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Endocrine Reviews 25 (3): 426-457
Copyright © 2004 by The Endocrine Society

Biological, Physiological, Pathophysiological, and Pharmacological Aspects of Ghrelin

Aart J. van der Lely, Matthias Tschöp, Mark L. Heiman and Ezio Ghigo

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; Endocrine Research Department (M.L.H.), Eli Lilly and Co., Indianapolis, Indiana 46285; and Division of Endocrinology (E.G.), Department of Internal Medicine, University of Turin, Turin, Italy 10095

Correspondence: Address all correspondence and requests for reprints to: Aart Jan van der Lely, M.D., Department of Internal Medicine, Erasmus Medical Center, 40 Dr. Molewaterplein, 3015 GD Rotterdam, The Netherlands. E-mail: a.vanderlelij{at}erasmusmc.nl

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. C. Martini, R. Fernandez-Fernandez, S. Tovar, V. M. Navarro, E. Vigo, M. J. Vazquez, J. S. Davies, N. M. Thompson, E. Aguilar, L. Pinilla, et al.
Comparative Analysis of the Effects of Ghrelin and Unacylated Ghrelin on Luteinizing Hormone Secretion in Male Rats
Endocrinology, May 1, 2006; 147(5): 2374 - 2382.
[Abstract] [Full Text] [PDF]

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 J. Gerontol. A Biol. Sci. Med. Sci.Home page
A. E. Rigamonti, S. M. Bonomo, D. Scanniffio, S. G. Cella, and E. E. Muller
Orexigenic effects of a growth hormone secretagogue and nitric oxide in aged rats and dogs: correlation with the hypothalamic expression of some neuropeptidergic/receptorial effectors mediating food intake.
J. Gerontol. A Biol. Sci. Med. Sci., April 1, 2006; 61(4): 315 - 322.
[Abstract] [Full Text] [PDF]