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*  GHRP-6
... the hormone ghrelin is now considered the receptor's natural endogenous ligand, and it has been renamed as the ghrelin receptor ... This receptor was originally called the growth hormone secretagogue receptor (GHSR), but due to subsequent discoveries, ... "Design and characterization of a fluorescent ghrelin analog for imaging the growth hormone secretagogue receptor 1a". ... Therefore, these GHSR agonists act as synthetic ghrelin mimetics. It has been discovered that when GHRP-6 and insulin are ...
*  Growth hormone
... ghrelin through binding to growth hormone secretagogue receptors (GHSR) sex hormonesincreased androgen secretion during puberty ... Thus, GH exerts some of its effects by binding to receptors on target cells, where it activates the MAPK/ERK pathway. Through ... Yi S, Bernat B, Pál G, Kossiakoff A, Li WH (July 2002). "Functional promiscuity of squirrel monkey growth hormone receptor ... Lin-Su K, Wajnrajch MP (December 2002). "Growth Hormone Releasing Hormone (GHRH) and the GHRH Receptor". Rev Endocr Metab ...
*  Ipamorelin
Moulin, Aline; Ryan, Joanne; Martinez, Jean; Fehrentz, Jean-Alain (2007). "Recent Developments in Ghrelin Receptor Ligands". ... is a peptide selective agonist of the ghrelin/growth hormone secretagogue receptor (GHS) and a growth hormone secretagogue. It ... proof-of-concept study of the Ghrelin mimetic ipamorelin for the management of postoperative ileus in bowel resection patients ...
*  Examorelin
... but mimic ghrelin by acting as agonists at the ghrelin receptor. Examorelin substantially and dose-dependently increases plasma ... 117-. ISBN 978-94-011-4439-1. Moulin A, Ryan J, Martinez J, Fehrentz JA (2007). "Recent developments in ghrelin receptor ... Carpino, Philip A (2002). "Recent developments in ghrelin receptor (GHS)". Expert Opin. Ther. Patents. Informa Healthcare. 12 ( ... and highly selective agonist of the ghrelin/growth hormone secretagogue receptor (GHSR) and a growth hormone secretagogue which ...
*  Ghrelin
The receptor for ghrelin, the ghrelin/growth hormone secretagogue receptor (GHS-R), is found on the same cells in the brain as ... Ghrelin was discovered after the ghrelin receptor (called growth hormone secretagogue type 1A receptor or GHS-R) was discovered ... The ghrelin receptor GHS-R1a (a splice-variant of the growth hormone secretagogue receptor, with the GHS-R1b splice being ... Ghrelin was found to be upregulated by stress even in the absence of adrenal hormones. Blocking the ghrelin receptor during ...
*  Ulimorelin
Pharmacological demarcation of the growth hormone, gut motility and feeding effects of ghrelin using a novel ghrelin receptor ... Analysis of the ghrelin receptor-independent vascular actions of ulimorelin. Eur J Pharmacol. 2015 Apr 5;752:34-9. doi: 10.1016 ... Ghrelin and motilin receptor agonists: time to introduce bias into drug design. Neurogastroenterol Motil. 2014 Feb;26(2):149-55 ... Optimization of the potency and pharmacokinetic properties of a macrocyclic ghrelin receptor agonist (Part I): Development of ...
*  Growth hormone secretagogue receptor
... (GHS-R), also known as ghrelin receptor, is a G protein-coupled receptor that binds growth ... dopamine receptor type 2 (DRD2), melanocortin-3 receptor (MC3R), and serotonin receptor type 2C (5-HT2c receptor). See " ... "Ghrelin Receptor". IUPHAR Database of Receptors and Ion Channels. International Union of Basic and Clinical Pharmacology. ... Building on this, it was found that there are growth hormone secretagogue receptors in the VTA and that ghrelin acts on the VTA ...
*  Cyril Y. Bowers
... ghrelin receptor antagonists for overnutrition, i.e., obesity; 3) use of ghrelin agonists in diabetes; 4) use of ghrelin ... Bowers' current and future objectives include development of 1) ghrelin receptor agonists for undernutrition, i.e., cancer, ... A New Obesity Related Peptide Unnatural Growth Hormone-Releasing Peptide Begets Natural Ghrelin Octanoyl Ghrelin Is ... In: Ghrelin, Ghigo E, ed, Klerwer Academic Publishers, Boston/London; 2004, pg 1-13. 21. Iranmanesh A, Bowers CY, Veldhuis JD. ...
*  Pralmorelin
It acts as a ghrelin/growth hormone secretagogue receptor (GHSR) agonist, and was the first of this class of drugs to be ... Moulin, Aline; Brunel, Luc; Verdie, Pascal; Gavara, Laurent; Martinez, Jean; Fehrentz, Jean-Alain (2014). "Ghrelin Receptor ... "Ghrelin". Molecular Metabolism. 4 (6): 437-460. doi:10.1016/j.molmet.2015.03.005. ISSN 2212-8778. ...
