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ghrelin receptor

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Target not currently curated in GtoImmuPdb

Target id: 246

Nomenclature: ghrelin receptor

Family: Ghrelin receptor

Gene and Protein Information Click here for help
class A G protein-coupled receptor
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human 7 366 3q26.31 GHSR growth hormone secretagogue receptor 33
Mouse 7 364 3 A3 Ghsr growth hormone secretagogue receptor 80
Rat 7 364 2q24 Ghsr growth hormone secretagogue receptor 52
Previous and Unofficial Names Click here for help
growth hormone-releasing peptide receptor | GH-releasing peptide receptor | GHS-R | ghrelin receptor 1a
Database Links Click here for help
Specialist databases
GPCRdb ghsr_human (Hs), ghsr_mouse (Mm), ghsr_rat (Rn)
Other databases
Alphafold
ChEMBL Target
Ensembl Gene
Entrez Gene
Human Protein Atlas
KEGG Gene
OMIM
Orphanet
Pharos
RefSeq Nucleotide
RefSeq Protein
UniProtKB
Wikipedia
Natural/Endogenous Ligands Click here for help
[des-Gln14]ghrelin {Sp: Human} , [des-Gln14]ghrelin {Sp: Mouse, Rat}
ghrelin {Sp: Human} , ghrelin {Sp: Mouse, Rat}
Comments: The major circulating form of ghrelin is [des-octanoyl]ghrelin (human)/[des-octanoyl]ghrelin (mouse/rat).
Potency order of endogenous ligands (Human)
ghrelin (GHRL, Q9UBU3) = [des-Gln14]ghrelin (GHRL, Q9UBU3)  [2,51]

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Agonists
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Value Parameter Reference
[125I][His9]ghrelin (human) Peptide Ligand is labelled Ligand is radioactive Hs Full agonist 9.4 pKd 37
pKd 9.4 (Kd 4x10-10 M) [37]
[125I][Tyr4]ghrelin (human) Peptide Ligand is labelled Ligand is radioactive Hs Full agonist 9.4 pKd 56
pKd 9.4 (Kd 4x10-10 M) [56]
[35S]ibutamoren Small molecule or natural product Ligand is labelled Ligand is radioactive Hs Full agonist 9.2 pKd 52
pKd 9.2 [52]
ghrelin {Sp: Human} Peptide Ligand is endogenous in the given species Hs Full agonist 8.6 – 9.4 pKd 29-30
pKd 8.6 – 9.4 (Kd 2.3x10-9 – 3.6x10-10 M) [29-30]
[125I]Tyr-Ala-hexarelin Peptide Ligand is labelled Ligand is radioactive Hs Full agonist 8.2 pKd 63
pKd 8.2 [63]
examorelin Peptide Hs Full agonist 7.9 pKd 63
pKd 7.9 (Kd 1.3x10-8 M) [63]
GHRP-6 Peptide Hs Full agonist 6.6 – 8.8 pKd 29,52
pKd 6.6 – 8.8 (Kd 2.5x10-7 – 1.6x10-9 M) [29,52]
ibutamoren Small molecule or natural product Ligand has a PDB structure Hs Full agonist 9.3 pKi 28
pKi 9.3 (Ki 4.6x10-10 M) [28]
pralmorelin Peptide Approved drug Rn Full agonist 9.3 pKi 52
pKi 9.3 [52]
HM01 Small molecule or natural product Hs Agonist 8.9 pKi 36
pKi 8.9 (Ki 1.4x10-9 M) [36]
GHRP-6 Peptide Rn Full agonist 8.8 pKi 52
pKi 8.8 [52]
[125I][His9]ghrelin (human) Peptide Ligand is labelled Ligand is radioactive Rn Full agonist 8.4 pKi 37
pKi 8.4 [37]
ghrelin {Sp: Human} Peptide Ligand is endogenous in the given species Hs Full agonist 7.8 – 8.1 pKi 56
pKi 7.8 – 8.1 [56]
[des-octanoyl]ghrelin {Sp: Human} Peptide Rn Full agonist 7.9 pKi 7,56
