Abstract
Binding and stimulation of cAMP by the melanotropin peptides alpha-MSH (alpha-melanocyte-stimulating hormone) and its superpotent analogues [Nle4, DPhe7]alpha-MSH (MT-I) and Ac-[Nle4,[formula: see text]alpha-MSH4-10-NH2 (MT-II) were undertaken to examine their respective properties on the human peripheral melanocyte melanocortin receptor, hMC1R. alpha-MSH was found to possess a binding IC50 value of 6.5 +/- 0.9 x 10(-9) M and cAMP EC50 value of 2.0 +/- 0.6 x 10(-9) M. MT-I possesses a binding IC50 value of 1.2 +/- 0.3 x 10(-9) M and a cAMP EC50 of 0.5 +/- 0.03 x 10(-9) M. MT-II possesses a binding IC50 of 0.57 +/- 0.08 x 10(-9) M and cAMP EC50 value of 0.20 +/- 0.05 x 10(-9) M.
Publication types
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Comparative Study
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Research Support, Non-U.S. Gov't
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Research Support, U.S. Gov't, Non-P.H.S.
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Research Support, U.S. Gov't, P.H.S.
MeSH terms
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Affinity Labels
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Amino Acid Sequence
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Animals
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Binding, Competitive
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Biological Assay
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Cloning, Molecular
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Cyclic AMP / metabolism*
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Humans
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Kinetics
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L Cells
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Lizards
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Melanocyte-Stimulating Hormones / pharmacology*
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Melanocytes / metabolism
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Mice
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Molecular Sequence Data
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Peptide Fragments / chemical synthesis
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Peptide Fragments / pharmacology*
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Peptides, Cyclic / pharmacology
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Ranidae
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Receptors, Corticotropin / biosynthesis
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Receptors, Corticotropin / metabolism*
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Receptors, Melanocortin
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Recombinant Proteins / biosynthesis
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Recombinant Proteins / metabolism
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Skin / drug effects
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Skin Physiological Phenomena
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Structure-Activity Relationship
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Transfection
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alpha-MSH / analogs & derivatives
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alpha-MSH / metabolism
Substances
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Affinity Labels
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Peptide Fragments
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Peptides, Cyclic
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Receptors, Corticotropin
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Receptors, Melanocortin
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Recombinant Proteins
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alpha-MSH
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MSH, 4-Nle-7-Phe-alpha-
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Melanocyte-Stimulating Hormones
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Cyclic AMP