Ghrelin Receptors
Ghrelin is the endogenous ligand for the ghrelin receptor, also known as the growth hormone secretagog receptor (GHS-R1a). Alternative splicing of the prepro-ghrelin 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.
- IUPHAR Receptor code: Ghrelin
- BJP Guide: Ghrelin Receptors
Ghrelin Receptors - More Information
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.
Ghrelin Receptor Gene Data
| Species | Gene Symbol | Gene Accession No. | Protein Accession No. |
|---|
| Human | GHSR | NM_004122 | Q92847 |
| Mouse | Ghsr | NM_177330 | Q99P50 |
| Rat | Ghsr | NM_032075 | O08725 |
Ghrelin Receptor Products
Featured Products |
|
Cat.No. |
Product Name / Activity |
| 1463 | Ghrelin (human) |
| Endogenous ghrelin receptor agonist | |
| 1465 | Ghrelin (rat) |
| Endogenous ghrelin receptor agonist | |
Agonists |
|
Cat.No. |
Product Name / Activity |
| 1463 | Ghrelin (human) |
| Endogenous ghrelin receptor agonist | |
| 1465 | Ghrelin (rat) |
| Endogenous ghrelin receptor agonist | |
| 2261 | L-692,585 |
| Potent, non-peptide ghrelin receptor agonist | |
| 2308 | Tabimorelin hemifumarate |
| Potent, orally active ghrelin receptor agonist | |
Antagonists |
|
Cat.No. |
Product Name / Activity |
| 3033 | Cortistatin-8 |
| Ghrelin receptor antagonist | |
| 1922 | [D-Lys3]-GHRP-6 |
| Ghrelin receptor antagonist | |
| 1946 | [D-Arg1,D-Phe5,D-Trp7,9,Leu11]-Substance P |
| Potent ghrelin receptor full inverse agonist. Also antagonist at other neuropeptide receptors. Anticancer in vitro | |
Other |
|
Cat.No. |
Product Name / Activity |
| 3374 | Cortistatin 14 |
| Endogenous neuropeptide; binds GHS-R1a and sst1 - sst5 | |
| 2951 | [Des-octanoyl]-Ghrelin (rat) |
| Major circulating form of ghrelin; devoid of activity at GHS receptor | |
| 1346 | des-Gln14-Ghrelin (rat) |
| Endogenous ghrelin receptor ligand | |
| 2260 | [Des-octanoyl]-Ghrelin (human) |
| Major circulating form of ghrelin; devoid of activity at ghrelin receptor but is active in vivo | |
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