A Study on the Synthesis and Its Biodistribution of C-11 and F-18 Labelled Choline

2001 
Objectives: Recently, -Hydroxyethyl)trimethylammonium (choline) Has been discovered to be a very effective tracer in imaging various human tumors using positron omission tomography. Because of the short half-life of C-11, it is very difficult to use in a routine imaging procedure and needs a frequent synthesis of choline. This can be supplemented by the substitution of choline with fluorocholine. Here, we would like to report ceil uptake and biodistribution of choline and fluorocholine as a basic study. Methods: Choline was prepared by the treatment of with N,N-dimethylaminoethanol and fluorocholine was synthesized from reaction of with N,N-dimethylaminoethanol. The radiochemical purity was checked by high performance liquid chromatography (HPLC). The blodistribution of choline and fluorocholine was determined in balb/c mouse at 5 min, 20 min, 40 min and 80 min. The cell uptake was measured using glioma (9L) and colon adenocarcinoma (SW620). Results: The radiochemical purity was more than 98% after purification. In the liver, uptake did not change over time; the uptake was 20%ID/g for choline and 13%ID/g for fluorocholine. In the kidney, radioactivity decreased over time; the uptake was 15%ID/g for choline and 20%ID/g for fluorocholine, 80 min post-injection. The cell uptake of choline was 4.93% for glioma (9L) and 18.69% for colon adenocarcinoma (SW620). For fluorocholine, 1.77% for glioma (9L) and 2.77% for colon adenocarcinoma (SW620). Conclusion: Choline and fluorocholine showed a different cell uptake tendency, depending on cancer cell line.
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