]-α-MSH, an α-melanocyte stimulating hormone analogue
The α-melanocyte stimulating hormone (α-MSH) analogue [Nle4,D-Phe7]-α-MSH was labeled with 18F using N-succinimidyl 4-[18F]fluorobenzoate ([18F]SFB) in >80% radiochemical yield. The IC50 values of [Nle4,D-Phe7]-α-MSH and para-fluorobenzoyl-[Nle4,D-Phe7]-α-MSH ([Nle4,D-Phe7,Lys11-(18F)PFB]-α-MSH for inhibiting the binding of meta-[131I]iodobenzoyl-[Nle4,D-Phe7]-α-MSH ([Nle4,D-Phe7,Lys11-(131I)MIB]-α-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 α-MSH receptor binding affinity. Binding of [Nle4,D-Phe7,Lys11-(18F)PFB]-α-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]-α-MSH in mice was quite rapid, with little evidence for defluorination.
Vaidyanathan, G; Zalutsky, MR
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