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

Research output: Contribution to journalArticle

15 Citations (Scopus)

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

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Melanocyte-Stimulating Hormones
Tritium
Bioactivity
Peptides
Melanocytes
Norleucine
Lizards
Anura
Melanoma
Skin
Enzymes
Serum

ASJC Scopus subject areas

  • Pharmacology

Cite this

Synthesis of tritium labeled Ac-[Nle4, D-Phe7]-α-MSH4-11-NH2 : A superpotent melanotropin with prolonged biological activity. / Wilkes, Brian C.; Hruby, Victor J; Yamamura, Henry I.; Akiyama, Kazufumi; Castrucci, Ana Marie de L; Hadley, Mac E.; Andrews, Joseph R.; Wan, Y. P.

In: Life Sciences, Vol. 34, No. 10, 05.03.1984, p. 977-984.

Research output: Contribution to journalArticle

Wilkes, BC, Hruby, VJ, Yamamura, HI, Akiyama, K, Castrucci, AMDL, Hadley, ME, Andrews, JR & Wan, YP 1984, 'Synthesis of tritium labeled Ac-[Nle4, D-Phe7]-α-MSH4-11-NH2: A superpotent melanotropin with prolonged biological activity', Life Sciences, vol. 34, no. 10, pp. 977-984. https://doi.org/10.1016/0024-3205(84)90302-3
Wilkes, Brian C. ; Hruby, Victor J ; Yamamura, Henry I. ; Akiyama, Kazufumi ; Castrucci, Ana Marie de L ; Hadley, Mac E. ; Andrews, Joseph R. ; Wan, Y. P. / Synthesis of tritium labeled Ac-[Nle4, D-Phe7]-α-MSH4-11-NH2 : A superpotent melanotropin with prolonged biological activity. In: Life Sciences. 1984 ; Vol. 34, No. 10. pp. 977-984.
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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.",
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AU - Akiyama, Kazufumi

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AU - Andrews, Joseph R.

AU - Wan, Y. P.

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