pKi 7.9 [7,56]
SM-130,686 Small molecule or natural product Hs Partial agonist 9.5 pEC50 31
pEC50 9.5 (EC50 3.1x10-10 M) IP3 accumulation [31]
ibutamoren Small molecule or natural product Ligand has a PDB structure Hs Full agonist 8.6 – 9.7 pEC50 28-29
pEC50 8.6 – 9.7 (EC50 2.4x10-9 – 1.9x10-10 M) Calcium release, IP3 accumulation. [28-29]
GHRP-6 Peptide Hs Full agonist 8.3 – 9.1 pEC50 29
pEC50 9.1 (EC50 8.3x10-10 M) IP3 accumulation [29]
pEC50 8.3 (EC50 4.6x10-9 M) Calcium release [29]
ghrelin {Sp: Human} Peptide Ligand is endogenous in the given species Hs Full agonist 7.2 – 9.5 pEC50 25,29-30,62,74
pEC50 9.5 (EC50 3.4x10-10 M) IP3 accumulation [30,74]
pEC50 8.1 (EC50 7.1x10-9 M) [25]
Description: Measuring ghrelin-induced GHSR activation detected by β-arrestin recruitment in cells stably expressing hGHSR.
pEC50 7.2 – 7.5 (EC50 6.1x10-8 – 3.2x10-8 M) calcium release [29,62]
L-692,429 Small molecule or natural product Hs Agonist 7.3 – 7.6 pEC50 29
pEC50 7.3 – 7.6 (EC50 4.7x10-8 – 2.6x10-8 M) Calcium release, IP3 accumulation. [29]
L-692,429 Small molecule or natural product Rn Agonist 7.2 pEC50 75
pEC50 7.2 (EC50 6x10-8 M) GH release [75]
wFw-Isn-NH2 Peptide Hs Partial agonist 5.9 – 8.4 pEC50 74
pEC50 5.9 – 8.4 (EC50 1.2x10-6 – 3.9x10-9 M) IP3 accumulation, ERK phosphotylation, binding [74]
SM-130,686 Small molecule or natural product Hs Partial agonist 8.9 pIC50 83
pIC50 8.9 (IC50 1.2x10-9 M) [83]
macimorelin Small molecule or natural product Approved drug Primary target of this compound Hs Agonist 7.8 pIC50 6
pIC50 7.8 (IC50 1.56x10-8 M) [6]
Description: In a radioligand displacement assay using 125I-labeled ghrelin as the probe, and human pituitary gland samples.
View species-specific agonist tables
Agonist Comments
Ghrelin and des-Gln14-ghrelin are two different naturally occuring ghrelin variants that both activate the ghrelin receptor to induce Ca2+ release and GH secretion [32]. It is important to notice that the potency of ghrelin meassured in Ca2+ release compared to the potency observed in inositol phosphate accumulation is not the same and that the pharmacological profile of ghrelin receptor agonists differ between these two assays, indicating differences in signalling pathway. GHRP-2, GHRP-6 and hexarelin were initially discovered as synthetic peptide growth hormone secretagogues but are today known as high potency hexapeptide agonists for the ghrelin receptor [29,52]. [3H]MK677 and [35S]MK677 are both high affinity radioactive ghrelin receptor full agonists that are no longer comercially availiable, but have been used [3,87]. wFw-Isn-NH2 is a biased agonist that has a lower potency and efficacy in G12/13 coupling compared to other signalling pathways where it is a partial agonist. Only a few of the mentioned agonists have been characterized for receptor interaction pattern by mutation mapping [31]. One study reports the multifunctional glycoprotein CD36 to be a hexarelin binding site in membranes from rat heart [5].
