Biological, Physiological, Pathophysiological, and Pharmacological Aspects of Ghrelin
Abstract
Ghrelin is a peptide predominantly produced by the stomach. Ghrelin displays strong GH-releasing activity. This activity is mediated by the activation of the so-called GH secretagogue receptor type 1a. This receptor had been shown to be specific for a family of synthetic, peptidyl and nonpeptidyl GH secretagogues. Apart from a potent GH-releasing action, ghrelin has other activities including stimulation of lactotroph and corticotroph function, influence on the pituitary gonadal axis, stimulation of appetite, control of energy balance, influence on sleep and behavior, control of gastric motility and acid secretion, and influence on pancreatic exocrine and endocrine function as well as on glucose metabolism. Cardiovascular actions and modulation of proliferation of neoplastic cells, as well as of the immune system, are other actions of ghrelin. Therefore, we consider ghrelin a gastrointestinal peptide contributing to the regulation of diverse functions of the gut-brain axis. So, there is indeed a possibility that ghrelin analogs, acting as either agonists or antagonists, might have clinical impact.
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A large body of evidence supports the hypothesis that ghrelin acts on growth hormone secretion, at least in part, via stimulation of GHRH.
“A large body of evidence supports the hypothesis that ghrelin acts on GH secretion, at least in part, via a stimulation of GHRH [39, 50, 192]”
From Sleep and metabolic function (2012) · cites this paper as [192]
Leptin secretion is inhibited by sympathetic activity and ghrelin secretion is inhibited by parasympathetic activity.
“Since leptin secretion is inhibited by sympathetic activity [65] and ghrelin secretion is inhibited by parasympathetic activity [66], the changes in the activity of autonomic nervous system observed with sleep loss may be involved in the simultaneous reduction of leptin and increase of ghrelin.”
From Role of sleep duration in the regulation of glucose metabolism and appetite (2010) · cites this paper as [66]
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MethodInfluentialGhrelin promotes slow-wave sleep in humans
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Self-citationIdentification and Characterization of a Novel Human Cortistatin-like Peptide
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Ghrelin drives GH secretion during fasting in man
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Self-citationAnti-cachectic effect of ghrelin in nude mice bearing human melanoma cells
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Stimulatory Effects of Ghrelin on Circulating Somatostatin and Pancreatic Polypeptide Levels
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Ghrelin Can Bind to a Species of High Density Lipoprotein Associated with Paraoxonase
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Cortistatin Is Expressed in a Distinct Subset of Cortical Interneurons
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Ghrelin Expression in Fetal, Infant, and Adult Human Lung
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Growth Hormone-Independent Cardioprotective Effects of Hexarelin in the Rat1
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Ghrelin immunoreactivity in human plasma is suppressed by somatostatin
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Self-citationIdentification of a new G-protein-linked receptor for growth hormone secretagogues
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Enhanced leptin transport across the blood–brain barrier by α1-adrenergic agents
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Taheri, S., Lin, L., Austin, D., Young, T., & Mignot, E. (2004) · PLoS Medicine · doi:10.1371/journal.pmed.0010062 · Cited by 2,477 · see citing works
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Expression of ghrelin receptor mRNA in the rat and the mouse brain
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Self-citation<i>Associations between Sleep Loss and Increased Risk of Obesity and Diabetes</i>
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Central Fibroblast Growth Factor 21 Browns White Fat via Sympathetic Action in Male Mice
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Morselli, L. L., Guyon, A., & Spiegel, K. (2012) · Pflügers Archiv - European Journal of Physiology · doi:10.1007/s00424-011-1053-z · Cited by 199 · see citing works
“A large body of evidence supports the hypothesis that ghrelin acts on GH secretion, at least in part, via a stimulation of GHRH [39, 50, 192]: A positive interaction between central ghrelinergic activity and sleep, in particular SWS, should therefore be expected.”
Roles of ghrelin and leptin in the control of reproductive function
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Self-citationRegulation of Gastrointestinal Motility by Motilin and Ghrelin in Vertebrates
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Endogenous Circulating Ghrelin Does Not Mediate Growth Hormone Rhythmicity or Response to Fasting
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Arabinoxylan-enriched meal increases serum ghrelin levels in healthy humans
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Acylation, a Conductor of Ghrelin Function in Brain Health and Disease
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- Authors
- van der Lely, A. J., Tschöp, M., Heiman, M. L., & Ghigo, E.
- Affiliations
- Division of Endocrinology and Metabolism (A.J.v.d.L.), Department of Internal Medicine, Erasmus Medical Center, 3015 GD Rotterdam, The Netherlands;
- Department of Psychiatry (M.T.), University of Cincinnati, Cincinnati, Ohio 45237;
- Eli Lilly (United States) (US)
- University of Turin (IT)
- Venue
- Endocrine Reviews
- Publisher
- The Endocrine Society
- Published
- 2004-06-01
- Volume
- 25
- Issue
- 3
- Pages
- 426-457
- ISSN
- 0163-769X (ISSN-L)
- 1945-7189
- OpenAlex
- W2109993485
- Cited by
- 1,187
- References
- 502
- Citations by year
- 2026: 6 · 2025: 18 · 2024: 16 · 2023: 14 · 2022: 24 · 2021: 29 · 2020: 31 · 2019: 21 · 2018: 34 · 2017: 39 · 2016: 37 · 2015: 42 · 2014: 69 · 2013: 85 · 2012: 87
- FWCI
- 8.99
- Type
- journal article
- Language
- en
- Open access
- closed
- Locations
- Endocrine Reviews (publishedVersion)
- PubMed (publishedVersion)
- EUR Research Repository (Erasmus University Rotterdam) (publishedVersion)
- EUR Research Repository (Erasmus University Rotterdam) (submittedVersion)
- Topics
- Life Sciences › Neuroscience › Endocrine and Autonomic Systems › Regulation of Appetite and Obesity
- Health Sciences › Medicine › Endocrinology, Diabetes and Metabolism › Growth Hormone and Insulin-like Growth Factors
- Health Sciences › Medicine › Reproductive Medicine › Hypothalamic control of reproductive hormones
- Keywords
- ghrelin, growth hormone secretagogue receptor 1a, growth hormone secretion, appetite regulation, energy balance, gastric motility, gastric acid secretion, glucose metabolism, pituitary-gonadal axis, cardiovascular effects, immunomodulation, gut-brain axis
- MeSH terms
- Amino Acid Sequence, Animals, Appetite Regulation, Cardiovascular System, Clinical Trials as Topic, Digestive System, Energy Metabolism, Gastric Mucosa, Humans, Immune System, Neurosecretory Systems, Peptide Hormones, Receptors, G-Protein-Coupled, Ghrelin, Receptors, Ghrelin
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