Targeting islet cell using 18F-Fallypride: in vitro and histoautoradiography study
10.3760/cma.j.issn.2095-2848.2015.02.012
- VernacularTitle:18F-Fallypride靶向胰岛细胞摄取的实验研究
- Author:
Jianhua WANG
;
Jian ZHANG
;
Gaofeng SUN
;
Fei FENG
;
Yutao WANG
;
Can TU
;
Changjing ZUO
- Publication Type:Journal Article
- Keywords:
Islets of langerhans;
Fallypride;
Fluorine radioisotopes
- From:
Chinese Journal of Nuclear Medicine and Molecular Imaging
2015;35(2):131-134
- CountryChina
- Language:Chinese
-
Abstract:
Objective To evaluate the feasibility of dopamine D2 receptor imaging agent (s)-(-)-N-(1-allylpyrrolidine-2-N-methyl)-5-(3-18F)-2,3-dimethoxy Benzamide (18F-Fallypride) for targeting islet cell imaging.Methods (1) Cytology experiment:Islet cells of 15×103 cells/well were incubated with 3.70 kBq/well 18F-Fallypride for 1 h and the uptake rate of cells was calculated (cell counts/(supernatant counts + cell counts)× 100%).Under the same experiment conditions,6 inhibiting groups were administrated with different concentration of dopamine inhibitors droperidol (1.0× 10-6,4.0× 10-6,2.0× 10-5,1.0× 10-4,5.0× 10-4 and 1.0× 10-3 mol/L,respectively).After 30 min,3.70 kBq of 18F-Fallypride was added to each inhibiting group,and the inhibiting rate was calculated.(2) Autoradiography:18 normal ICR mice were divided into 6 groups.For group A,ICR mice were injected with 18F-Fallypride (55 ± 5) MBq/mice through tail vein.For the other 5 inhibiting groups (group B-F),ICR mice were injected with different doses of droperidol (0.2,0.4,0.6,0.8 and 1.0 mg/kg,respectively),and after 30 min 18F-Fallypride were injected through tail vein.Ten minutes later,pancreas of ICR mice was taken for preparation of tissue section autoradiography.The data were analyzed by one-way analysis of variance and the least significant difference t test.Results (1) The 18F-Fallypride uptake rate of control group was (18.40± 1.21) %.The uptake rates of inhibiting groups were (16.11±1.37)%,(15.76±0.99)%,(13.90±1.02)%,(8.86±0.73)%,(7.26±0.62)% and (6.92±0.58)%,respectively,which decreased with the decreasing concentration of droperidol (F=50.01,P<0.01).When the concentration of droperidol was 1.0× 10-4 mol/L,the uptake rate reached the lowest with inhibiting rate of 51.85%.(2) The autoradiography showed that the pancreas gray scale value of group A was 1.21×106 digital light units (DLU)/mm2.The pancreas gray scale value of groups B to F decreased with increasing concentration of inhibitor:0.93× 106,0.77× 106,0.59× 106,0.32× 106 and 0.25×106 DLU/mm2,respectively.Conclusions 18F-Fallypride may specifically and efficiently bind to dopamine receptors of islet cells.It may be a potential tracer for islet cells imaging.