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1.
Liqin Liu Manchen Zhao Zhuo Wang Yuanyan Qin Xuebin Wang 《Journal of Radioanalytical and Nuclear Chemistry》2014,301(3):731-737
A conjugate of 6-hydrazinopyridine-3-carboxylic acid (HYNIC) with the d-Glucosamine Hydrochloride (DG) was synthesized though a multiple-step reaction. HYNIC-DG could be labeled successfully and efficiently with 99mTc using N-[2-hydroxy-1,1-bis(hydroxymethyl)ethyl]glycine (tricine) and ethylenediamine-N,N′-diacetic acid (EDDA) or tricine and triphenylphosphine-3,3′,3″-trisulfonic acid trisodium salt (TPPTS) as co-ligands to form two 99mTc-HYNIC-DG complexes 99mTc-(t/E)HYNIC-DG and 99mTc-(t/T)HYNIC-DG in high yields (>95 %). The partition coefficient and electrophoresis results indicated they were very hydrophilic and electronegative. The biodistribution studies of two 99mTc-HYNIC-DG complexes in Kunming mice bearing S 180 tumor showed that 99mTc-(t/T)HYNIC-DG has more favorable characteristics than 99mTc-(t/E)HYNIC-DG. High tumor uptake, low or negligible accumulation in non-target organs, and good retention, suggesting 99mTc-(t/T)HYNIC-DG would be a novel potential tumor imaging agent. 相似文献
2.
Xuebin Wang 《Journal of Radioanalytical and Nuclear Chemistry》2001,249(3):523-525
In this study, the preparation of the 99m TcN complex of DMSA (dimercaptosuccinicacid) was carried out as a freeze-dried formulation, through a simple procedureinvolving the initial of 99m TcO 4 – with succinic dihydrazide in thepresence of stannous chloride as reducing agent, followed by the additionof the ligand DMSA to afford the final product. The radiochemical purity ofthe 99m TcN-DMSA complex was over 90% determined by thin layer chromatography.It was stable over 8 hours at room temperature. Its partition coefficientindicated that it was a good hydrophilic complex. Biodistribution in miceshowed that the 99m TcN-DMSA complex was accumulated in bone with high uptakeand good retention, suggesting it would be potentially useful as a bone imagingagent containing the [ 99m TcN] 2+ core. The biodistribution comparison inmice of the 99m TcN-DMSA complex and the 99m Tc-DMSA complex indicate thatthe presence of the 99m Tc nitrido group significantly alters the biologicalproperties of the 99m Tc complex. 相似文献
3.
JunBo Zhang XueBin Wang ChunJun Tian 《Journal of Radioanalytical and Nuclear Chemistry》2004,262(2):505-507
The preparation of the bis(N-propyl dithiocarbamato) nitrido technetium-99m complex 99mTcN(PDTC)2 (PDTC: N-propyl dithiocarbamato) was carried out as a freeze-dried formulation, through a simple procedure involving the
initial of 99mTcO4- with succinic dihydrazide in the presence of stannous chloride as reducing agent and propylenediamine tetraacetic acid (PDTA)
as complexant, followed by the addition of the ligand sodium salt of N-propyl dithiocarbamate to afford the final product.
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 12 hours. Its partition coefficient indicated that it was a good lipophilic
complex. Biodistribution in mice showed that the complex accumulated in the brain with high uptake. The brain uptake (ID%/g)
was 5.07 and the brain/blood ratio 1.34 at 5-minute post-injection. This suggested a potential usefulness of the complex as
a brain perfusion imaging agent.
This revised version was published online in July 2006 with corrections to the Cover Date. 相似文献
4.
