摘要:~3H-QNB Saturation analysis revealed typical single-site saturation curve inCHO cell line transfected with cDNA of m1, m2or m4 receptors, with Hill numbersof nearly 1. Inhibition study of ~3H-QNB binding to muscarinic receptors inmembranes of these cells revealed that PZP had an affinity of m1>m4>m2 in theCHO cells, while METH had an affinity of m2>m4>m1. Using the m2 transfectedcells, carbachol could partially inhibit the foskolin induced cAMP elevation,indicating that there was a complete pathway for the trasduction of signals raised byagonist stimulation of M2 receptors. The time course of M2 receptor density in m2transfected CHO cell lines showed a peak value at about 48h and then dropped downgradually. The above results suggest that the cell lines could be used as models forthe study of structure and function of single subtypes of muscarinic receptors as wellas for screening of drugs.
摘要:The carbachol-stimulated [~35S]GTP r S binding method was used to observe theeffect of ZMS, an active component from Zhimu, on the coupling of M-receptor toG-protein. The effect of ZMS on the ability of learning and memory in aged rats wasalso observed. It was shown that the carbachol-stimulated elevation of [~35S]GTP r Sbinding was significantly decreased in aged rats as compared with young rats. Thecarbachol-induced [~35S]GTPr S binding showed that administration of ZMS atmedian or high dose have a definite elevation effect on the coupling activity ofM-receptors to G-protein in brain, and this elevation was accompanied by animprovement of learning and memory ability.
关键词:ZMS;[35S]GTP r S binding;Muscarinie receptor;G-protein
摘要:The objective of this paper is to investigate the characteristics of expression anddistribution of 3 subtypes of somatostatin receptors (SSTRI-3) in breast cancer.With [a-~35S] dATP labeled oligonucleotide of the 3 SSTR subtypes as probe, using insitu hybridization, patterns of mRNA expression were detected in 10 breast cancercases. Additionally, semi-quantitative analysis of the densities of the expression wereestimated by a compreterized image-analysis system. Patterns of SSTR1-3expression in breast cancer were as follows: SSTR2 expression was dominant in 10cases than that of the other 2 subtypes; Therefore, it has positive prospects forsomatostatin analog-oriented agents to be used in treatment of breast cancers.
摘要:To explore the mechanism of mitogenic effect of aFGF on vascular endothelialcell(EC) and smooth muscle cell(SMC), the ~125I-acid fibroblast growth factor (aFGF)was used as radioligand. The radioassay was applied to detect the expression of aFGFreceptor of vascular EC and SMC. The results showed that the specific binding sitesand affinity of aFGF receptor in EC and SMC increased significantly in exponentproliferating phase vs quiescent phase and aFGF mediated cellular response bybinding and activation of specific high-affinity cell surface receptor.
摘要:Nuclear Ca~2+ regulates many biochemical processes in the nucleus. There existCa~2+ uptake and release systems in the nucleus, which control [Ca~2+] in the nucleus.Several techniques are described here including Ca~2+ uptake and releasemeasurement in isolated nuclei, the measurement of Ca~2+ transporting into innernuclear membrane vesicles, etc. These techniques are efficient to study the roles ofnuclear Ca~2+ -uptaking and releasing system in physiological and pathologicalprocesses.
摘要:Galactosylneoglycoalbumin (NGA) is aspecific ligand of asialoglycoproteinreceptor (ASGPR) in hepatocyte surface.In this paper,the imaging comparison of~99mTc-NGA and ~99mTc-HSA in normal rabbit imaging are reported. ~99mTo-HSAgenerated a blood pool image when injected into normal rabbit, while ~99mTo-NGAshowed a hepatic receptor image charateristics. If rabbit hepatic receptor had beensaturated with 100 times amounts of NGA, ~99mTc-NGA would generate a blood poolimaging sunilar to ~99mTc-HSA. Flow cytometry (FCM) analysis with FITC-NGA alsoshowed that ASGPR could be obviously saturated. Therefore, ~99mTc-NGA is ahepatic receptor image agent.
摘要:An automatic method of extracting left ventricle from SPECT myocardialperfusion data was introduced. This method was based on the least square analysis ofthe positions of all short-axis slices pixels from the half sphere-cylinder myocardialmodel, and used a iterative reconstrution technique to automatically cut off thenon-left rentricular tissue from the perfusion images. Thereby, this techniqueprovided the bases for further quantitative analysis.
