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.
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 |
| 6347 | PF 04628935New |
| Potent ghrelin receptor inverse agonist | |
Antagonists |
|
| Cat No | Product Name / Activity |
| 1922 | [D-Lys3]-GHRP-6 |
| Ghrelin receptor antagonist | |
| 5830 | K-(D-1-Nal)-FwLL-NH2 |
| High affinity and potent ghrelin receptor inverse agonist | |
| 1946 | [D-Arg1,D-Phe5,D-Trp7,9,Leu11]-Substance P |
| Potent ghrelin receptor full inverse agonist and antagonist at other neuropeptide receptors; anticancer in vitro | |
| 3959 | YIL 781 |
| 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 | |
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
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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.
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Our Peptides Involved in Appetite Modulation review gives an overview of the peptides implicated in appetite regulation and energy homeostasis.
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