Melanin concentrating hormone analogues: Contraction of the cyclic structure. II. Antagonist activity

Michal Lebi, Victor J Hruby, Ana M. Ana, Mac E. Hadley

Research output: Contribution to journalArticle

16 Citations (Scopus)

Abstract

Asp-Thr-Met-Arg-Cys-Met-Val-Gly-Arg-Val-Tyr-Arg-Pro-Cys-Trp-Glu-Val, melanin concentrating hormone (MCH), is a cyclic hormone possessing both MCH-like (melanin granule aggregating effect) and melanocyte stimulating hormone (MSH)-like (melanin granule dispersing effect) activities. Nine ring-contracted analogues were synthesized and characterized for their melanotropic activity on the fish (Synbranchus marmoratus) and frog (Rana pipiens) bioassays. In most cases, these analogues were totally devoid of MCH-like agonist activity, demonstrating the essential role of the disulfide bridge between residues 5 and 14 of the hormone. [Ala5, Cys10]MCH, for example, was totally devoid of MCH-like activity. This analogue, like α-MSH, however, antagonized the melanosome aggregating actions of MCH on fish melanocytes. The antagonistic activity of the analogue, like that of α-MSH, was Ca2+-dependent. Evidence suggested that this antagonism of MCH activity was related to the intrinsic MSH-like activity of the analogue. These results suggest that MCH and α-MSH may be structurally and, therefore, evolutionarily related.

Original languageEnglish (US)
Pages (from-to)451-457
Number of pages7
JournalLife Sciences
Volume44
Issue number7
DOIs
StatePublished - 1989

Fingerprint

Melanocyte-Stimulating Hormones
Melanins
Fish
Fishes
Hormones
Rana pipiens
Melanosomes
melanin-concentrating hormone
Bioassay
Melanocytes
Disulfides
Biological Assay
Anura

ASJC Scopus subject areas

  • Pharmacology

Cite this

Melanin concentrating hormone analogues : Contraction of the cyclic structure. II. Antagonist activity. / Lebi, Michal; Hruby, Victor J; Ana, Ana M.; Hadley, Mac E.

In: Life Sciences, Vol. 44, No. 7, 1989, p. 451-457.

Research output: Contribution to journalArticle

Lebi, Michal ; Hruby, Victor J ; Ana, Ana M. ; Hadley, Mac E. / Melanin concentrating hormone analogues : Contraction of the cyclic structure. II. Antagonist activity. In: Life Sciences. 1989 ; Vol. 44, No. 7. pp. 451-457.
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