafloxacin kit: a novel infection imaging agent
S. S. Qaiser A. U. Khan M. R. Khan 《Journal of Radioanalytical and Nuclear Chemistry》2010,284(1):189-193
Radiosynthesis of 99mTc-sitafloxacin (99mTc-STF) complex and its efficacy as a potential infection imaging agent was evaluated. Effect of sitafloxacin (STF) concentration,
sodium pertechnetate (Na99mTcO4), stannous chloride dihydrate (SnCl2·2H2O), and pH on the % radiochemical purity yield (RCP) of 99mTc-STF complex was studied. A stable 99mTc-STF complex up to 120 min with maximum %RCP yield was observed by mixing 2 mg of STF with 3 mCi of Na99mTcO4 and 150 μL of SnCl2·2H2O (1 μg/μL in 0.01 N HCl) at a pH 5.5. Artificially infected rats with Staphylococcus aureus were used for studying the biodistribution behavior of the 99mTc-STF complex. After 30 min of the intravenous (I.V.) administration of the 99mTc-STF complex, 7.50 ± 0.10% was absorbed in the infected thigh of the rats and the uptake gradually increased to 18.50 ± 0.20%
within 90 min. Rabbits with artificially induced infection were used for evaluating the scintigraphic accuracy. Higher uptake
in the infected thigh was observed after 2 h of I.V. administration of the 99mTc-STF complex. Target to non-target organ ratio of the % absorbed dose incase of infected/normal muscle was 6.82 ± 0.40,
17.11 ± 0.60, and 23.13 ± 1.00% at 30, 60 and 90 min of administration. Stable and higher %RCP, higher uptake in the infected
thigh, and spectral studies, recommend the 99mTc-STF for routine infection imaging. 相似文献
11.
Shuye Yang Xuebin Wang Haixun Guo Jian Liu Fenglong Wang Xianzhong Zhang 《Journal of Radioanalytical and Nuclear Chemistry》2008,278(1):165-171
Mixed ligand fac-tricarbonyl complex of [99mTc(CO)3-DMSA-MIBI] has been prepared starting from the precursor [99mTc(OH2)3(CO)3]+. The complex can be obtained in good yield and purity in a two-step procedure by first attaching meso-2,3-dimercaptosuccinic acid (DMSA, HOOCCH(SH)CH(SH)COOH) with [99mTc(OH2)3(CO)3]+, followed by addition of MIBI [tetrakis-2-methoxyisobutylisonitrile (CH3OC(CH3)2CH2-N≡C) copper(I) tetrafluoroborate] solution. The complex was characterized by TLC and HPLC and was studied by means of octanol-water
partition coefficient, electrophoresis, stability in vitro, and normal mice experiment. Biodistribution in mice demonstrated
that the complex showed higher myocardial uptake after 0.5-hour p.i. The ratios of heart/liver (%ID/g) in the case of 99mTc(CO)3-DMSA-MIBI was higher (1.88) than that observed in case of 99mTc-MIBI1 (0.93) after 0.5-hour p.i. (P<0.05). Results showed that the complex may be developed to a novel myocardial perfusion-imaging agent. 相似文献
12.
Various plutonium compounds are handled in nuclear facilities of BARC. Hence, there is a possibility of occupational workers
getting exposed to Pu. In vitro bioassay monitoring in which Pu is separated by chemical procedures from excreta samples and
estimated by alpha-spectrometry, is the method of choice for the evaluation of internal dose to the occupational workers handling
Pu. However, this method requires a suitable Pu tracer for reducing the uncertainties due to chemical yield in the separation,
electro-deposition and counting efficiency. 242Pu is commonly used as a tracer but due to its non-availability, efforts were made earlier to indigenously synthesis 236Pu by proton irradiation of 237Np in BARC-TIFR pelletron facility. The present study, reports the feasibility of using 236Pu as a radiochemical yield monitor (tracer) in bioassay samples. 相似文献
13.
14.
Nakisa Zarrabi Ahrabi Mostafa Erfani Kazem Parivar Davood Beiki Amir Reza Jalilian 《Journal of Radioanalytical and Nuclear Chemistry》2014,299(1):461-469
Neurotensin receptors are overexpressed in several human tumors and can be targets for tumors diagnosis and therapy. In this study, a new neurotensin analogue was labeled with 99mTc via HYNIC and tricine/EDDA as coligands and investigated further. [HYNIC0, Gly7, Lys9, d-Tyr11]-Neurotensin (7–13) was synthesized using a standard Fmoc strategy. Labeling with 99mTc was performed at 100 °C for 10 min and radiochemical analysis involved ITLC and HPLC methods. The stability of radiopeptide was checked in the presence of humane serum at 37 °C up to 24 h. The receptor bound internalization and externalization rates were studied in neurotensin receptor expressing HT-29 cells. Biodistribution of radiopeptide was studied in nude mice bearing HT-29 tumor. Labeling yield of 98.6 ± 0.54 % (n = 3) was obtained corresponding to a specific activity of 81 MBq/nmol. Peptide conjugate showed good stability in the presence of human serum. The radioligand showed specific internalization into HT-29 cells (12.43 ± 0.52 % at 4 h). In biodistribution studies, a receptor-specific uptake was observed in neurotensin receptor positive organs so that after 1 h the uptakes in mouse intestine and tumor were 0.87 ± 0.16 and 0.63 ± 0.12 % ID/g respectively. 相似文献
15.
