Preparation and microPET imaging of somatostatin receptor antagonist 68 Ga-NOTA-JR11
10.3760/cma.j.issn.2095-2848.2019.08.006
- VernacularTitle:生长抑素受体拮抗剂68Ga-NOTA-JR11的制备及其microPET显像
- Author:
Qing XIE
1
;
Hua ZHU
;
Teli LIU
;
Xiaoyi GUO
;
Jiangyuan YU
;
Zhi YANG
Author Information
1. 北京大学肿瘤医院暨北京市肿瘤防治研究所核医学科、恶性肿瘤发病机制及转化研究教育部重点实验室 100142
- Keywords:
Antistatic agents;
Receptors;
somatostatin;
Isotope labeling;
Gallium radioisotopes;
Positron-emission tomography;
Mice
- From:
Chinese Journal of Nuclear Medicine and Molecular Imaging
2019;39(8):473-477
- CountryChina
- Language:Chinese
-
Abstract:
Objective To prepare a novel somatostatin receptor (SSTR) antagonist 68Ga-1,4,7-triazacyclononane-1,4,7-triacetic acid (NOTA)-JR11 (Cpa-c(D-Cys-Aph(Hor)-D-Aph(Cbm)-Lys-Thr-Cys)-D-Tyr-NH2 ) tracer and observe its biodistribution and microPET imaging in mice. Methods One ml HCl (0.05 mol/L) containing 68GaCl3(148 MBq) was added into 65μl NaAc (1 mol/L) and 4μg NOTA-JR11. The mixture reacted at 95 ℃ for 15 min, and then was purified with Sep-Pak? C18 Light column to obtain 68 Ga-NOTA-JR11. 68 Ga-NOTA-JR11 was subjected to quality control analysis including radiochemical purity and in vitro stability by radio-high performance liquid chromatography. Biodistribution of 68Ga-NOTA-JR11 (0.37 MBq) in BALB/c mice (n=9) at 5, 30, 60 min postinjection were observed (n=3 for each time point), and the percentage activity of injection dose per gram of tissue (％ID/g) was calculated. 68Ga-NOTA-JR11 (14.8 MBq) microPET imaging of BALB/c mice (n=1) at 60 min postinjection was observed. Results 68 Ga-NOTA-JR11 was obtained successfully within 15 min, with yielding rate of 90％, radiochemical purity of more than 99％, and specific activity of 6. 10 GBq/μmol. The tracer showed excellent stability ( radio-chemical purity:95％) in different buffers within 150 min. The biodistribution was basically consistent with microPET imaging results. 68 Ga-NOTA-JR11 was metabolized through the kidneys and had low uptake in the liver ((0.75±0.26) ％ID/g) at 60 min postinjection. Conclusions 68 Ga-NOTA-JR11 can be prepared rapidly, with high yielding rate and radiochemical purity. Biodistribution and imaging results provide basic information for the further study of somatostatin receptor imaging in neuroendocrine tumors.
