Page last updated: 2024-11-11

hexarelin

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Description

hexarelin: a synthetic growth hormone releasing peptide; structurally similar to GHRP-6, with the substitution of D-Trp with its 2-methyl derivative; more potent & stable and less toxic than GHRP-6 [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID6918297
CHEMBL ID108335
SCHEMBL ID26959
SCHEMBL ID18428170
MeSH IDM0228499

Synonyms (23)

Synonym
ep-23905
hexarelin
examorelin
CHEMBL108335
mf-6003
140703-51-1
(2s)-6-amino-2-[[(2r)-2-[[(2s)-2-[[(2s)-2-[[(2r)-2-[[(2s)-2-amino-3-(1h-imidazol-5-yl)propanoyl]amino]-3-(2-methyl-1h-indol-3-yl)propanoyl]amino]propanoyl]amino]-3-(1h-indol-3-yl)propanoyl]amino]-3-phenylpropanoyl]amino]hexanamide
l-lysinamide, l-histidyl-2-methyl-d-tryptophyl-l-alanyl-l-tryptophyl-d-phenylalanyl-
unii-09qf37c617
examorelin [inn]
09qf37c617 ,
l-histidyl-2-methyl-d-tryptophyl-l-alanyl-l-tryptophyl-d-phenylalanyl-l-lysinamide
bdbm50370294
examorelin [mart.]
SCHEMBL26959
hexarelin, >=90% (hplc)
HY-19235
SCHEMBL18428170
(s)-2-((2r,5s,8s,11r,14s)-5-((1h-indol-3-yl)methyl)-14-amino-2-benzyl-15-(1h-imidazol-4-yl)-8-methyl-11-((2-methyl-1h-indol-3-yl)methyl)-4,7,10,13-tetraoxo-3,6,9,12-tetraazapentadecanamido)-6-aminohexanamide
Q21098927
AMY22775
DTXSID401032408
AKOS040744417

Research Excerpts

Overview

Hexarelin is a synthetic small peptide ghrelin analogue, which has been shown to protect cardiomyocytes from the ischemia-reperfusion process. Hexarelin (HEX) is a peptide GH secretagogue with a potent ability to stimulate GH secretion.

