Conjugations of 6-Boo-hydrazinopyridine-3-carboxylic acid(Boc-HYNIC) with RC-160 [Lys5, Boc] using different coupling methods were studied. After deprotection, the resulted peptide conjugates were purified by RP-HPLC ...Conjugations of 6-Boo-hydrazinopyridine-3-carboxylic acid(Boc-HYNIC) with RC-160 [Lys5, Boc] using different coupling methods were studied. After deprotection, the resulted peptide conjugates were purified by RP-HPLC and characterized by Fab-MS. Combination with different coligands, 99mTc labeling of HYNIC modified RC-160 conjugate was carried out with high radiolabeling yield (>95%). In vitro stability studies indicated that the final radio-compound remained stable at least up to 20 h when nicotinic acid (NA) used as second coligand (tricine/NA).展开更多
One novel complex of （）99mTc-salicylidene-tyrosine Schiff base was designed and synthesized, and its biodistribution was investigated. The theoretical simulation revealed that the cis- and trans-（isomers） might co...One novel complex of （）99mTc-salicylidene-tyrosine Schiff base was designed and synthesized, and its biodistribution was investigated. The theoretical simulation revealed that the cis- and trans-（isomers） might co-exist in aqueous solution. A yield higher than 90% under the optimal condition of synthesis was obtained. Good water-solubility was demonstrated. Very little uptakes in muscle, brain, heart and S-180 sarcoma, as well as very rapid blood clearance were revealed in mice. Good accumulation in bone was shown. At 1 h postinjection the bone uptake was 10.9%ID/g. At 3 and 5 h postinjection, bone-to-muscle ratios were 19.0 and 9.3, and bone-to-blood ratios were 31.6 and 28.9, respectively. The result indicates a bone imaging potency of the complex.展开更多
To investigate a new kind of tumor tracer ^99mTc-YIGSR developed from a five amino structure （YIGSR） of the Laminin -chain, which can bind to the laminin receptors of tumor specifically, and radiolabeled with MAG3. ...To investigate a new kind of tumor tracer ^99mTc-YIGSR developed from a five amino structure （YIGSR） of the Laminin -chain, which can bind to the laminin receptors of tumor specifically, and radiolabeled with MAG3. （1） Preparation of the ^99mTc-YIGSR probe： with S-Acetly-NH3- MAG3as the chelator and with proper reductants YIGSR was labeled with ^99mTc;（2） Cell culture and viability measurement： EAC was maintained in RPMI 1640 supplemented with calf serum; the trypan blue exclusion was applied to calculate the cell viability; （3） Study of the cell dynamic： The EAC＇s uptake of ^99mTc-YIGSR and ^99mTc-MIBI was observed at 37℃ and 22 ℃, respectively. （1） The labeling efficiencies of ^99mTc-YIGSR and^99mTc-MIBI were （62±3） % and （96±2） %, respectively; （2） The cell viability was declined with time of incubation; （3） At 37 ℃, the EAC＇S uptake of ^99mTc YIGSR and^99mTc-MIBI reached the peak of （43. 16±2.4） % and （24.4±1.8） % at 60 min, respectively; and at 22 ℃, the highest uptake was （26.5±2. 1） % and （9.47±1.9） % at 60 min, respectively. The in vitro study suggests that ^99mTc-YIGSR is superior to ^99mTc-MIBI in cell uptake and has potential value in tumor imaging.展开更多
文摘Conjugations of 6-Boo-hydrazinopyridine-3-carboxylic acid(Boc-HYNIC) with RC-160 [Lys5, Boc] using different coupling methods were studied. After deprotection, the resulted peptide conjugates were purified by RP-HPLC and characterized by Fab-MS. Combination with different coligands, 99mTc labeling of HYNIC modified RC-160 conjugate was carried out with high radiolabeling yield (>95%). In vitro stability studies indicated that the final radio-compound remained stable at least up to 20 h when nicotinic acid (NA) used as second coligand (tricine/NA).
文摘One novel complex of （）99mTc-salicylidene-tyrosine Schiff base was designed and synthesized, and its biodistribution was investigated. The theoretical simulation revealed that the cis- and trans-（isomers） might co-exist in aqueous solution. A yield higher than 90% under the optimal condition of synthesis was obtained. Good water-solubility was demonstrated. Very little uptakes in muscle, brain, heart and S-180 sarcoma, as well as very rapid blood clearance were revealed in mice. Good accumulation in bone was shown. At 1 h postinjection the bone uptake was 10.9%ID/g. At 3 and 5 h postinjection, bone-to-muscle ratios were 19.0 and 9.3, and bone-to-blood ratios were 31.6 and 28.9, respectively. The result indicates a bone imaging potency of the complex.
文摘To investigate a new kind of tumor tracer ^99mTc-YIGSR developed from a five amino structure （YIGSR） of the Laminin -chain, which can bind to the laminin receptors of tumor specifically, and radiolabeled with MAG3. （1） Preparation of the ^99mTc-YIGSR probe： with S-Acetly-NH3- MAG3as the chelator and with proper reductants YIGSR was labeled with ^99mTc;（2） Cell culture and viability measurement： EAC was maintained in RPMI 1640 supplemented with calf serum; the trypan blue exclusion was applied to calculate the cell viability; （3） Study of the cell dynamic： The EAC＇s uptake of ^99mTc-YIGSR and ^99mTc-MIBI was observed at 37℃ and 22 ℃, respectively. （1） The labeling efficiencies of ^99mTc-YIGSR and^99mTc-MIBI were （62±3） % and （96±2） %, respectively; （2） The cell viability was declined with time of incubation; （3） At 37 ℃, the EAC＇S uptake of ^99mTc YIGSR and^99mTc-MIBI reached the peak of （43. 16±2.4） % and （24.4±1.8） % at 60 min, respectively; and at 22 ℃, the highest uptake was （26.5±2. 1） % and （9.47±1.9） % at 60 min, respectively. The in vitro study suggests that ^99mTc-YIGSR is superior to ^99mTc-MIBI in cell uptake and has potential value in tumor imaging.
