Ghrelin Receptors

Supporting information

Ghrelin is the endogenous ligand for the ghrelin receptor, also known as the growth hormone secretagog receptor (GHS-R1a). Alternative splicing of the preproghrelin yields two active peptides: ghrelin and des-Gln14-ghrelin, which differ by the deletion of one amino acid residue. The predominant form, ghrelin, is highly expressed in endocrine cells of the stomach, with low levels also found in the hypothalamus.

The G-protein-coupled ghrelin receptor is expressed in the pituitary, hypothalamus, hippocampus, gastrointestinal tract and the vasculature including the aorta, coronary arteries, pulmonary arteries, arcuate arteries, and saphenous veins. Ghrelin potently stimulates the release of growth hormone from the anterior pituitary. Ghrelin is thought to act on ghrelin receptors present on pituitary somatotrophs and on growth hormone-releasing hormone (GHRH) positive cells in the hypothalamus triggering GHRH release. The peptide also acts as a potent vasodilator in vivo and in vitro.

Ghrelin peptide was the first circulating hormone shown to stimulate eating and weight gain. In humans circulating ghrelin levels are decreased in acute states of positive energy balance and obesity, and are elevated during weight loss induced by sustained fasting and anorexia nervosa. The development of ghrelin antagonists, or a means to inhibit ghrelin release may be an important pharmaceutical goal for the management of obesity.

To view external sources of pharmacological information for Ghrelin Receptors, please click here: IUPHAR Receptor Code and BJP Guide

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Species Gene Symbol Gene Accession No. Protein Accession No.
Human GHSR NM_004122 Q92847
Mouse Ghsr NM_177330 Q99P50
Rat Ghsr NM_032075 O08725

Literature for Ghrelin Receptors

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