Synthesis of tritium labeled Ac-[Nle4, D-Phe7]-α-MSH4-11-NH2: A superpotent melanotropin with prolonged biological activity

Brian C. Wilkes, Victor J. Hruby, Henry I. Yamamura, Kazufumi Akiyama, Ana Marie de L. Castrucci, Mac E. Hadley, Joseph R. Andrews, Y. P. Wan

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15 Scopus citations

Abstract

Ac-[Nle4, D-Phe7]-α-MSH4-11-NH2 an octapeptide, is a melantropin analogue (Ac-Nle-Glu-His-D-Phe-Arg-Trp-Gly-Lys-NH2), which is a superpotent agonist of frog and lizard skin melanocytes and mouse S 91 (Cloudman) melanoma cells. This malanotropin possesses ultraprolonged activity on melanocytes, both in vitro and in vivo, and the peptide is resistant to inactivation by serum enzymes. The tritiumlabeled congener was prepared by direct incorporation of [3H]-labeled norleucine into the peptide. The melanotropic activity of the labeled peptide is identical to the unlabeled analogue. This labeled peptide should be useful for studies on the localization and characterization of melanotropin receptors.

Original languageEnglish (US)
Pages (from-to)977-984
Number of pages8
JournalLife Sciences
Volume34
Issue number10
DOIs
StatePublished - Mar 5 1984

ASJC Scopus subject areas

  • Biochemistry, Genetics and Molecular Biology(all)
  • Pharmacology, Toxicology and Pharmaceutics(all)

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    Wilkes, B. C., Hruby, V. J., Yamamura, H. I., Akiyama, K., Castrucci, A. M. D. L., Hadley, M. E., Andrews, J. R., & Wan, Y. P. (1984). Synthesis of tritium labeled Ac-[Nle4, D-Phe7]-α-MSH4-11-NH2: A superpotent melanotropin with prolonged biological activity. Life Sciences, 34(10), 977-984. https://doi.org/10.1016/0024-3205(84)90302-3