Antagonists
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Value Parameter Reference
GSK1614343 Small molecule or natural product Rn Antagonist 8.0 pKB 66
pKB 8.0 [66]
[D-Arg1,D-Phe5,D-Trp7,9,Leu11]substance P Peptide Hs Antagonist 7.3 pKd 30
pKd 7.3 (Kd 4.5x10-8 M) [30]
PF-05190457 Small molecule or natural product Primary target of this compound Ligand has a PDB structure Hs Antagonist 8.9 pKi 41
pKi 8.9 (Ki 1.42x10-9 M) [41]
Description: Measured in vitro in recombinant receptor over-expressing cells.
PF-05190457 Small molecule or natural product Ligand has a PDB structure Rn Antagonist 8.5 pKi 41
pKi 8.5 (Ki 3.2x10-9 M) [41]
Description: Measured in vitro in recombinant receptor over-expressing cells
PF-05190457 Small molecule or natural product Ligand has a PDB structure Mm Antagonist 8.1 pKi 41
pKi 8.1 (Ki 7.7x10-9 M) [41]
Description: Measured in vitro in recombinant receptor over-expressing cells
BIM 28163 Peptide Hs Antagonist 8.1 pKi 27
pKi 8.1 (Ki 8.1x10-9 M) [27]
YIL781 Small molecule or natural product Hs Antagonist 7.8 pKi 20
pKi 7.8 (Ki 1.7x10-8 M) [20]
PF-6870961 Small molecule or natural product Hs Inverse agonist 7.1 pKi 14
pKi 7.1 (Ki 7.36x10-8 M) [14]
PF-6870961 Small molecule or natural product Rn Inverse agonist 6.6 pKi 14
pKi 6.6 (Ki 2.39x10-7 M) [14]
GSK1614343 Small molecule or natural product Hs Antagonist 8.4 pIC50 70
pIC50 8.4 (IC50 4x10-9 M) [70]
JMV3008 Small molecule or natural product Hs Antagonist 8.3 pIC50 55
pIC50 8.3 (IC50 5.6x10-9 M) [55]
liver enriched antimicrobial peptide 2 {Sp: Human} Peptide Immunopharmacology Ligand Hs Antagonist 8.2 pIC50 25
pIC50 8.2 (IC50 6x10-9 M) [25]
Description: IC50 for LEAP2 antagonism of GHSR activation in the presence of ghrelin.
Abbott 14c Small molecule or natural product Hs Antagonist 8.1 pIC50 94
pIC50 8.1 (IC50 7x10-9 M) [94]
View species-specific antagonist tables
Antagonist Comments
It has been observed that in heterologous expression systems the constitutive signalling of the ghrelin receptor via the IP3 signallling pathway, can be completely abolished by the inverse agonist [D-Arg1,D-Phe, D-Trp7,9, Leu11] [30]. The peptide ligand BIM28163 is an antagonist when measuring ghrelin induced calicium secretion and GH-release, however when measuring food intake it acts as a full agonist [27]. The same has been observed for the non-peptide ligand GSK161443 that behaves as an antagonist both in GH release and [35S]GTPγS. However, this compound turned out to be an agonist on food intake [9]. D-Lys3-GHRP-6 is another ghrelin receptor antagonist, but no binding data is available for this ligand because it has never been tested in binding assays in tissues expressing the ghrelin receptor. Antagonism observed in functional assays was not quantitated and expressed in terms of potency.
Allosteric Modulators
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Value Parameter Reference
L-692,429 Small molecule or natural product Hs Positive 7.0 pEC50 29
pEC50 7.0 (EC50 1x10-7 M) [29]
Allosteric Modulator Comments
L-692,429 is both a "super-agonist", that displays a larger efficacy than ghrelin and an allosteric ligand by increasing the potency of ghrelin when measuring IP accumulation [29,31]. In membrane preparations overexpressing both the ghrelin receptor and Gqi, a similar ligand L-692,585 did not act as an allosteric modulator, when GTPγS was meassured [4].