ExcerptReferenceRelevance
"Hexarelin is a synthetic growth hormone-releasing peptide that exerts cardioprotective effects. "( Hexarelin protects cardiac H9C2 cells from angiotensin II-induced hypertrophy
Agbo, E; Li, MX; Massaro, J; Saahene, RO; Tian, GZ; Wang, YQ, 2019
)
3.4
"Hexarelin is a synthetic growth hormone-releasing peptide that exerts cardioprotective effects. "( Modulation of PTEN by hexarelin attenuates coronary artery ligation-induced heart failure in rats
Agbo, E; Chen, L; Li, M; Liu, D; Saahene, RO; Tian, G; Wang, Y; Zhao, L, 2019
)
2.27
"Hexarelin (Hex) is a synthetic small peptide ghrelin analogue, which has been shown to protect cardiomyocytes from the ischemia-reperfusion process."( Hexarelin Protects Rodent Pancreatic Β-Cells Function from Cytotoxic Effects of Streptozotocin Involving Mitochondrial Signalling Pathways In Vivo and In Vitro.
Chen, C; Chen, J; Lin, C; Shao, R; Yan, C; Zhang, X; Zhao, Y, 2016
)
2.6
"Hexarelin (HEX) is a peptide GH secretagogue with a potent ability to stimulate GH secretion and recently reported cardioprotective actions. "( Growth hormone-releasing peptide hexarelin reduces neonatal brain injury and alters Akt/glycogen synthase kinase-3beta phosphorylation.
Brywe, KG; Destefanis, S; Ghigo, E; Granata, R; Gustavsson, M; Hagberg, H; Isgaard, J; Leverin, AL; Mallard, C; Volante, M, 2005
)
2.05
"Hexarelin is a synthetic growth hormone secretagogue (GHS), which possesses a variety of cardiovascular protective activities mediated via the GHS receptor (GHSR), including improving cardiac dysfunction and remodeling."( Hexarelin suppresses cardiac fibroblast proliferation and collagen synthesis in rat.
Cao, JM; Chen, C; Hao, W; Li, M; Pang, J; Xu, X; Yin, H, 2007
)
2.5
"Hexarelin is a recently developed six amino acid residue GHRP."( The effect of an opiate antagonist on the hormonal changes induced by hexarelin.
Besser, GM; Korbonits, M; Trainer, PJ, 1995
)
1.25
"Hexarelin (Hex) is a new synthetic hexapeptide with potent GH-releasing activity in both animals and men. "( The effect of hexarelin on growth hormone (GH) secretion in patients with GH deficiency.
Cambiaso, P; Cappa, M; Colao, A; Deghenghi, R; Faedda, A; Imbimbo, BP; Loche, S; Lombardi, G; Merola, B, 1995
)
2.09
"Hexarelin (Hex) is a new synthetic hexapeptide with potent growth hormone (GH)-releasing activity in both animals and men. "( The growth hormone-releasing activity of hexarelin, a new synthetic hexapeptide, in short normal and obese children and in hypopituitary subjects.
Borrelli, P; Cambiaso, P; Cappa, M; Carta, D; Imbimbo, BP; Loche, S; Pintor, C; Setzu, S, 1995
)
2
"Hexarelin is a new synthetic growth hormone releasing peptide. "( Growth hormone releasing activity by intranasal administration of a synthetic hexapeptide (hexarelin).
Boutignon, F; Deghenghi, R; Frenkel, J; Gil-Ad, I; Klinger, B; Laron, Z; Lengerts, V; Lubin, E; Wuthrich, P, 1994
)
1.95
"Hexarelin is a new hexapeptide (His-D-2-methyl-Trp-Ala-Trp-D-Phe-Lys-NH2) that stimulates the release of growth hormone both in vitro and in vivo. "( Growth hormone-releasing activity of hexarelin in humans. A dose-response study.
Amin, D; Boutignon, F; Dalton, N; Deghenghi, R; Edwards, M; Imbimbo, BP; Lenaerts, V; Mant, T; Wüthrich, P, 1994
)
2
"Hexarelin is a potent GH secretagogue subject to partial feedback inhibition by rhGH. "( Hexarelin induced growth hormone release is influenced by exogenous growth hormone.
Brook, CG; Hindmarsh, PC; Massoud, AF, 1995
)
3.18
"Hexarelin is a recently synthesized small growth hormone releasing peptide (GHRP) (His-D-2-methyl-Trp-Ala-Trp-D-Phe-Lys- NH2). "( Intranasal administration of the GHRP hexarelin accelerates growth in short children.
Anin, S; Deghenghi, R; Frenkel, J; Klinger, B; Laron, Z; Silbergeld, A, 1995
)
2
"Hexarelin is a synthetic six-amino-acid compound capable of releasing GH in animals and in man. "( The effect of repeated administration of hexarelin, a growth hormone releasing peptide, and growth hormone releasing hormone on growth hormone responsivity.
Brook, CG; Hindmarsh, PC; Massoud, AF; Matthews, DR, 1996
)
2
"Hexarelin (Hex) is a new synthetic GH-releasing peptide (GHRP) similar to GHRP-6 with potent GH-releasing activity in animals and men."( Exogenous growth hormone administration does not inhibit the growth hormone response to hexarelin in normal men.
Bernardini, S; Cappa, M; Carta, D; Federici, G; Grossi, A; Loche, S; Setzu, S, 1995
)
1.23