Synthesis and biodistribution of 99mTcN(CHIPDTC)2 as a potential myocardial perfusion imaging agent 总被引:1,自引:0,他引:1
JunBo Zhang XueBin Wang ChunYun Li 《Journal of Radioanalytical and Nuclear Chemistry》2002,254(1):99-101
The bis(N-cyclohexyl, N-isopropyl dithiocarbamato) nitrido technetium-99m complex [99mTcN(CHIPDTC)2] (CHIPDTC: N-cyclohexyl, N-isopropyl dithiocarbamato) has been synthesized through a ligand-exchange reaction. The two-step procedure involved the initial reaction of 99mTcO4
- with succinic dihydrazide (SDH) in the presence of stannous chloride as reducing agent and propylenediamine tetraacetic acid (PDTA) as complexant, followed by the addition of the sodium salt of N-cyclohexyl, N-isopropyl dithiocarbamate. The radiochemical purity (RCP) of the complex was 96±2% as measured by thin layer chromatography (TLC). No decomposition of the complex at room temperature (r. t.) was observed within a period of 6 hours. Its partition coefficient indicated that it was a lipophilic complex. The electrophoresis results showed that the complex was neutral. Biodistribution in mice indicated that the complex accumulated in the heart with high uptake and good retention. The heart/blood, heart/lung ratio was 6.28 and 1.35, respectively, at 60-minute post-injection, suggesting that it would be a potential myocardial perfusion imaging agent. 相似文献
5.
M. S. Iqbal M. H. Rizvi A. Naqvi 《Journal of Radioanalytical and Nuclear Chemistry》1992,162(1):139-144
New Schiff bases, salicylidene- and pyridoxylidene-thyroxine have been prepared and characterized. They were labeled with99mTc. The labeling yield of the Schiff bases was over 95%. About 60% of the activity was bound to -globulin and albumin fractions when the labled compounds were incubated with a serum sample. The labeled compounds, after i.v. administration to rats, rapidly cleared from blood and excreted into the small intestine. They appeared to behave as hepatobiliary agents. 相似文献
6.
《Journal of Coordination Chemistry》2012,65(3):470-481
Diethylenetriaminepentaacetic di(L-dopa ethyl ester) ligand (DTPA-2LDEE) was synthesized by reaction between diethylenetriaminepentaacetic dianhydride (DTPAA) and L-dopa ethyl ester (LDEE). This ligand reacted with gadolinium chloride and sodium pertechnetate to make the corresponding neutral gadolinium complex Gd-DTPA-2LDEE and technetium-99m-labeled complex 99mTc-DTPA-2LDEE, respectively. The ligand and complexes were characterized and their properties in vitro and in vivo were also evaluated. Gd-DTPA-2LDEE possessed higher relaxation effectiveness and lower cytotoxicity to human hepatoma HepG-2 cells than Gd-DTPA. 99mTc-DTPA-2LDEE had enhanced single-photon emission computed tomography (SPECT) signal enhancements of the kidneys in rats and provided longer duration time than that of 99mTc-DTPA. Therefore, 99mTc-DTPA-2LDEE can be selectively excreted by the kidneys and used as a potential radioactive probe in SPECT. 相似文献
7.
Miao Liu Xiao Lin Xiaoqing Song Yang Cui Peiwen Li Xuebin Wang Junbo Zhang 《Journal of Radioanalytical and Nuclear Chemistry》2013,298(3):1659-1663
In the present study, proline dithiocarbamate (PRODTC) ligand was radiolabeled with the [99mTc≡N]2+ core successfully to obtain the 99mTcN-PRODTC complex with high radiochemical purity. No decomposition of the complex at room temperature was observed over a period of 6 h. Its partition coefficient indicated that it was a hydrophilic complex. The electrophoresis results showed that the complex was negative. The biodistribution of 99mTcN-PRODTC in mice bearing S 180 tumor showed that the complex accumulated in the tumor with a certain uptake. The tumor/blood and tumor/muscle ratios reached 2.19 and 4.54 at 2 h post-injection, suggesting it would be a promising candidate for tumor imaging. 相似文献
8.
