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Cited by 40Neuropeptides and Animal PhysiologyCardiovascular, Neuropeptides, and Oxidative Stress ResearchChemical Synthesis and Analysis

Cardiovascular effects of γ-MSH/ACTH-like peptides: structure-activity relationship

Van Bergen, Patricia, Janssen, Paul M.L., Hoogerhout, Peter, De Wildt, Dick J., Versteeg, Dirk H.G.·1995·European Journal of Pharmacology
DOI 10.1016/0014-2999(95)00657-5
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Abstract

Intravenous administration of gamma2-melanocyte-stimulating hormone (gamma2-MSH) to conscious rats causes a dose-dependent increase in blood pressure and heart rate, while the structurally related peptide adrenocorticotropic hormone-(4-10) (ACTH-(4-10)) is 5-10 times less potent in this respect. This prompted us to investigate which amino acid sequence is determinant for the cardiovascular selectivity of peptides of the gamma-MSH family. Lys-gamma2-MSH, most likely the endogenously occurring gamma-MSH analog, was as potent as gamma2-MSH in inducing increases in blood pressure and heart rate. Removal of C-terminal amino acids resulted in gamma-MSH-fragments which were devoid of cardiovascular activities. Removal of amino acids from the N-terminal side of gamma2-MSH resulted in fragments which were less potent, but had an intrinsic activity not different from that of gamma-MSH. Surprisingly, gamma-MSH-(6-12) was more potent than gamma2-MSH. The shortest fragment which displayed pressor and tachycardiac responses was the MSH 'core', His-Phe-Arg-Trp (= gamma-MSH-(5-8)), which is identical to ACTH-(6-9). This was corroborated by testing fragments of ACTH-(4-10). We conclude that the message essential for cardiovascular effects resides in the gamma-MSH-(5-8)/ACTH-(6-9) sequence. Proper C-terminal elongation is required for full expression of cardiovascular activity of gamma2-MSH, as the sequence of Asp9-Arg10-Phe11 appears to play an important role in establishing intrinsic activity. The amino acids N-terminal to the MSH 'core' sequence appear to be essential for the potency of the peptides.

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Crossref · 10.1016/0014-2999(95)00657-5

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  • The Arg-Phe sequence in γ-MSH is critical for its acute hypertensive actions since synthetic analog peptides lacking this sequence do not raise blood pressure.

    “The Arg-Phe sequence in γ-MSH is critical for its acute hypertensive actions since synthetic analog peptides lacking this sequence do not raise BP [16, 17].”

    From Role of the brain melanocortins in blood pressure regulation (2017) · cites this paper as [17]

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Authors
Van Bergen, P., Janssen, P. M. L., Hoogerhout, P., De Wildt, D. J., & Versteeg, D. H. G.
Affiliations
  • Utrecht University (NL)
  • National Institute for Public Health and the Environment (NL)
ORCID
Janssen, Paul M.L.
Venue
European Journal of Pharmacology
Publisher
Elsevier BV
Published
1995-12
Volume
294
Issue
2-3
Pages
795-803
ISSN
0014-2999 (ISSN-L)
DOI
10.1016/0014-2999(95)00657-5
OpenAlex
W2069526769
Cited by
40
References
25
Citations by year
2026: 1 · 2017: 1 · 2015: 2 · 2013: 1 · 2012: 1
FWCI
1.20
Type
journal article
Language
en
Open access
closed
Licence
www.elsevier.com/tdm/userlicense/1.0/ (tdm)
Locations
  • European Journal of Pharmacology (publishedVersion)
  • PubMed (publishedVersion)
  • Rivm (National Institute for Public Health and the Environment) (submittedVersion)
Funders
Universiteit Utrecht
Topics
  • Life Sciences › Neuroscience › Cellular and Molecular Neuroscience › Neuropeptides and Animal Physiology
  • Health Sciences › Medicine › Surgery › Cardiovascular, Neuropeptides, and Oxidative Stress Research
  • Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › Chemical Synthesis and Analysis
Keywords
gamma-MSH, ACTH4-10, structure-activity relationship, cardiovascular effects, blood pressure, heart rate, C-terminal amino acids, N-terminal amino acids, peptide fragments, pressor activity
MeSH terms
Adrenocorticotropic Hormone, Amino Acid Sequence, Animals, Blood Pressure, Dose-Response Relationship, Drug, Heart Rate, Male, Molecular Sequence Data, Melanocyte-Stimulating Hormones, Peptide Fragments, Structure-Activity Relationship, Rats, Wistar, Receptors, Corticotropin, Receptors, Melanocortin, Rats

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