"Hexarelin is an analog of GHRP-6 which releases GH in part via somatostatin inhibition."( Hypothalamic control of growth hormone (GH) secretion in type I diabetic men: effect of the combined administration of GH-releasing hormone and hexarelin, a novel GHRP-6 analog.
Bugari, G; Deghenghi, R; Desenzani, P; Giustina, A; Giustina, G; Perini, P; Wehrenberg, WB, 1996
)
1.22
"Hexarelin is a synthetic hexapeptide with potent GH-releasing activity in both animals and men. "( Acute administration of hexarelin stimulates GH secretion during day and night in normal men.
Cappa, M; Colao, A; Deghenghi, R; Faedda, A; Ferone, D; Imbimbo, BP; Loche, S; Lombardi, G; Merola, B, 1997
)
2.05
"Hexarelin (HEX) is a synthetic hexapeptide belonging to the growth hormone-releasing peptide (GHRP) family. "( Low hexarelin dose and pyridostigmine have additive effect and potentiate to the same extent the GHRH-induced GH response in man.
Arvat, E; Camanni, F; Deghenghi, R; Di Vito, L; Ghigo, E; Gianotti, L; Giordano, R; Ramunni, J, 1997
)
2.3
"Hexarelin (HEX) is a synthetic growth-hormone-releasing peptide (GHRP) which acts via specific receptors at both the pituitary and the hypothalamic level to stimulate GH release both in animals and in man. "( Hexarelin, a synthetic growth-hormone releasing peptide, shows no interaction with corticotropin-releasing hormone and vasopressin on adrenocorticotropin and cortisol secretion in humans.
Arvat, E; Broglio, F; Camanni, F; Deghenghi, R; Di Vito, L; Ghigo, E; Maccagno, B; Ramunni, J, 1997
)
3.18
"Hexarelin (HEX) is a synthetic growth hormone-releasing peptide (GHRP) which acts on specific receptors at both the pituitary and the hypothalamic level to stimulate GH release in an age-dependent manner. "( The GH, prolactin, ACTH and cortisol responses to Hexarelin, a synthetic hexapeptide, undergo different age-related variations.
Arvat, E; Baffoni, C; Bartolotta, E; Bellone, J; Broglio, F; Deghenghi, R; Di Vito, L; Ghigo, E; Ramunni, J, 1997
)
1.99
"Hexarelin (HEX) is a synthetic GHRP which acts on specific receptors at both the pituitary and the hypothalamic level to stimulate GH release both in animals and in humans. "( Effects of dexamethasone and alprazolam, a benzodiazepine, on the stimulatory effect of hexarelin, a synthetic GHRP, on ACTH, cortisol and GH secretion in humans.
Arvat, E; Benso, A; Broglio, F; Camanni, F; Deghenghi, R; Di Vito, L; Ghigo, E; Gianotti, L; Maccagno, B; Ramunni, J, 1998
)
1.97
"Hexarelin (Hex) is a synthetic hexapeptide with potent GH-releasing activity in both animals and men. "( The growth hormone response to hexarelin in patients with Prader-Willi syndrome.
Cappa, M; Deghenghi, R; Faedda, A; Gurreri, F; Loche, S; Neri, G; Palmiotto, T; Raguso, G, 1998
)
2.03
"Hexarelin (HEX) is a synthetic GH-secretagogue (GHS) which acts on specific receptors either at the pituitary or the hypothalamic level to stimulate GH release both in animal and in man. "( Influence of galanin and serotonin on the endocrine response to Hexarelin, a synthetic peptidyl GH-secretagogue, in normal women.
Arvat, E; Benso, A; Broglio, F; Deghenghi, R; Ghigo, E; Giordano, R; Lanfranco, F; Maccagno, B; Ramunni, J, 1998
)
1.98
"Hexarelin (HEX) is a peptidyl GH secretagogue (GHS) which markedly stimulates GH release but, like other GHS, possesses also CNS-mediated ACTH- and cortisol-releasing activity. "( Effects of the combined administration of hexarelin, a synthetic peptidyl GH secretagogue, and hCRH on ACTH, cortisol and GH secretion in patients with Cushing's disease.
Arvat, E; Benso, A; Broglio, F; Deghenghi, R; Ghigo, E; Giordano, R; Maccagno, B; Ramunni, J, 1999
)
2.01
"Hexarelin (HEX) is a synthetic hexapeptide with strong GH-stimulating activity. "( Hexarelin-induced growth hormone response in short stature. Comparison with growth hormone-releasing hormone plus pyridostigmine and arginine plus estrogen.
Grugni, G; Guzzaloni, G; Morabito, F, 1999
)
3.19
"Hexarelin is a growth hormone-releasing peptide with GH-, ACTH/cortisol- and prolactin-releasing effects which involve both hypothalamic and direct pituitary mechanisms."( Hexarelin as a test of pituitary reserve in patients with pituitary disease.
Besser, GM; Grossman, AB; Kaltsas, G; Korbonits, M; Monson, JP; Perry, LA; Trainer, PJ, 1999
)
2.47
"Hexarelin (HEX) is a new synthetic analog of the Growth Hormone releasing peptides and is stronger than GHRH in releasing GH in vivo. "( Role of food intake in the modulation of hexarelin-induced growth hormone release in normal human subjects.
Bianchi, A; De Marinis, L; Desenzani, P; Gentilella, R; Giampietro, A; Giustina, A; Izzi, D; Mancini, A; Valle, D, 2000
)
2.02