Immuno Process Associations
Immuno Process:  Inflammation
Immuno Process:  Immune regulation
Immuno Process:  Cytokine production & signalling
Primary Transduction Mechanisms Click here for help
Transducer Effector/Response
Gq/G11 family Phospholipase C stimulation
References:  10,76
Secondary Transduction Mechanisms Click here for help
Transducer Effector/Response
Gi/Go family
G12/G13 family
G protein independent mechanism
Other - See Comments
Comments:  In addition the ghrelin receptor activates the following intracellular responses: β-arrestin [10,29], adaptor-related protein complex [10]. The ghrelin receptor has been shown to dimerize with the following receptors: dopamine D1 receptor [34], dopamine D2 receptor [38], melanocortin MC3 receptor [69], serotonin 5-HT2c receptor [71], thus affecting signalling. The promitotic actions of ghrelin in pancreatic tumour cells can be abolished by the PI3-kinase inhibitor wortmannin [18]. Several studies have shown constitutive production of inositol phosphate and components of other signalling pathways in cells expressing the ghrelin receptor [10,18].
References:  10,29,74
Tissue Distribution Click here for help
Radioligand binding has demonstrated ghrelin receptors in human heart, large conduit vessels and brain. Ghrelin receptor density is significantly upregulated in human atherosclerosis.
Species:  Human
Technique:  Radioligand binding.
References:  37
Immunocytochemsitry has detected ghrelin in human testis and ovary (Leydig, Sertoli, follicular and luteal cells as well as germ cells).
Species:  Human
Technique:  immunocytochemistry.
References:  24
Arcuate nucleus and pituitary.
Species:  Rat
Technique:  immunocytochemistry.
References:  54
Heart: aorta, left ventricle, left atria.
Species:  Rat
Technique:  RT-PCR.
References:  58
Rat brain, NB also in mouse brain.
Species:  Rat
Technique:  in situ hybridisation
References:  97
Radioligand binding has demonstrated ghrelin receptors in the rat heart, brain and chondrocytes.
Species:  Rat
Technique:  Radioligand binding.
References:  37
Pancreas, pituitary.
Species:  Rat
Technique:  Western blotting, RT-PCR
References:  42
Small intestine, large intestine > stomach.
Species:  Rat
Technique:  RT-PCR
References:  11
Pancreatic islets.
Species:  Rat
Technique:  immunocytochemistry.
References:  35
Expression Datasets Click here for help

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Log average relative transcript abundance in mouse tissues measured by qPCR from Regard, J.B., Sato, I.T., and Coughlin, S.R. (2008). Anatomical profiling of G protein-coupled receptor expression. Cell, 135(3): 561-71. [PMID:18984166] [Raw data: website]

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Functional Assays Click here for help
Ghrelin induces GH release from isolated rat pituitary cells (EC50: 2nM).
Species:  Rat
Tissue:  Pituitary cells.
Response measured:  GH release.
References:  40
Ca2+ release (32nM)
Species:  Human
Tissue:  HEK 293 cells
Response measured:  Ca2+ release
References:  62
Ghrelin induces inositol phosphate accumulation (EC50=0.2nM)
Species:  Human
Tissue:  COS-7 cells
Response measured:  Inositol phosphate accumulation
References:  30
Ghrelin receptor in lipid dics, couples to Gi and increases GTPγS binding.
Species:  Human
Tissue:  cell free conditions
Response measured: 
References:  10,49
Activation of RhoA (RhoA-GTP) by ghrelin at 0.1uM.
Species:  Rat
Tissue:  RC-4B/C cells
Response measured: 
References:  74
Ghrelin induces arrestin recruitment (EC50=0.5nM) and recruitment of the u-subunit of AP2 (at 1uM ghrelin).
Species:  Human
Tissue:  HEK 293 cells, U2OS cells
Response measured: 
References:  10,53
Systematic testing of short ghrelin peptides truncated at the c-terminus revealed that Gly-Ser-Ser(Octanoyl)-Phe is the active core of ghrelin showing comparable potency in eliciting increase in intracellular calcium from CHO cells expressing the ghrelin receptor as mature ghrelin. Other acyl modifications on Ser3 do not substantially hamper the receptor activation potency of ghrelin.
