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Ghrelin Receptors

Ghrelin is the endogenous ligand for the ghrelin receptor, also known as the growth hormone secretagog receptor (GHS-R1a). Alternative splicing of preproghrelin yields two active peptides: ghrelin and des-Gln14-ghrelin, which differ by the deletion of one amino acid.

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Products
Background
Literature (3)
Gene Data

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
5272 MK 0677
High affinity ghrelin receptor agonist
2308 Tabimorelin hemifumarate
Potent, orally active ghrelin receptor agonist

Inverse Agonists
Cat. No. Product Name / Activity
5830 K-(D-1-Nal)-FwLL-NH2
High affinity and potent ghrelin receptor inverse agonist
6347 PF 04628935
Potent ghrelin receptor inverse agonist
6350 PF 05190457
High affinity and selective ghrelin receptor inverse agonist
1946 [D-Arg1,D-Phe5,D-Trp7,9,Leu11]-Substance P
Potent ghrelin receptor inverse agonist; Antagonist at other neuropeptide receptors

Antagonists
Cat. No. Product Name / Activity
1922 [D-Lys3]-GHRP-6
Ghrelin receptor antagonist
3959 YIL 781 hydrochloride
Ghrelin receptor (GHS-R1a) antagonist

Other
Cat. No. Product Name / Activity
3374 Cortistatin 14
Endogenous neuropeptide; binds ghrelin receptor 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
5560 Obestatin (human)
Endogenous anorexigenic peptide; opposes actions of ghrelin
2445 Obestatin (rat)
Endogenous anorexigenic peptide; opposes actions of ghrelin

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.

External sources of pharmacological information for Ghrelin Receptors :

Literature for Ghrelin Receptors

Tocris offers the following scientific literature for Ghrelin Receptors to showcase our products. We invite you to request* your copy today!

*Please note that Tocris will only send literature to established scientific business / institute addresses.

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Peptides Involved in Appetite Modulation Scientific Review

Written by Sonia Tucci, Lynsay Kobelis and Tim Kirkham, this review provides a synopsis of the increasing number of peptides that have been implicated in appetite regulation and energy homeostasis; putative roles of the major peptides are outlined and compounds available from Tocris are listed.

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