Effects

Hexarelin has been demonstrated to improve heart function in various types of cardiomyopathy. It has been reported to regulate peroxisome proliferator-activated receptor gamma (PPAR-γ) in macrophages and adipocytes.

ExcerptReferenceRelevance
"Hexarelin has been demonstrated to improve heart function in various types of cardiomyopathy via its receptor GHS-R."( Improvement of cardiomyocyte function by in vivo hexarelin treatment in streptozotocin-induced diabetic rats.
Chen, C; Chen, L; Qu, L; Zhang, X, 2018
)
1.46
"Hexarelin has been reported to regulate peroxisome proliferator-activated receptor gamma (PPAR-γ) in macrophages and adipocytes."( Implications of ghrelin and hexarelin in diabetes and diabetes-associated heart diseases.
Chen, C; Chen, J; Deng, C; Mosa, RM; Shao, R; Zhang, Z, 2015
)
1.43

Treatment

Hexarelin treatment significantly increased the pulsatile GH secretion without detectable alteration on basal GH secretion in MC4RKO mice. Hexarelin was more effective than ghrelin treatment, as indicated by the ejection fraction, dP/dt max (peak rate of pressure rise), and dp/dt min.

ExcerptReferenceRelevance
"Hexarelin treatment significantly increased the pulsatile GH secretion without detectable alteration on basal GH secretion in MC4RKO mice."( Stimulation of endogenous pulsatile growth hormone secretion by activation of growth hormone secretagogue receptor reduces the fat accumulation and improves the insulin sensitivity in obese mice.
Chen, C; Cowley, MA; Huang, L; Huang, Z; Lu, X; Veldhuis, JD; Zhang, C, 2021
)
1.34
"Hexarelin treatment significantly improved glucose and insulin intolerance and decreased plasma and liver triglycerides in MKR mice."( Hexarelin, a Growth Hormone Secretagogue, Improves Lipid Metabolic Aberrations in Nonobese Insulin-Resistant Male MKR Mice.
Chen, C; Fung, C; Huang, L; LeRoith, D; Mallawakankanamalage, O; Mosa, R; Wu, Y, 2017
)
2.62
"Hexarelin treatment was more effective than ghrelin treatment, as indicated by the ejection fraction, dP/dt max (peak rate of pressure rise), and dP/dt min."( Hexarelin treatment in male ghrelin knockout mice after myocardial infarction.
Hosoda, H; Kangawa, K; Kishimoto, I; Mao, Y; Minamino, N; Miyazato, M; Nagai, C; Otani, K; Tokudome, T, 2013
)
2.55
"Hexarelin treatment concurrently lowered plasma epinephrine and dopamine levels, and shifted the balance of autonomic nervous activity toward parasympathetic nervous activity as evidenced by a smaller low/high-frequency power ratio and larger normalized high-frequency power on heart rate variability analysis."( One dose of oral hexarelin protects chronic cardiac function after myocardial infarction.
Kangawa, K; Kishimoto, I; Mao, Y; Miyazato, M; Otani, K; Tokudome, T, 2014
)
1.46
"Hexarelin treatment significantly reduced cardiac fibrosis in SHRs by decreasing interstitial and perivascular myocardial collagen deposition and myocardial hydroxyproline content and reducing mRNA and protein expression of collagen I and III in SHR hearts."( Chronic administration of hexarelin attenuates cardiac fibrosis in the spontaneously hypertensive rat.
Cao, JM; Chen, C; Ding, F; Gao, X; Hao, W; Pang, J; Xu, RK; Xu, X, 2012
)
1.4
"Hexarelin treatment significantly increased pituitary and hypothalamic GHS-R1a mRNA levels in normal infant rats, but not in normal young adult rats."( Hexarelin modulates the expression of growth hormone secretagogue receptor type 1a mRNA at hypothalamic and pituitary sites.
Avallone, R; Bresciani, E; Gaylinn, B; Locatelli, V; Müller, EE; Nass, R; Thorner, MO; Torsello, A, 2004
)
2.49
"Hexarelin treatment stimulated insulin-like growth factor-I (IGF-I) secretion raising the level from 10.4 +/- 3.9 (SD) to 14.1 +/- 4.6 nmol/l (P < 0.004). "( Intranasal administration of the GHRP hexarelin accelerates growth in short children.
Anin, S; Deghenghi, R; Frenkel, J; Klinger, B; Laron, Z; Silbergeld, A, 1995
)
2
"Hexarelin treatment did not alter GH mRNA levels in control pups."( Hexarelin stimulation of growth hormone release and mRNA levels in an infant and adult rat model of impaired GHRH function.
Deghenghi, R; Grilli, R; Guidi, M; Locatelli, V; Luoni, M; Müller, EE; Torsello, A; Wehrenberg, WB, 1997
)
2.46