摘要:The study was performed with cold-induced ~99mTc (MIBI) myocardial imaging(MI) in 23 patients with systematic scleroderma. The left ventricular function andwall motion were also observed by dimensional echocardiography(UCG). 14 patientshad myocardial perfusion abnormalities visualized by MI, including 5 cases with fixeddefects of 9 segments, 3 cases with reversible defects of 6 segments and 6 cases withboth fixed and reversible one of 14 segments. The positive rate in myocardial imaginghad no significant differences between patients with and without Raynaud’sphenomenon (0.5>P>0.25). Compared with baseline, the ejection fraction, strokevolume, cardiac output were significantly decreased during cold--induced in patientswith abnormal myocardial scinti-graphy (P<0.05), and had significant differencecompared with normal group (P<0.05). 4 cases with cold-induced reversibleperfusion defects had anatomically correlated regional ventricular hypokinesis inUCG.
摘要:The effects of attenuation correction coefficient, radioactivity, volumedimensions, radio deficit area and threshold on the measurement of organ volumewere investigated using 3 groups of phantom. The results showed that the measuredvolume without attenuation correction was higher than the real volume of phantomsin the reconstruction of SPECT images. The measured volume was getting smaller asthe correction coefficient increased. When correction coefficient’ was 0.1, themeasured volume approximated mostly the real volume of phantom. There was nosignificant change in the measured volumed when radioactivity ranged from 37 to185kBq/mL (P>0.05). The measured volume decreased as threshold increasing andbest results were obtained when the threshold was 48%. The presence of radio deficitarea showed no influence for the determination of functional volume. Conclusions:the best results can be obtained with Change’s attenuation correction method inreconstruction with correction coefficient 0.1 and threshold 48%.
关键词:SPECT;Radionuclide;Determination of organ volume
摘要:1,2-dihydroxy-1,2-his (dihydroxy phosphonyl) ethane (DHPE), 2,3-dihydroxy2,3-bis (dihydroxy phosphonyl) butane (DHPB) and 2,4-dihydroxy-2,4-bis(dihydroxy phosphonyl) pentane (DHPP) were synthesized and were labelled by ~99mTc.The influencing factors were studied and the best labelling procedures.were obtained.The biodistribution of ~99mTc-DHPE, 99mTc-DHPB and ~99mTc-DHPP in mice wereevaluated. The results of the biodistribution show significant accumulation of all theabove three ligands in mouse bone.
摘要:Due to the high affinity of biotin to Av or SA. We labelled a biotin derivative(DTPA-biotin) with ~153Sm and then bound this 153Sm labelled DTPA-biotin to Av orSA. The in vivo kinetics and biodistribution of 153~Sm labelled, Av, SA andDTPA-biotin were studied in the rat and mice. The results demonstrated that153Sm-Av cleared from the blood rapidly with high liver and renal uptake; ~153Sm-SAcleared from blood slowly with high retention in liver, spleen and kidney, whereas153Sm metabolize more fast, and excreted mainly through the kidney. Thereby, thebiodistribution difference of SA and Av mentioned above provided an expermentalbasis for the selection of different components of A-V system in pretagetingradioimmuno imaging and radioimmunotherapy.
摘要:~188Re labelled stannic sulfur suspension was prepared with two-steps: At firstacid ~188Re labelled suspension was obtained by adding stannous chloride into acidicsolution of ~188Re perrhenate and sodium thioslphate, then adjust the pH of thesolution to neutral point with NaOH and Na2HPO4 and 188Re labelled stannic sulfursuspension was formed. The particles sizes of this suspension were 2-5 U m mainly.The radiochemical purity was above 95%. The suspension was stable in vitro andvivo tests. Finally, animal experiments observed that the tumor inhibiting rate of this~188Re labelled stannic sulfur suspension was 90% in human glioma bearing nude mice.
摘要:A new complex: ~188Re-tetrofosmin has been prepared by heating in a water bath.The RCP of ~188Re-tetrofosmin was over 90% by TLC, and stable over 6h at roomtemperature. The biodistribution of the complex in mice was similar to that of themyocardial imaging agent: ~99mTc-tetrofosmin, 188Re-tetyofosmin should be a cationiccomplex with a linear trans-oxo core.
摘要:Monoclonal Antibody can be directly labelled with 186Re or 188Re. Usinganti-human brain glioma monoclonal antibody (SZ-39) as a model, we studied somefactors that influence labelling efficiency, such as PH of reaction mixture, varioustranschelation agents (sodium tartrate, sodium citrate, sodium gluconate), thelabelling time and reduction agents (AA, DTT, 2-ME) for reducing disulfide groupsin SZ39. At last, we established a better labelling method. The optimum PH wasshowed to be 2.54, sodium gluconate was used as transchelation agent. The labellingefficiency as determined by thin-layer chromatography and HPLC analysis was96.2%. The labelled SZ39 was tested by quantitative HPLC to determine theradiochemical purity and subsequent purification was collected for testing stability invitro. The labelled SZ39 has high radiochemical purity and was stable in 4°C by whenBSA was added.
关键词:186ReO4-;SZ39;Transchelation agent;Reducing agent;Stability in vitro