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Rapid radiosynthesis of two [ 18 F]-labeled nicotinamide derivatives for malignant melanoma imaging.
- Source :
-
Applied radiation and isotopes : including data, instrumentation and methods for use in agriculture, industry and medicine [Appl Radiat Isot] 2018 Feb; Vol. 132, pp. 142-146. Date of Electronic Publication: 2017 Dec 05. - Publication Year :
- 2018
-
Abstract
- The rapid synthesis of two radiofluoronicotinamide derivatives, namely, [ <superscript>18</superscript> F]MEL050 and [ <superscript>18</superscript> F]MEL-2F has been simply performed starting from commercial materials. [ <superscript>18</superscript> F]MEL-2F is a new, potential analogue PET-probe for melanoma imaging. [ <superscript>18</superscript> F]MEL050 is already an excellent PET imaging probe for early specific diagnosis. The synthesis involves coupling step to obtain the precursor followed by radiofluorination. During the synthesis of the precursors different coupling reagents, such as HBTU, TFFH, HOBT, COMU and PyCIU have been applied. PyClU was found the best to reduce the coupling period to < 1h. The labeled compounds were isolated and purified by HPLC. In the in-vitro study three kinds of cells, namely, Melur (melanin free), KB-3 carcinoma cell line (non-melanoma) and B16-F10 melanoma cell line were used to evaluate the uptake of the radiotracers.<br /> (Copyright © 2017 Elsevier Ltd. All rights reserved.)
- Subjects :
- Animals
Carbon-13 Magnetic Resonance Spectroscopy
Cell Line, Tumor
Chromatography, High Pressure Liquid
Fluorine Radioisotopes pharmacokinetics
Indicators and Reagents chemistry
Mass Spectrometry
Melanoma, Experimental metabolism
Melanoma, Experimental pathology
Mice
Niacinamide chemistry
Niacinamide pharmacokinetics
Proton Magnetic Resonance Spectroscopy
Radiopharmaceuticals pharmacokinetics
Fluorine Radioisotopes chemistry
Melanoma, Experimental diagnostic imaging
Niacinamide chemical synthesis
Radiopharmaceuticals chemistry
Subjects
Details
- Language :
- English
- ISSN :
- 1872-9800
- Volume :
- 132
- Database :
- MEDLINE
- Journal :
- Applied radiation and isotopes : including data, instrumentation and methods for use in agriculture, industry and medicine
- Publication Type :
- Academic Journal
- Accession number :
- 29227835
- Full Text :
- https://doi.org/10.1016/j.apradiso.2017.12.004