Pharmacokinetics

ExcerptReferenceRelevance
"A radioimmunoassay (RIA) method for hexarelin, a peptidic growth hormone secretagogue, has been developed and applied to pharmacokinetic studies in dogs following an IV dose of 1 microgram/kg, and three SC doses of 1, 10, and 100 micrograms/kg."( Radioimmunoassay for hexarelin, a peptidic growth hormone secretagogue, and its pharmacokinetic studies.
Adam, A; Bellemare, M; Boutignon, F; Deghenghi, R; Lenaerts, V; Ong, H; Roumi, M; Wuthrich, P, 1995
)
0.89

Compound-Compound Interactions

ExcerptReferenceRelevance
" When combined with arginine, however, GHRH becomes a potent and reproducible test, which is unaffected by gender and aging, showing excellent specificity."( Growth hormone-releasing hormone combined with arginine or growth hormone secretagogues for the diagnosis of growth hormone deficiency in adults.
Aimaretti, G; Arvat, E; Camanni, F; Ghigo, E, 2001
)
0.31

Bioavailability

Hexarelin, a hexapeptide with growth hormone-releasing activity, has been found in man to have a biological bioavailability (estimated from growth hormone levels) of 0. Although the results obtained in this study are promising, pharmacokinetic and toxicological studies are required to investigate if this delivery system is a suitable and safe candidate.

ExcerptReferenceRelevance
" Although the results obtained in this study are promising, pharmacokinetic and toxicological studies are required to investigate if this delivery system is a suitable and safe candidate for improving the oral bioavailability of hexarelin."( The effect of a drug-delivery system consisting of soybean phosphatidyl choline and medium-chain monoacylglycerol on the intestinal permeability of hexarelin in the rat.
Fagerholm, U; Lennernäs, H; Sjöström, B; Sroka-Markovic, J; Svensson, M; Wijk, A, 1998
)
0.68

Dosage Studied

Hexarelin is a potent GH secretagogue active after two successive doses. Over-stimulation of the pituitary adrenal axis and prolactin secretion do not occur.

ExcerptRelevanceReference
"This study shows that hexarelin is a potent GH secretagogue active after two successive doses; the magnitude of the GH response to the second dose was influenced by the dosing interval."( The effect of repeated administration of hexarelin, a growth hormone releasing peptide, and growth hormone releasing hormone on growth hormone responsivity.
Brook, CG; Hindmarsh, PC; Massoud, AF; Matthews, DR, 1996
)
0.87
" Dose-response curves for the maximum GH response and maximum percent change in serum PRL and cortisol concentrations from baseline were constructed."( Hexarelin-induced growth hormone, cortisol, and prolactin release: a dose-response study.
Brook, CG; Hindmarsh, PC; Massoud, AF, 1996
)
1.74
" An iv dose-response study in six 20- to 40-yr-old well nourished hemodialysis (HD) patients was followed by administration of the maximally effective dose to six 20- to 40-yr-old healthy controls, six 20- to 40-yr-old poorly nourished HD patients, and six 50- to 70-yr-old poorly nourished HD patients."( The effects of dose, nutrition, and age on hexarelin-induced anterior pituitary hormone secretion in adult patients on maintenance hemodialysis.
Brown, CB; El Nahas, AM; Ghigo, E; Jenkins, RC; Jones, J; Ross, RJ; Wilkie, ME, 1999
)
0.57
"The present study demonstrates clearly that in this hexarelin dosage regimen, over-stimulation of the pituitary adrenal axis and prolactin secretion do not occur."( The effect of chronic hexarelin administration on the pituitary-adrenal axis and prolactin.
O'Neill, PA; Rahim, A; Shalet, SM, 1999
)
0.87
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (2)

