Fluorine-18-labeled [Nle4,D-Phe7]-alpha-MSH, an alpha-melanocyte stimulating hormone analogue.
Journal Article (Journal Article)
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.
Full Text
Duke Authors
Cited Authors
- Vaidyanathan, G; Zalutsky, MR
Published Date
- February 1997
Published In
Volume / Issue
- 24 / 2
Start / End Page
- 171 - 178
PubMed ID
- 9089709
International Standard Serial Number (ISSN)
- 0969-8051
Digital Object Identifier (DOI)
- 10.1016/s0969-8051(96)00211-9
Language
- eng
Conference Location
- United States