Synthesis of a technetium-99m-labeled thymidine analog: a potential HSV1-TK substrate for non-invasive reporter gene expression imaging 总被引:1,自引:0,他引:1
{2-[5-(2′-Fluoro-2′-deoxyuridin-5-yl)pent-4(E)-enyl] [2-(2-mercaptoethyl)aminoethyl]aminoethanethiolato(3)-N,N′,S,S′}oxo-[99mTc]technetium(V), a potential viral thymidine kinase substrate, was synthesized by coupling 2′-fluoro-2′-deoxyuridine analog with a N2S2 radiometal chelator, followed by [Tc-99m]technetium conjugation. The chemical structure of the radioactive probe was characterized by 1H NMR and high resolution MS using Re-188 conjugated mimics. The radiochemical purity and yield were identified as 98% and 42%, respectively. 相似文献
9.
Ayfer Yurt Kilcar Fazilet Zumrut Biber Muftuler Huseyin Enginar Volkan Tekin Emin Ilker Medine Perihan Unak 《Journal of Radioanalytical and Nuclear Chemistry》2014,302(1):563-573
Recently, the development of novel brain imaging agents has aroused much interest thanks to limited number of brain cancer or diseases diagnosis agents. It is aimed to synthesize a novel brain imaging agent including a promise for further studies on AD diagnosis potential and investigate its bioaffinity with biodistribution studies on healthy Balb/c mice. A novel radiolabeled agent was synthesized and characterized. Quality control of 99mTc-BH was performed utilizing solvent extraction and chromatographic (Radio TLC and Radio HPLC) methods. Bioaffinity of the 99mTc-BH was investigated on male Balb/c mice at various time points (5, 30, 60, 120 min post-injection). Paper electrophoresis showed that 99mTc-BH has a neutral structure. Radiochemical purity of 99mTc-BH was over 95 % with appropriate stability for imaging period. Selected brain regions have uptakes over 4 % ID/g following intravenous injection. Hippocampus has uptake approximately 10 % ID/g. 99mTc-BH has shown brain uptake, so it may prove to be valuable for brain imaging as a novel technetium-labeled agent. Further investigations with AD animal model are our on going effort to show that this agent has AD diagnosis potential. 相似文献
10.
A. Bumbálová E. Havránek M. Harangozó P. Křenek S. Lübkeová 《Journal of Radioanalytical and Nuclear Chemistry》1991,154(1):53-59
The preparation of N1-(octadecylcarbomyl-methy)-ethylenediaminetriacetic acid labelled with99mTc is described. Reduction of technetium was made using sodium borohydride (procedure A) or stannous chloride (procedure B), and the labelling efficiency was checked by thin layer chromatography. Preliminary studies of biol-behavior of this complex were performed in white rats. 相似文献
11.
HaiXun Guo JunBo Zhang Zhi Wei Ma ZueBin Wang 《Journal of Radioanalytical and Nuclear Chemistry》2008,275(1):121-123
A novel 99mTc nitrido xanthate complex 99mTcN(IPEXT)2 (IPEXT: isopentyl xanthate) has been synthesized by the reduction of 99mTcO4
− into [99mTcN]2+ with stannous chloride in the presence of succinic dihydrazide and propylenediamine tetraacetic acid, followed by the addition
of the corresponding xanthate ligand. The radiochemical purity of the complex was over 90% as measured by thin layer chromatography
(TLC). 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 99mTcN(IPEXT)2 complex accumulated in the heart with high uptake. The heart uptake (%IDg) was 8.00% at 5-minute post-injection, but the
heart/lung, heart/liver and heart/blood ratios were not high, thereby, restricting the use of the complex as a good myocardial
imaging agent. 相似文献
12.
Junbo Zhang Qian Yu Jinfeng Huo Yan Pang Sheng Yang Yining He Tingting Tang Chenchen Yang Xuebin Wang 《Journal of Radioanalytical and Nuclear Chemistry》2010,283(2):481-485
The dimercaptosuccinic acid metronidazole ester (DMSAMe) was synthesized and radiolabeled with 99mTc to form the 99mTc-DMSAMe complex in high yield. The radiochemical purity of the 99mTc-DMSAMe complex was over 90%, as measured by TLC and by HPLC, without any notable decomposition at room temperature over
a period of 6 h. Its partition coefficient indicated that it was a lipophilic complex. The tumor cell experiment and the biodistribution
in mice bearing S 180 tumor showed that the 99mTc-DMSAMe complex had a certain hypoxic selectivity and accumulated in the tumor with high uptake and good retention. The
tumor/blood and tumor/muscle ratios increased with time, suggesting it would be a possible tumor hypoxia imaging agent. 相似文献
13.