Species:  Human
Tissue:  CHO cells, HEK 293 cells
Response measured:  Increase in Ca2+ levels.
References:  3,51
Ghrelin induces cAMP response element binding protein (EC50=0.6nM), serum response element transcription (EC50=2.8nM) and extracellular signal regulated kinase 1/2 (EC50=~0.1nM).
Species:  Human
Tissue:  HEK 293 cells
Response measured: 
References:  29
Physiological Functions Click here for help
Ghrelin potently reverses nicotine and VitaminD3 induced calcification of the aortic vessel wall.
Species:  Rat
Tissue:  Aorta.
References:  43
Intravenous infusion of ghrelin in humans results in a significant increase in growth hormone (GH) as well as ACTH, cortisol and prolactin.
Species:  Human
Tissue:  In vivo.
References:  59,65,79
Ghrelin (intravenous, intracerebroventricular) has been shown to stimulate food intake and lead to body weight gain both in rats. This effect is independent of the GH secretagogue action of ghrelin as it was also observed in GH deficient rats. Ghrelin increases expression of AGRP and NPY in the arcuate and paraventricular nucleus and ghrelin actions can partly be abolished using a NPY antagonist, suggesting that ghrelin actions are mediated by the orexigenic AGRP and NPY pathways.
Species:  Rat
Tissue:  In vivo.
References:  39,61
Ghrelin (intravenous) has been shown to stimulate food intake and lead to body weight gain both in humans.
Species:  Human
Tissue:  In vivo.
References:  17,92
Intravenous infusion of ghrelin in rats results in a significant increase in growth hormone (GH).
Species:  Rat
Tissue:  In vivo.
References:  84
In GH deficient rats unilateral infusion of ghrelin and des-octanoyl ghrelin into the tibial bone marrow stimulated bone marrow adipogenesis.
Species:  Rat
Tissue:  bone marrow in vivo
References:  82
Ghrelin infusion (ICV) in rats resulted in a decreased sympathetic nerve acivity in brown adipose tissue leading to decreased thermogensis and energy expenditure.
Species:  Rat
Tissue:  Brown adipose tissue.
References:  96
Both intravenous and intraperitoneal infusion of ghrelin induces gastric motility and gastric acid and pepsin secretion in rats.
Species:  Rat
Tissue:  Stomach in vivo.
References:  13,19,50
Chronic subcutaneous administration of ghrelin improves left ventricular dysfunction and decreases the development of cardiac cachexia in rats with chronic heart failure.
Species:  Rat
Tissue:  In vivo.
References:  60
Intravenous infusion of ghrelin causes a decrease in mean arterial pressure with no change in heart rate.
Species:  Human
Tissue:  In vivo.
References:  58-59
Ghrelin showed vasodilator actions in studies determining forearm blood flow in healthy volunteers and in endothelium denuded human isolated internal mammary artery.
Species:  Human
Tissue:  In vivo.
References:  91
The acute haemodynamic response was also observed in GH deficient rats and hypotensive actions have been observed for des-octaboyl ghrelin after central administration in the rat nucleus of the solitary tract. The role of endothelial vasodilators in mediating ghrelin-induced vasodilatation is not clear.
Species:  Rat
Tissue:  In vivo.
References:  86
Intracerebroventricular injection of ghrelin into the nucleus of the solitary tract resulted in a decrease in mean arterial pressure and heart rate as well as supressed renal sympathetic nerve activity.
Species:  Rat
Tissue:  In vivo.
References:  46,86
Ghrelin causes increased cell proliferation of H9c2 cardiomyocytes in vitro.
Species:  Rat
Tissue:  Cardiomyocytes in vitro.
References:  1,67
Intracerebroventricular and intravenous injection of ghrelin in rats induces fasted motor activity in the stomach and duodenum.
Species:  Rat
Tissue:  Stomach and duodenum in vivo.
References:  23
Ghrelin significantly reduced infarct size in isolated rat hearts with temporary coronary ligation.
Species:  Rat
Tissue:  Heart.
