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.

More Information and Gene Data »

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
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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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