M. Neves H. Ferronha L. Patricio 《Journal of Radioanalytical and Nuclear Chemistry》1989,132(2):241-249
Labelling kinetic studies, radiochemical characterization and particle size evaluation of technetium-99m rhenium sulfide colloid using formamidine sulfinic acid as reducing agent are described. Comparison with the same colloid which makes use of Sn-sodium pyrophosphate complex as reducing agent has shown higher labelling yields, simplification of labelling procedure and a longer shelf life when formamidine sulfinic acid is used. 相似文献
14.
HE Qiange CHEN Xiangji MIAO Yubin & LIU Boli Chemistry Department Beijing Normal University Beijing China 《中国科学B辑(英文版)》2004,47(6):499-506
Quantification of regional cerebral blood flow(rCBF) plays an important role in the diagnosis ofvarious cerebrovascular and neurological diseases. Innuclear medicine, brain perfusion imaging can providesituation of whole or regional cerebral blood flowperfusion (CBF or rCBF) to neurologists, help to findabnormality of cerebral blood flow before cere-brovascular and neurological diseases induce patho-logical changes in configuration or structure of brain.They offer important information for … 相似文献
15.
André Luís Branco de Barros Saulo Fernandes de Andrade José Dias de Souza Filho Valbert Nascimento Cardoso Ricardo José Alves 《Journal of Radioanalytical and Nuclear Chemistry》2013,298(1):605-609
Glycodendrimers are neoglycoconjugates that can be considered as bioisosters of glycoproteins, since they can mimic the multivalent interactions of lectin-carbohydrate. The ability of glycodendrimers to present multivalent interactions with lectins as compared to a monovalent ligand is referred to as “cluster effect”. It is expected that, because of the cluster effect, glycodendrimers would result in a better association with lectins than mono-carbohydrate anchored systems. Radioisotopes are useful to evaluate biodistribution of molecules. This study is important to obtain information about molecule–receptor interactions. Indeed, such study can provide an exquisite tool to evaluate the affinity of certain molecules to specific areas in the body, leading to the development of new radiopharmaceuticals and/or drug delivery systems. Herein, we describe a d-galactose coated low molecular weight PAMAM G0 dendrimer that was successfully radiolabeled with technetium-99m. Biodistribution studies and scintigraphic images were performed in healthy mice. It was observed high liver uptake which was significantly reduced in blocking studies, indicating hepatic specificity. Therefore, low molecular weight glycodendrimer can be considered as useful platform for selective targeting of drugs to the liver and to assess hepatic function. 相似文献
16.
This paper describes biologic distributions, sequential images and macroautoradiograms of 99mTcO4 (pertechnetate), 99mTc-Sn-HSA (human serum albumin) and 99mTc-Sn-TSL (trasylol) in tumor-bearing mice as the first report on tumor affinity of 99mTc-labeled radiopharmaceutical. (1) Maximum tumor concentration (% administered dose/g of tissue weight) of 99mTcO4, 99mTc-HSA and 99mTc-TSL in Ehrlich's tumor-bearing mice resulted in 2.03+/-0.57 at 1 hr, 4.02+/-0.19 at 3 hr and 1.97+/-0.31 at 1 hr respectively. (2) However, tumor to blood concentration ratio of 99mTc-HSA was lowest among them. (3) The corrected tumor accumulation (% 100g dose/g of tissue wt.=% dose/% body weight) of 99mTc-TSL to Ehrlich's tumor in mouse was not different from that of Yoshida's sarcoma in rat, on the contrary to our expectation that the tumor concentration of 99mTc-TSL in them might be different due to differency of the tissue fibrinolytic activity between the respective tumors. (4) Sequential images of the implanted tumor in mouse was best positively delineated with 99mTc-HSA. (5) Macroautoradiograms of Ehrlich's tumor with 99mTcO4, 99mTc-HSA and 99mTc-TSL demonstrated the following findings: all of them were not only accumulated markedly into the tumor cells which were shown as basophilic tissue with H?matoxylin-Eosin staining but also accumulated around the tumor tissue and on the interstitial tissue which were stained as eosinophilic tissue with the above same staining. 相似文献
17.