References:  22
Ghrelin promotes pancreatic adenocarcinoma cell proliferation and invasiveness.
Species:  Human
Tissue:  Pancreatic adenocarcinoma cells.
References:  18
Ghrelin inhibits proliferation of human thyroid carcinoma cells.
Species:  Human
Tissue:  Thyroid carcinoma cell lines.
References:  8,89
Ghrelin is a growth-hormone-releasing peptide secreted from the stomach, that acts both on the hypothalamus and the pituitary.
Species:  Rat
Tissue:  Pituitary
References:  40
Ghrelin induces adiposity in rodents. Administration of ghrelin increases the acute food intake both after intracerebral and peripheral administration. Chronic administration of ghrelin also increases fat accumulation independen of food intake. Ghrelin has also been shown to increase food intake in humans.
Species:  Rat
Tissue:  Hypothalamus
References:  61,81,85,93
Ghrelin inhibits leptin- and activation-induced proinflammatory cytokine expression by human monocytes and T cells. Both the ghrelin receptor and ghrelin are expressed in human T lymphocytes and monocytes, where ghrelin acts to specifically inhibit the expression of proinflammatory anorectic cytokines such as IL-1β, IL-6, and TNFα.
Species:  Human
Tissue:  Hypothalamus, endothelial cells
References:  15-16,44
Ghrelin, a novel growth hormone-releasing peptide, in the treatment of cardiopulmonary-associated cachexia.
Species:  Human
Tissue: 
References:  57
Ghrelin regulates gut motility by central and peripheral mechanisms. Ghrelin for example regulates gastrointestinal motility by the activation of receptors on enteric neurons.
Species:  Human
Tissue: 
References:  64,88,95
Ghrelin protects against ethanol-induced gastric ulcers.
Species:  Rat
Tissue:  Stomach
References:  90
Physiological Consequences of Altering Gene Expression Click here for help
Ghrelin receptor knockout mice show no obvious changes in their bodyweight or food intake phenotype. The GH secretory and feeding inducing effects of ghrelin however are abolished in the ghrelin receptor knockouts.
Species:  Mouse
Tissue: 
Technique:  Gene knock-outs
References:  78
Targeted knockdown of the Ghrelin receptor gene in the arcuate nucleus of the rat results in a significant decrease in food intake, body weight, body fat content and feeding response to growth hormone secretagogues. GH and insulin-like growth factor levels in these rats are also reduced.
Species:  Rat
Tissue: 
Technique:  Gene targeting in embryonic stem cells
References:  73
Simultaneous deletion of ghrelin and its receptor increases motor activity and energy expenditure.
Species:  Mouse
Tissue: 
Technique:  Gene knockouts.
References:  68
Mice lacking ghrelin receptors resist the development of diet induced obesity.
Species:  Mouse
Tissue: 
Technique:  Gene knockouts.
References:  98
Ablation of ghrelin receptor in leptin-deficient ob/ob mice has paradoxical effects on glucose homeostasis whencompared with ablation of ghrelin in ob/ob mice.
Species:  Mouse
Tissue: 
Technique:  Gene knockouts.
References:  48
Impaired wake-promoting mechanisms in ghrelin receptor-deficient mice.
Species:  Mouse
Tissue: 
Technique:  Not specified.
References:  21
Ablation of ghrelin receptor reduces adiposity and improves insulin sensitivity during aging by regulating fat metabolism in white and brown adipose tissues.
Species:  Mouse
Tissue: 
Technique:  Gene knockouts.
References:  45
Ghrelin is produced in taste cells and ghrelin receptor null mice show reduced taste responsivity to salty (NaCl) and sour (citric acid) tastants.
Species:  Mouse
Tissue: 
Technique:  Gene knockouts.
References:  72
Unacylated ghrelin rapidly modulates lipogenic and insulin signaling pathway gene expression in metabolically active tissues of Ghsr deleted mice.
Species:  Mouse
Tissue: 
Technique:  Gene knockouts.