*  Neurotensin receptor 2
"Common structural basis for constitutive activity of the ghrelin receptor family". The Journal of Biological Chemistry. 279 (51 ... However, unlike NT1 receptor, this gene recognizes, with high affinity, levocabastine, a histamine H1 receptor antagonist ... "Neurotensin Receptors: NTS2". IUPHAR Database of Receptors and Ion Channels. International Union of Basic and Clinical ... These activities suggest that this receptor may be of physiological importance and that a natural agonist for the receptor may ...
*  GPR39
2005). "Common structural basis for constitutive activity of the ghrelin receptor family". J. Biol. Chem. 279 (51): 53806-17. ... G-protein coupled receptor 39 is a protein that in humans is encoded by the GPR39 gene. GRCh38: Ensembl release 89: ... "Entrez Gene: GPR39 G protein-coupled receptor 39". Popovics P, Stewart AJ (2011). "GPR39: A Zn2+-activated G protein-coupled ... 2006). "Obestatin does not activate orphan G protein-coupled receptor GPR39". Biochem. Biophys. Res. Commun. 351 (1): 21-5. doi ...
*  Ingestive behaviors
Ghrelin antibodies or ghrelin receptor antagonists inhibit eating. Ghrelin also stimulates energy production and signals ... The stomach contains receptors that can detect the presence of nutrients, but there are detectors in the intestines as well, ... 2005). "Ghrelin stimulates appetite, imagination of food, GH, ACTH, and cortisol, but does not affect leptin in normal controls ... CCK is secreted in response to the presence of fats, which are detected in by receptors in the duodenum. Another satiety signal ...
*  Relamorelin
Ghrelin receptor agonist, treatment of constipation, treatment of anorexia nervosa, treatment of diabetic gastroparesis". Drugs ... selective agonist of the ghrelin/growth hormone secretagogue receptor (GHSR) which is under development by Rhythm ... Relamorelin (RM-131): Ghrelin Peptide Agonist: A New Drug Class for the Treatment of GI Functional Disorders - Rhythm ... It is a pentapeptide and an analogue of ghrelin with improved potency and pharmacokinetics. In humans, relamorelin produces ...
*  Macimorelin
... is a growth hormone secretagogue receptor (ghrelin receptor) agonist causing release of growth hormone from the ... Koch, Linda (2013). "Growth hormone in health and disease: Novel ghrelin mimetic is safe and effective as a GH stimulation test ...
*  Ibutamoren
PMID 11238495 Smith RG, Sun Y, Jiang H, Albarran-Zeckler R, Timchenko N. Ghrelin receptor (GHS-R1A) agonists show potential as ... and non-peptide agonist of the ghrelin receptor and a growth hormone secretagogue, mimicking the growth hormone (GH)- ... and biological activity of specific receptors for natural (ghrelin) and synthetic growth hormone secretagogues and analogs in ... Small Molecule Agonists and Ago-allosteric Modulators on the Ghrelin Receptor. Molecular Pharmacology. 2008 Oct 15. PMID ...
*  List of growth hormone secretagogues
... gut motility and feeding effects of ghrelin using a novel ghrelin receptor agonist". Endocrinology. 149 (12): 6280-8. doi: ... SM-130686 Note that while ulimorelin is a ghrelin receptor agonist, it is not a GHS as it is peripherally selective and has ... Ghrelin (GHRL) GHRP-1 GHRP-3 GHRP-4 GHRP-5 GHRP-6 (SKF-110679) Ipamorelin (NNC 26-0161) Lenomorelin Pralmorelin (GHRP-2) (GHRP ...
*  Anamorelin
... selective agonist of the ghrelin/growth hormone secretagogue receptor (GHSR) with appetite-enhancing and anabolic effects which ... pharmacokinetics and safety of the ghrelin receptor agonist anamorelin". Clinical Pharmacology in Drug Development. 4 (2): 112- ... Garcia, José M.; Polvino, William J. (2009). "Pharmacodynamic hormonal effects of anamorelin, a novel oral ghrelin mimetic and ... Garcia, José M.; Friend, John; Allen, Suzan (2012). "Therapeutic potential of anamorelin, a novel, oral ghrelin mimetic, in ...
*  Arcuate nucleus
... of the Hypothalamus Are Decreased in Transgenic Rats Whose Expression of Ghrelin Receptor Is Attenuated: Evidence that Ghrelin ... The role of this population is not known; many neurons in the arcuate nucleus express receptors for ghrelin, but these are ... These neurons express estrogen receptors and also coexpress neurokinin B in female rats. GHRH neurons help to control growth ... These neurons are inhibited by leptin, insulin, and peptide YY and activated by ghrelin. Centrally projecting neurons that ...
