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  • Title: Fluorine-18-labeled [Nle4,D-Phe7]-alpha-MSH, an alpha-melanocyte stimulating hormone analogue.
    Author: Vaidyanathan G, Zalutsky MR.
    Journal: Nucl Med Biol; 1997 Feb; 24(2):171-8. PubMed ID: 9089709.
    Abstract:
    The alpha-melanocyte stimulating hormone (alpha-MSH) analogue [Nle4,D-Phe7]-alpha-MSH was labeled with 18F using N-succinimidyl 4-[18F]fluorobenzoate ([18F]SFB) in > 80% radiochemical yield. The IC50 values of [Nle4,D-Phe7]-alpha-MSH and para-fluorobenzoyl-[Nle4, D-Phe7]-alpha-MSH ([Nle4,D-Phe7, Lys 11 -(18F)PFB]-alpha-MSH) for inhibiting the binding of meta-[131I]iodobenzoyl -[Nle4,D-Phe7]-alpha-MSH ([Nle4,D-Phe7, Lys11-(131I)MIB]-alpha-MSH) to B16-F1 murine melanoma cells were 89 +/- 9 pM and 112 +/- 22 pM, respectively, suggesting that addition of 4-fluorobenzoate did not compromise alpha-MSH receptor binding affinity. Binding of [Nle4,D-Phe7,Lys11-(18F)PFB]-alpha-MSH was influenced by the specific activity of the preparation (400-1000 Ci/mmol). The normal tissue clearance of [Nle4, D-Phe7, Lys11-(18F) PFB]-alpha-MSH in mice was quite rapid, with little evidence for defluorination.
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