Fluorine-18-labeled [Nle(4),D-Phe(7)]-alpha-MSH, an alpha-melanocyte stimulating hormone analogue

被引：62

作者：

Vaidyanathan, G

Zalutsky, MR

机构：

[1] Box 3808, Department of Radiology, Duke University Medical Center, Durham

来源：

NUCLEAR MEDICINE AND BIOLOGY | 1997年 / 24卷 / 02期

关键词：

fluorine-18; melanocyte; MSH; specific activity;

D O I：

10.1016/S0969-8051(96)00211-9

中图分类号：

R8 [特种医学]; R445 [影像诊断学];

学科分类号：

1002 ; 100207 ; 1009 ;

摘要：

The alpha-melanocyte stimulating hormone (alpha-MSH) analogue [Nle(4),D-Phe(7)]-alpha-MSH was labeled with F-18 using N-succinimidyl 4-[F-18]fluorobenzoate ([F-18]SFB) in >80% radiochemical yield. The IC50 values of [Nle(4),D-Phe(7)]-alpha-MSH and para-fluorobenzoyl-[Nle(4),D-Phe(7)]-alpha-MSH ([Nle(4),D-Phe(7),Lys(11)- (F-18)PFB]-alpha-MSH) for inhibiting the binding of meta-[I-131]iodobenzoyl-[Nle(4),D-Phe(7)]-alpha-MSH-([Nle(4),D- Phe(7),Lys(11)-(I-131)MIB]-alpha-MSH) to B16-F1 murine melanoma cells werc 89 +/- 9 pM and 112 +/- 22 pM, respectively, suggesting that addition of 4-fluorobenzoate did not compromise alpha-MSH receptor binding affinity. Binding of [Nle(4),D-Phe(7),Lys(11)-(F-18)PEB]-alpha-MSH was influenced by the specific activity of the preparation (400-1000 Ci/mmol). The normal tissue clearance of [Nle(4),D-Phe(7),Lys(11)-(F-18)PFB]-alpha-MSH in mice was quite rapid, with little evidence for defluorination. (C) 1997 Elsevier Science Inc.

引用

页码：171 / 178

页数：8

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