N. Farouk M. El-Tawoosy S. Ayoub A. S. El-Bayoumy 《Journal of Radioanalytical and Nuclear Chemistry》2011,290(3):685-690
Celecoxib was labelled effectively with 99mTc. The labeling yield was found to be influenced by the amount of celecoxib, the amount of stannous chloride dihydrate, the
reaction time, the temperature and the pH of the reaction mixture. The importance of stannous chloride dihydrate arises from
its function as a reducing agent for pertechnetate to form complex celecoxib. The suitable amount required to produce high
labeling yield of 99mTc-celecoxib was 500 μg SnCl2·2H2O. The pH of the reaction medium was found to play a significant role in this labeling process. The labeling reaction was
performed at a neutral medium (pH 7). The labeling reaction proceeds well at room temperature (25 ± 1 °C) and the complex
decomposes by heat. The labeled celecoxib (99mTc-celecoxib) showed a good localization in inflamed foci and a good imaging must be taken 4 h post injection. 相似文献
16.
S. P. Shirmardi M. Gandomkar M. Mazidi M. Shafiei M. Ghannadi Maragheh 《Journal of Radioanalytical and Nuclear Chemistry》2011,288(2):327-335
Tumors such as prostate, small cell lung cancer, breast, gastric and colon cancer are known to overexpress receptors to bombesin (BBN). In this study, a new bombesin analogue was labeled with 99mTc via HYNIC and tricine/EDDA as coligands and investigated further. HYNIC-GABA-Bombesin (7–14) NH2 was synthesized using a standard Fmoc strategy. Labeling with 99mTc was performed at 100 °C for 10 min and radiochemical analysis involved ITLC and HPLC methods. The stability of radiopeptide was checked in the presence of humane serum at 37 °C up to 24 h. The receptor bound internalization and externalization rates were studied in GRP receptor expressing PC-3 cells. Biodistribution of radiopeptide was studied in nude mice bearing PC-3 tumor. Labeling yield of >98% was obtained corresponding to a specific activity of ~2.6 MBq/nmol. Peptide conjugate showed good stability in the presence of human serum. The radioligand showed high and specific internalization into PC-3 cells (14.63 ± 0.41% at 4 h). In biodistribution studies, a receptor-specific uptake was observed in GRP-receptor-positive organs so that after 4 h the uptakes in mouse tumor and pancreas were 1.31 ± 0.18 and 1.2 ± 0.13% ID/g, respectively. 相似文献
17.
18.
Boris Remenec Silvia Dulanská Veronika Pau?ová L’ubomír Mátel 《Journal of Radioanalytical and Nuclear Chemistry》2011,290(2):403-407
This paper describes a simple and rapid method of 99Tc pre-concentration, separation and purification by using AnaLig? Tc02 gel in two stages or AnaLig? Tc02 gel in a first stage and TEVA? resin in a second stage, which are commercially available from IBC advanced technologies, Inc. and Eichrom technologies,
Inc., respectively. The method is suitable for analyzing large volume concentrate samples in a relatively short time. The
use and effectiveness of AnaLig? Tc02 and Eichrom’s TEVA? resin were successfully tested by analysis of evaporator concentrate samples which belong to the class of most difficult
matrices to analyze. 相似文献
19.
Amir Reza Jalilian Mahdokht Jouiaei Alireza Doroudi Javad Garousi Sedigheh Moradkhani 《Journal of Radioanalytical and Nuclear Chemistry》2010,285(3):555-561
In this work, recently prepared 67Ga-labeled glucagon (67Ga-DTPA-GCG) for imaging studies (radiochemical purity >94%; HPLC, S.A. 296–370 GBq/mM) was used in biological studies. The wild-type rat biodistribution results, 2 h post injection, demonstrated high tissue:muscle ratios for target tissues (liver, kidney, heart, spleen, fat intestine stomach and pancreas), 234, 18.45, 7.12, 1.75, 128.7, 4.9, 6.3 and 1.11, respectively. The tracer binding capacity using freshly prepared rat brain homogenate demonstrated significant specific binding of the tracer to neuronal GCG receptors (67Ga-DTPA-GCG/67Ga:3 and 67Ga-DTPA-GCG/67GaDTPA:2.2 at 90 min). SPECT images also demonstrated target specific binding of the tracer at 4 h. The data suggests the tracer is accumulated in GCGR rich tissues 2–4 h post injection, suggesting potentials of the tracer for future imaging studies in glocagonoma models. 相似文献
20.
FAN Caiyun JIA Hongmei Deuther-Conrad Winnie Brust Peter Steinbach Jrg LIU Boli 《中国科学B辑(英文版)》2006,49(2)
A novel 99mTc labeled complex, [N-[2-((2-oxo-2-(4-(3-phenylpropyl)piperazin-1-yl)ethyl) (2-mercaptoethyl)amino)acetyl]-2-aminoethanethiolato]Technetium(V) oxide (PPPE-MAMA′-99mTcO) ([99mTc]-2) has been designed and prepared based on the integrated approach. The corresponding rhenium complex (PPPE-MAMA′-ReO)(Re-2) has been prepared and characterized. In vitro competition binding assays show moderate affinity of Re-2 towards σ1 and σ2 receptors with Ki values of 8.67 ± 0.07 and 5.71 ± 1.88 μmol, respectively. Planar images obtained at 0.5 h, 4 h, 20 h after I.v. Injection indicate the accumulation of [99mTc]-2 in MCF-7 human breast tumor bearing mice at 20 h. Furthermore, the accumulation of [99mTc]-2 has been inhibited at 20 h after co-injection of [99mTc]-2 plus haloperidol (1 mg/kg). Biodistribution studies of [99mTc]-2 display an in vivo tumor uptake of 0.14% ± 0.01% ID/g at 24 h post I.v. Injection with a tumor/muscle ratio of 6.02 ± 0.87. The above results suggest that [99mTc]-2, derived from a previously published lead compound, retains certain tumor uptake and affinity for σ receptors. [99mTc]-2 may be used as a basis for further structural modifications to develop tumor imaging agents with high affinity for σ receptors. 相似文献