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Platelet glycoprotein 4Rattus norvegicus (Norway rat)IC50 (µMol)2.08001.82001.95002.0800AID698140
Growth hormone secretagogue receptor type 1Homo sapiens (human)IC50 (µMol)0.01700.00040.58926.0000AID698139; AID75332
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (47)

Processvia Protein(s)Taxonomy
G protein-coupled receptor signaling pathwayGrowth hormone secretagogue receptor type 1Homo sapiens (human)
spermatogenesisGrowth hormone secretagogue receptor type 1Homo sapiens (human)
learning or memoryGrowth hormone secretagogue receptor type 1Homo sapiens (human)
actin polymerization or depolymerizationGrowth hormone secretagogue receptor type 1Homo sapiens (human)
adult feeding behaviorGrowth hormone secretagogue receptor type 1Homo sapiens (human)
response to hormoneGrowth hormone secretagogue receptor type 1Homo sapiens (human)
hormone-mediated signaling pathwayGrowth hormone secretagogue receptor type 1Homo sapiens (human)
negative regulation of norepinephrine secretionGrowth hormone secretagogue receptor type 1Homo sapiens (human)
growth hormone secretionGrowth hormone secretagogue receptor type 1Homo sapiens (human)
response to foodGrowth hormone secretagogue receptor type 1Homo sapiens (human)
negative regulation of appetiteGrowth hormone secretagogue receptor type 1Homo sapiens (human)
positive regulation of appetiteGrowth hormone secretagogue receptor type 1Homo sapiens (human)
response to follicle-stimulating hormoneGrowth hormone secretagogue receptor type 1Homo sapiens (human)
response to estradiolGrowth hormone secretagogue receptor type 1Homo sapiens (human)
negative regulation of interleukin-1 beta productionGrowth hormone secretagogue receptor type 1Homo sapiens (human)
negative regulation of interleukin-6 productionGrowth hormone secretagogue receptor type 1Homo sapiens (human)
negative regulation of tumor necrosis factor productionGrowth hormone secretagogue receptor type 1Homo sapiens (human)
cellular response to insulin stimulusGrowth hormone secretagogue receptor type 1Homo sapiens (human)
ghrelin secretionGrowth hormone secretagogue receptor type 1Homo sapiens (human)
positive regulation of multicellular organism growthGrowth hormone secretagogue receptor type 1Homo sapiens (human)
regulation of hindgut contractionGrowth hormone secretagogue receptor type 1Homo sapiens (human)
positive regulation of insulin-like growth factor receptor signaling pathwayGrowth hormone secretagogue receptor type 1Homo sapiens (human)
positive regulation of fatty acid metabolic processGrowth hormone secretagogue receptor type 1Homo sapiens (human)
negative regulation of insulin secretionGrowth hormone secretagogue receptor type 1Homo sapiens (human)
decidualizationGrowth hormone secretagogue receptor type 1Homo sapiens (human)
insulin-like growth factor receptor signaling pathwayGrowth hormone secretagogue receptor type 1Homo sapiens (human)
negative regulation of inflammatory responseGrowth hormone secretagogue receptor type 1Homo sapiens (human)
regulation of synapse assemblyGrowth hormone secretagogue receptor type 1Homo sapiens (human)
regulation of transmission of nerve impulseGrowth hormone secretagogue receptor type 1Homo sapiens (human)
regulation of growth hormone secretionGrowth hormone secretagogue receptor type 1Homo sapiens (human)
response to growth hormoneGrowth hormone secretagogue receptor type 1Homo sapiens (human)
cellular response to lipopolysaccharideGrowth hormone secretagogue receptor type 1Homo sapiens (human)
response to dexamethasoneGrowth hormone secretagogue receptor type 1Homo sapiens (human)
negative regulation of locomotion involved in locomotory behaviorGrowth hormone secretagogue receptor type 1Homo sapiens (human)
cellular response to thyroid hormone stimulusGrowth hormone secretagogue receptor type 1Homo sapiens (human)
regulation of neurotransmitter receptor localization to postsynaptic specialization membraneGrowth hormone secretagogue receptor type 1Homo sapiens (human)
postsynaptic modulation of chemical synaptic transmissionGrowth hormone secretagogue receptor type 1Homo sapiens (human)
regulation of postsynapse organizationGrowth hormone secretagogue receptor type 1Homo sapiens (human)
positive regulation of small intestinal transitGrowth hormone secretagogue receptor type 1Homo sapiens (human)
response to L-glutamateGrowth hormone secretagogue receptor type 1Homo sapiens (human)
positive regulation of sprouting angiogenesisGrowth hormone secretagogue receptor type 1Homo sapiens (human)
positive regulation of eating behaviorGrowth hormone secretagogue receptor type 1Homo sapiens (human)
positive regulation of small intestine smooth muscle contractionGrowth hormone secretagogue receptor type 1Homo sapiens (human)
regulation of gastric motilityGrowth hormone secretagogue receptor type 1Homo sapiens (human)
positive regulation of vascular endothelial cell proliferationGrowth hormone secretagogue receptor type 1Homo sapiens (human)
cellular response to insulin-like growth factor stimulusGrowth hormone secretagogue receptor type 1Homo sapiens (human)
negative regulation of macrophage apoptotic processGrowth hormone secretagogue receptor type 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (4)

