Radiosynthesis and Biological Evaluation of N-[18F]Labeled Glutamic Acid as a Tumor Metabolic Imaging Tracer: e93262

• Published in: PloS one Vol. 9; no. 3
• Main Authors: Hu, Kongzhen, Du, Kan, Tang, Ganghua, Yao, Shaobo, Wang, Hongliang, Liang, Xiang, Yao, Baoguo, Huang, Tingting, Zang, Linquan
• Format: Journal Article
• Language: English
• Published: 01.03.2014
• DOI: 10.1371/journal.pone.0093262

We have previously reported that N-(2-[18F]fluoropropionyl)-L-methionine ([18F]FPMET) selectively accumulates in tumors. However, due to the poor pharmacokinetics of [18F]FPMET in vivo, the potential clinical translation of this observation is hampered. In this study, we rationally designed and synthesized [18F] or [11C]labeled N-position L-glutamic acid analogues for tumor imaging. N-(2-[18F]fluoropropionyl)-L-glutamic acid ([18F]FPGLU) was synthesized with a 30 plus or minus 10% (n = 10, decay-corrected) overall radiochemical yield and a specific activity of 40 plus or minus 25 GBq/ mu mol (n = 10) after 130 min of radiosynthesis. In vitro cell experiments showed that [18F]FPGLU was primarily transported through the XAG- system and was not incorporated into protein. [18F]FPGLU was stable in urine, tumor tissues, and blood. We were able to use [18F]FPGLU in PET imaging and obtained high tumor to background ratios when visualizing tumors tissues in animal models.