A chelating derivative of alpha-melanocyte stimulating hormone as a potential imaging agent for malignant melanoma

Br J Cancer. 1990 Dec;62(6):919-22. doi: 10.1038/bjc.1990.409.

Abstract

A chelating derivative of alpha-melanocyte stimulating hormone (MSH) has been synthesised, in which two molecules of the hormone are cross-linked by diethylenetriamine pentaacetic acid (DTPA). This compound, bisMSH-DTPA, was equipotent with MSH in an in vitro tyrosinase assay with Cloudman S91 melanoma cells. When DBA/2 mice bearing the same tumour were injected with bisMSH-DTPA labelled with the gamma-emitting isotope indium-111 (111In), the radioactivity became rapidly associated with the melanoma tissue. By 24 h post-injection, radioactivity in tumour tissue was significantly higher (P less than 0.001) than in spleen, lung, brain, eye and skin. Uptake of radioactivity by the tumours was inhibited by a 200-fold molar excess of MSH, whereas uptake by liver, kidney, spleen, lung, brain, eye and skin was unaffected. We conclude that bisMSH-DTPA may offer an alternative to antibody targeting in the imaging of malignant melanoma.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Drug Stability
  • Indium Radioisotopes*
  • Melanocyte-Stimulating Hormones* / analogs & derivatives
  • Melanocyte-Stimulating Hormones* / pharmacokinetics
  • Melanoma / diagnostic imaging*
  • Mice
  • Mice, Inbred DBA
  • Pentetic Acid*
  • Radionuclide Imaging
  • Tissue Distribution

Substances

  • Indium Radioisotopes
  • Pentetic Acid
  • Melanocyte-Stimulating Hormones