Synthesis of opiate receptor radioligand 11C-carfentanil and its biodistribution in rats
10.3760/cma.j.issn.0253-9780.2011.01.012
- VernacularTitle:阿片受体PET显像剂11C-卡芬太尼的制备及其生物学分布
- Author:
Hui-chun, WANG
;
Zheng-wei, ZHANG
;
Ping, LIU
;
Fang-ping, XUE
;
Hai-bo, TAN
;
Chuan-tao, ZUO
;
Feng-chun, HUA
;
Zhe-min, HUANG
;
Jun, ZHAO
;
Yi-hui, GUAN
- Publication Type:Journal Article
- Keywords:
Receptors,opioid,mu;
Carfentanil;
Carbon radioisotopes;
Rats
- From:Chinese Journal of Nuclear Medicine
2011;31(1):46-49
- CountryChina
- Language:Chinese
-
Abstract:
Objective To establish an automatic synthesis method for 11C-carfentanil (CFN) as an novel opiate receptor radioligand and study its biodistribution in rats. Methods 11C-Triflate-CH3 was bubbled into 0.5 mg precursor desmethyl-CFN (which was dissolved in 0.15 ml DMSO) to generate 11C-CFN in a V-tube at room temperature. Sep-Pak C2 column was used for purification of 11C-CFN, which was eluted by 3ml binary system aqueous solution, 10 ml water thrice, and then I ml ethanol. The biodistribution (% ID/g) of 11C-CFN in SD rats was studied. SPSS 13.0 was used for statistical analysis. Non-normal distribution data were analyzed using nonparametric test. Results The synthesis time for 11C-CFN was 20 min (end of bombardment, EOB). The synthesis yield was (35.5 ± 2.2) % on average (n = 12, uncorrected)with the radiochemical purity over 98%. Biodistribution study in rats showed that the tracer had a high brain uptake, rapid blood clearance, and a metabolic pathway via liver and kidney. The highest tracer uptake was in thalamus (4.26 ± 0.89) % ID/g and striatum (4.05 ± 1.08) % ID/g at 5 min after injection, followed by cerebral cortex (2.63±0.89) %ID/g, pons (2.26 ±0.57) % ID/g, hippocampus (2. 17 ±0.55) %ID/g and cerebellum (2. 15 ±0.39) %ID/g. Conclusions The automatic synthesis of 11C-CFN is fast and reliable, and this radioligand can be used for opiate receptor imaging.
