Biologic activities of growth hormone secretagogues in humans

Biologic activities of growth hormone secretagogues in humans / E. Ghigo, E. Arvat, R. Giordano, F. Broglio, L. Gianotti, M. Maccario, G. Bisi, A. Graziani, M. Papotti, G. Muccioli, R. Deghenghi, F. Camanni

  • Endocrine 14 (2001) 1 (Feb); p. 87-93
  • PMID: 11322506
  • DOI: 10.1385/ENDO:14:1:087


Growth hormone secretagogues (GHSs) are synthetic peptidyl and nonpeptidyl molecules with strong, dose-dependent, and reproducible growth hormone (GH)-releasing activity even after oral administration. GHSs release GH via actions on specific receptors (GHS-R) at the pituitary and, mainly, at the hypothalamic levels. GHSs likely act as functional somatostatin antagonists and meantime enhance the activity of GH-releasing hormone (GHRH)-secreting neurons. The GH-releasing effect of GHSs is independent of gender but undergoes marked age-related variations. Estrogens play a major role in enhancing the GH response to GHSs at puberty, which GHRH hypoactivity, somatostatinergic hyperactivity and impaired activity of the putative GHS-like ligand and receptors probably explain the reduced GH-releasing effect of GHSs in aging. The activity of GHSs is not fully specific for GH. Their slight prolactin-releasing activity probably comes from direct pituitary action. In physiological conditions, the ACTH-releasing activity of GHSs is dependent on central actions; a direct action on GHS-R in pituitary ACTH-secreting tumors likely explains the peculiar ACTH and cortisol hyperresponsiveness to GHSs in Cushing disease. GHSs have specific receptor subtypes in other central and peripheral endocrine and nonendocrine tissues mediating GH-independent biologic activities. GHSs influence sleep pattern, stimulate food intake, and have cardiovascular activities. GHs have specific binding in normal and neoplastic follicular derived human thyroid tissue and inhibit the proliferation of follicular-derived neoplastic cell lines. The discovery of ghrelin, a 28 amino acid peptide synthesized in the stomach but also in other tissues, has opened new fascinating perspectives of research in this field.

Original document


1 February 2001
Arvat, Emanuela
Bisi, G.
Broglio, Fabio
Camanni, Franco
Deghenghi, Romano
Ghigo, Ezio
Gianotti, L.
Giordano, Roberta
Graziani, A.
Maccario, Mauro
Muccioli, Giampiero
Papotti, Mauro
Other organisations
Università degli Studi di Torino (UNITO) - University of Turin
Doping classes
S2. Peptide Hormones, Growth Factors
Growth Hormone Secretagogues (GHS)
Growth hormone-releasing hormone (GHRH)
Medical terms
Health effects
Document category
Scientific article
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Pdf file
Date generated
8 December 2021
Date of last modification
24 January 2022
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