期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 96, 期 -, 页码 -出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2023.129528
关键词
Procainamide; Malignant melanoma; 18 F-labeling; Positron emission tomography; Molecular imaging
In this study, 18F-labeled procainamide (PCA) was synthesized and evaluated for its potential as a PET imaging agent for melanoma detection. The results showed that 18F-PCA exhibited high melanoma uptake and could be a promising tool for direct melanoma detection using PET imaging.
Malignant melanoma has an aggressive nature and a high metastatic propensity resulting in the highest mortality rate of any skin cancer. In this study, we synthesized 18F-labeled procainamide (PCA) for detection of melanoma using positron emission tomography (PET), and evaluated its biological characteristics. The non-decay-corrected radiochemical yield of 18F-PCA was 10-15% and its in vitro stability was over 98% for 2 h. At 1 h, cellular uptake of 18F-PCA was 3.8-fold higher in a group with the presence of L-tyrosine than in a non-L-tyrosine-treated group. Furthermore, 18F-PCA permitted visualization of B16F10 (mouse melanoma) xenografts on microPET after intravenous injection, and was retained in the tumor for 60 min, with a high tumor-to-liver uptake ratio. 18F-PCA showed specific melanoma uptake in primary lesions with a high melanin targeting ability in small animal models. 18F-PCA may have potential as a PET imaging agent for direct melanoma detection.
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