Processvia Protein(s)Taxonomy
growth hormone secretagogue receptor activityGrowth hormone secretagogue receptor type 1Homo sapiens (human)
G protein-coupled receptor activityGrowth hormone secretagogue receptor type 1Homo sapiens (human)
growth hormone-releasing hormone receptor activityGrowth hormone secretagogue receptor type 1Homo sapiens (human)
peptide hormone bindingGrowth hormone secretagogue receptor type 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (8)

Processvia Protein(s)Taxonomy
plasma membraneGrowth hormone secretagogue receptor type 1Homo sapiens (human)
cell surfaceGrowth hormone secretagogue receptor type 1Homo sapiens (human)
neuron projectionGrowth hormone secretagogue receptor type 1Homo sapiens (human)
membrane raftGrowth hormone secretagogue receptor type 1Homo sapiens (human)
synaptic membraneGrowth hormone secretagogue receptor type 1Homo sapiens (human)
Schaffer collateral - CA1 synapseGrowth hormone secretagogue receptor type 1Homo sapiens (human)
postsynapseGrowth hormone secretagogue receptor type 1Homo sapiens (human)
glutamatergic synapseGrowth hormone secretagogue receptor type 1Homo sapiens (human)
plasma membraneGrowth hormone secretagogue receptor type 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (16)