*  Agouti-related peptide
Ghrelin has receptors on NPY/AgRP neurons that stimulate the secretion of NPY and AgRP to increase appetite. AgRP is stored in ... The melanocortin receptors, MC3-R and MC4-R, are directly linked to metabolism and body weight control. These receptors are ... Ollmann MM, Wilson BD, Yang YK, Kerns JA, Chen Y, Gantz I, Barsh GS (Oct 1997). "Antagonism of central melanocortin receptors ... AGRP has been demonstrated to be an inverse agonist of melanocortin receptors, to be specific MC3-R and MC4-R. ...
*  Orexigenic
... pregabalin Ghrelin receptor agonists such as anamorelin, GHRP-6, ibutamoren, ipamorelin, and pralmorelin MC4 receptor ... This can be a naturally occurring neuropeptide hormone such as ghrelin, orexin or neuropeptide Y, or a medication which ... Agents with orexigenic effects include the following: 5-HT2C receptor antagonists/inverse agonists - mirtazapine, olanzapine, ... clonidine CB1 receptor agonists (cannabinoids - THC/dronabinol (a component of Cannabis), nabilone Corticosteroids - ...
*  Cachexia
Ghrelin and ghrelin receptor agonist Anabolic catabolic transforming agents such as MT-102 Selective androgen receptor ... Those suffering from the eating disorder anorexia nervosa appear to have high plasma levels of ghrelin. Ghrelin levels are also ... "Active ghrelin levels and active to total ghrelin ratio in cancer-induced cachexia". J. Clin. Endocrinol. Metab. 90 (5): 2920-6 ... NF-κB is a known regulator of the genes that encode cytokines, and cytokine receptors. The increased production of cytokines ...
*  Motilin
Ghrelin stimulates growth hormone secretagogue receptors in the pituitary. These receptors are distinct from the growth hormone ... Growth hormone secretagogue receptors share 52% of their DNA with motilin receptors, and agonists of these receptors, termed ... Because of its ability to stimulate gastric activity, it was named "motilin". Apart from in humans, the motilin receptor has ... ISBN 0-07-022001-8. Kangawa K, Matsuo H, Kojima M, Hosoda H (2001). "Ghrelin: discovery of the natural endogenous ligand for ...
*  Adenosine
... is an endogenous agonist of the ghrelin/growth hormone secretagogue receptor. However, while it is able to increase ... The A1 receptors couple to Gi/o and decreases cAMP levels, while the A2 adenosine receptors couple to Gs, which stimulates ... are G-protein-coupled receptors. The four receptor subtypes are further classified based on their ability to either stimulate ... Activation of A2A receptors produces a constellation of responses that in general can be classified as anti-inflammatory. In ...
*  5-HT receptor
... serotonin reuptake inhibitors modify physiological gastrointestinal motor activities via 5-HT2c receptor and acyl ghrelin". ... 5-hydroxytryptamine receptors or 5-HT receptors, or serotonin receptors, are a group of G protein-coupled receptor and ligand- ... 5-hydroxytryptamine receptors or 5-HT receptors, or serotonin receptors are found in the central and peripheral nervous systems ... A number of receptors were classed as "5-HT1-like" - by 1998 it was being argued that, since these receptors were "a ...
*  Dopamine receptor D2
D1-D2 dopamine receptor heteromer D2-adenosine A2A D2-ghrelin receptor D2sh-TAAR1 The D2 receptor has been shown to form ... UNC9994 The dopamine receptor D2 has been shown to interact with EPB41L1, PPP1R9B and NCS-1. The D2 receptor forms receptor ... The dopamine D2 receptor is the main receptor for most antipsychotic drugs. This gene encodes the D2 subtype of the dopamine ... Piribedil - also D3 receptor agonist and α2-adrenergic antagonist Pramipexole - also D3, D4 receptor agonist Quinelorane - ...
*  Basal electrical rhythm
"Inositol 1,4,5-trisphosphate Receptors and Pacemaker Rhythms." Journal of Molecular and Cellular Cardiology 53.3 (2012): 375-81 ... CCK stimulates secretion of PPY and inhibits the secretion of ghrelin. PPY - inhibition of upper GI tract motility GLP-1 - ... or by receptor mediated calcium influx. These efferent motor neuronns of the enteric nervous system are cholinergic and ...
*  Ghrelin O-acyltransferase
Liu B, Garcia EA, Korbonits M (November 2011). "Genetic studies on the ghrelin, growth hormone secretagogue receptor (GHSR) and ... Heppner KM, Tong J, Kirchner H, Nass R, Tschöp MH (February 2011). "The ghrelin O-acyltransferase-ghrelin system: a novel ... "The ghrelin O-acyltransferase-ghrelin system reduces TNF-α-induced apoptosis and autophagy in human visceral adipocytes". ... "Genetic variation of the ghrelin activator gene ghrelin O-acyltransferase (GOAT) is associated with anorexia nervosa". Journal ...