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Bioorg Med Chem Lett ; 96: 129528, 2023 11 15.
Artigo em Inglês | MEDLINE | ID: mdl-37852422

RESUMO

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.


Assuntos
Melanoma , Neoplasias Cutâneas , Animais , Camundongos , Humanos , Procainamida , Melanoma/diagnóstico por imagem , Melanoma/patologia , Tomografia por Emissão de Pósitrons/métodos , Compostos Radiofarmacêuticos , Linhagem Celular Tumoral , Radioisótopos de Flúor , Melanoma Maligno Cutâneo
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