Assay IDTitleYearJournalArticle
AID1859425Oral bioavailability in human2022European journal of medicinal chemistry, May-05, Volume: 235An insight into the multifunctional role of ghrelin and structure activity relationship studies of ghrelin receptor ligands with clinical trials.
AID312916Effect on food intake per 100 gm of body weight in rat at 80 ug/kg, sc after 6 hrs2008Journal of medicinal chemistry, Feb-14, Volume: 51, Issue:3
New trisubstituted 1,2,4-triazole derivatives as potent ghrelin receptor antagonists. 3. Synthesis and pharmacological in vitro and in vivo evaluations.
AID590161Antagonist activity at human CD36-oxLDL binding at 1 uM after 2 hrs by ELISA2011European journal of medicinal chemistry, Apr, Volume: 46, Issue:4
Synthesis and structure-activity relationship of N-(2-arylethyl) isoquinoline derivatives as human scavenger receptor CD36 antagonists.
AID1465894Inhibition of photoactivatable [125I]-Tyr-Bpa-Ala-hexarelin binding to CD36 in Sprague-Dawley rat heart membranes after 60 mins by SDS-PAGE analysis2017Journal of medicinal chemistry, 11-22, Volume: 60, Issue:22
Influences of Histidine-1 and Azaphenylalanine-4 on the Affinity, Anti-inflammatory, and Antiangiogenic Activities of Azapeptide Cluster of Differentiation 36 Receptor Modulators.
AID698139Displacement of [125I]ghrelin expressed in in LLC-PK1 cells incubated for 1 hr by gamma counting method2012Journal of medicinal chemistry, Jul-26, Volume: 55, Issue:14
Azapeptide analogues of the growth hormone releasing peptide 6 as cluster of differentiation 36 receptor ligands with reduced affinity for the growth hormone secretagogue receptor 1a.
AID75332Binding affinity towards human pituitary Growth hormone secretagogue receptor using [125I][Tyr4]-ghrelin as radioligand2003Journal of medicinal chemistry, Mar-27, Volume: 46, Issue:7
New active series of growth hormone secretagogues.
AID171951compound was evaluated for GH release in rat1998Journal of medicinal chemistry, Aug-13, Volume: 41, Issue:17
Peptidomimetic growth hormone secretagogues. Design considerations and therapeutic potential.
AID1181136Increase in food intake in po dosed C57Bl6j mouse free feeding model measured in 2 hrs intervals2014Journal of medicinal chemistry, Jul-24, Volume: 57, Issue:14
Identification, optimization, and pharmacology of acylurea GHS-R1a inverse agonists.
AID281434Stimulation of cumulative food intake in Sprague-Dawley rat at 80 ug/kg, sc at 6 hrs2007Journal of medicinal chemistry, Apr-19, Volume: 50, Issue:8
Synthesis and pharmacological in vitro and in vivo evaluations of novel triazole derivatives as ligands of the ghrelin receptor. 1.
AID75345Binding affinity towards cloned human Growth hormone secretagogue receptor type I in LLC PK-1 cells using [125I][His9]-ghrelin as radioligand2003Journal of medicinal chemistry, Mar-27, Volume: 46, Issue:7
New active series of growth hormone secretagogues.
AID1465895Inhibition of photoactivatable [125I]-Tyr-Bpa-Ala-hexarelin binding to CD36 in Sprague-Dawley rat heart membranes after 60 mins by SDS-PAGE analysis relative to H-His-D-Trp-Ala-aza(3-hydroxy)Phe-D-Phe-Lys-NH22017Journal of medicinal chemistry, 11-22, Volume: 60, Issue:22
Influences of Histidine-1 and Azaphenylalanine-4 on the Affinity, Anti-inflammatory, and Antiangiogenic Activities of Azapeptide Cluster of Differentiation 36 Receptor Modulators.
AID187245Ratio of GH release stimulated by 300 ug/kg of compound to that of GH release stimulated by 300 ug/kg of hexarelin in infant rat (sc injection)2003Journal of medicinal chemistry, Mar-27, Volume: 46, Issue:7
New active series of growth hormone secretagogues.
AID698140Displacement of photoactivatable [125I]-Tyr-Bpa-Ala-Hexarelin from CD36 in Sprague-Dawley rat cardiac membranes incubated for 60 mins by densitometry2012Journal of medicinal chemistry, Jul-26, Volume: 55, Issue:14
Azapeptide analogues of the growth hormone releasing peptide 6 as cluster of differentiation 36 receptor ligands with reduced affinity for the growth hormone secretagogue receptor 1a.
AID312926Effect on growth hormone secretion in infant rat at 80 ug/kg, sc2008Journal of medicinal chemistry, Feb-14, Volume: 51, Issue:3
New trisubstituted 1,2,4-triazole derivatives as potent ghrelin receptor antagonists. 3. Synthesis and pharmacological in vitro and in vivo evaluations.
AID281439Effect on growth hormone secretion in Sprague-Dawley rat at 80 ug/kg, sc2007Journal of medicinal chemistry, Apr-19, Volume: 50, Issue:8
Synthesis and pharmacological in vitro and in vivo evaluations of novel triazole derivatives as ligands of the ghrelin receptor. 1.
AID312913Effect on food intake per 100 gm of body weight in rat at 80 ug/kg, sc after 2 hrs2008Journal of medicinal chemistry, Feb-14, Volume: 51, Issue:3
New trisubstituted 1,2,4-triazole derivatives as potent ghrelin receptor antagonists. 3. Synthesis and pharmacological in vitro and in vivo evaluations.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (255)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's114 (44.71)18.2507
2000's95 (37.25)29.6817
2010's39 (15.29)24.3611
2020's7 (2.75)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 53.52

According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be very strong demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index53.52 (24.57)
Research Supply Index5.76 (2.92)
Research Growth Index4.34 (4.65)
Search Engine Demand Index97.34 (26.88)
Search Engine Supply Index2.21 (0.95)

This Compound (53.52)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials56 (21.46%)5.53%
Reviews24 (9.20%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other181 (69.35%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]