Attempts have been made to employ magnesium oxide as the preconcentration agent for determination of trace metal sin seawater by neutron activation analysis. Hydrous magnesium oxide can efficienthy adsorb most cationic transition metals and rare earths in a simple water system. The adsorption behavior is believed to depend mainly from the association of the cationic species of the metals with MgO
2
2–
adsorbent. In seawater matrix some of the metal ions such as Hg2+, Ni2+, etc. may become inefficiently adsorbed owing to the formation of highly stable metal-chloro complexes with chloride ion. Usually the adsorption efficiencies of the metals can be recovered to be as high as the case in the simple water system if an acidified seawater (to pH1) is subjected to the adsorption experiment. In practice, a large volume of seawater (5 1) is stirred with a small amount of hydrous MgO (1 g). Thereafter, the trace metals adsorbed MgO is separated and taken to be neutron activated. The abundant sodium ion and ubiquitous bromide ion can be obviated by the adsorption process, thereby beneficial to the -spectrometry of the metals enriched on MgO. 相似文献
18.
19.
Liqin Liu Min Zhang Guangrong Zhong Xuebin Wang 《Journal of Radioanalytical and Nuclear Chemistry》2011,287(3):847-852
A conjugate of 6-hydrazinopyridine-3-carboxylic acid (HYNIC) with the amino analogue of metronidazole (MN) was synthesized
through a multiple-step reaction. HYNIC-MN could be labeled easily and efficiently with 99mTc using N-(2-hydroxy-1,1-bis(hydroxymethyl)ethyl)glycine (tricine) and ethylenediamine -N,N′-diacetic acid (EDDA) as coligands to form the 99mTc–HYNIC–MN complex in high yield (>95%). Its partition coefficient indicated that it was a good hydrophilic complex. The
tumor cell experiment showed that the 99mTc–HYNIC–MN complex had a certain hypoxic selectivity. The biodistribution studies of 99mTc–HYNIC–MN in Kunming mice bearing S180 tumor showed a favorable tissue distribution profile with high tumor uptake, and
low or negligible accumulation in non-target organs, suggesting 99mTc–HYNIC–MN would be a novel potential tumor hypoxia imaging agent. 相似文献
20.
Mohamed A. Motaleb Mostafa Y. Nassar 《Journal of Radioanalytical and Nuclear Chemistry》2014,299(3):1759-1766
Phytochlorin [21H, 23H-Porphine-7-propanoicacid, 3-carboxy-5-(carboxymethyl)13-ethenyl-18-ethyl-7,8-dihydro-2,8,12,17-tetramethyl-,(7S,8S)] was labeled with 99mTc and the factors affecting the labeling yield of 99mTc-phytochlorin complex were studied in details. At pH 10, 99mTc-phytochlorin complex was obtained with a high radiochemical yield of 98.4 ± 0.6 % by adding 99mTc to 100 mg phytochlorin in the presence of 75 μg SnCl2·2H2O after 30 min reaction time. The molecular modeling study showed that the structure of 99mTc-phytochlorin complex presents nearly linear HO–Tc–OH unit with an angle of 179.27° and a coplanar Tc(N1N2N3N4) unit. Biodistribution of 99mTc-phytochlorin complex in tumor bearing mice showed high T/NT ratio (T/NT = 3.65 at 90 min post injection). This preclinical study showed that 99mTc-phytochlorin complex is a potential selective radiotracer for solid tumor imaging and afford it as a new radiopharmaceutical suitable to proceed through the clinical trials for tumor imaging. 相似文献