Fluorine-18-labeled [Nle4,D-Phe7]-alpha-MSH, an alpha-melanocyte stimulating hormone analogue.

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.

• Authors: G Vaidyanathan, M R Zalutsky
• Journal: Nuclear medicine and biology (Nucl Med Biol) Vol. 24 Issue 2 Pg. 171-8 (Feb 1997) ISSN: 0969-8051 [Print] United States
• PMID: 9089709 (Publication Type: Comparative Study, Journal Article, Research Support, U.S. Gov't, Non-P.H.S.)

Chemical References

• Fluorine Radioisotopes
• Iodine Radioisotopes
• MSH, alpha, 4-fluorobenzoyl-Nle(4)-Phe(7)-
• Receptors, Pituitary Hormone
• alpha-MSH
• MSH, 4-Nle-7-Phe-alpha-
• MSH receptor
• Melanocyte-Stimulating Hormones

Topics

• Animals
• Binding, Competitive
• Fluorine Radioisotopes (pharmacokinetics)
• Iodine Radioisotopes (pharmacokinetics)
• Kinetics
• Melanocyte-Stimulating Hormones (chemical synthesis, pharmacokinetics)
• Melanoma, Experimental (metabolism)
• Metabolic Clearance Rate
• Mice
• Mice, Inbred BALB C
• Receptors, Pituitary Hormone (metabolism)
• Tissue Distribution
• alpha-MSH (analogs & derivatives, pharmacokinetics)