References:  12
Improved insulin sensitivity and metabolic flexibility in ghrelin receptor knockout mice.
Species:  Mouse
Tissue: 
Technique:  Gene knockouts.
References:  47
Physiological Consequences of Altering Gene Expression Comments
Characterization of adult ghrelin and ghrelin receptor knockout mice under positive and negative energy balance [77].
Phenotypes, Alleles and Disease Models Click here for help Mouse data from MGI

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Allele Composition & genetic background Accession Phenotype Id Phenotype Reference
Ghsrtm1.1Lex Ghsrtm1.1Lex/Ghsrtm1.1Lex
involves: 129S4/SvJae * 129S5/SvEvBrd * C57BL/6
MGI:2441906  MP:0001663 abnormal digestive system physiology PMID: 18657539 
Ghsrtm1Lowl Ghsrtm1Lowl/Ghsrtm1Lowl
involves: C57BL/6J
MGI:2441906  MP:0005450 abnormal energy expenditure PMID: 16322794 
Ghsrtm1Rgs Ghsrtm1Rgs/Ghsrtm1Rgs
involves: 129/Sv * C57BL/6J
MGI:2441906  MP:0005449 abnormal food intake PMID: 15070777 
Ghsrtm1Rgs Ghsrtm1Rgs/Ghsrtm1Rgs
involves: 129/Sv * C57BL/6J
MGI:2441906  MP:0003968 abnormal growth hormone level PMID: 15070777 
Ghsrtm1Mws Ghsrtm1Mws/Ghsrtm1Mws
Not Specified
MGI:2441906  MP:0002803 abnormal operant conditional behavior PMID: 19633195 
Ghsrtm1.1Lex Ghsrtm1.1Lex/Ghsrtm1.1Lex
involves: 129S4/SvJae * 129S5/SvEvBrd * C57BL/6
MGI:2441906  MP:0008872 abnormal physiological response to xenobiotic PMID: 18657539 
Ghsrtm1Rgs Ghsrtm1Rgs/Ghsrtm1Rgs
involves: 129/Sv * C57BL/6J
MGI:2441906  MP:0003638 abnormal response/metabolism to endogenous compounds PMID: 15070777 
Ghsrtm1Lowl Ghsrtm1Lowl/Ghsrtm1Lowl
involves: C57BL/6J
MGI:2441906  MP:0003638 abnormal response/metabolism to endogenous compounds PMID: 16322794 
Ghsrtm1Rgs Ghsrtm1Rgs/Ghsrtm1Rgs
involves: 129/Sv * C57BL/6J
MGI:2441906  MP:0001262 decreased body weight PMID: 15070777 
Ghsrtm1Lowl Ghsrtm1Lowl/Ghsrtm1Lowl
involves: C57BL/6J
MGI:2441906  MP:0001262 decreased body weight PMID: 16322794 
Ghsrtm1Lowl Ghsrtm1Lowl/Ghsrtm1Lowl
involves: C57BL/6J
MGI:2441906  MP:0005560 decreased circulating glucose level PMID: 16322794 
Ghsrtm1Rgs Ghsrtm1Rgs/Ghsrtm1Rgs
involves: 129/Sv * C57BL/6J
MGI:2441906  MP:0004701 decreased circulating insulin-like growth factor I level PMID: 15070777 
Ghsrtm1Lowl Ghsrtm1Lowl/Ghsrtm1Lowl
involves: C57BL/6J
MGI:2441906  MP:0003910 decreased eating behavior PMID: 16322794 
Ghsrtm1Lowl Ghsrtm1Lowl/Ghsrtm1Lowl
involves: C57BL/6J
MGI:2441906  MP:0010379 decreased respiratory quotient PMID: 16322794 
Ghsrtm1Lowl Ghsrtm1Lowl/Ghsrtm1Lowl
involves: C57BL/6J
MGI:2441906  MP:0010025 decreased total body fat amount PMID: 16322794 
Ghsrtm1Lowl Ghsrtm1Lowl/Ghsrtm1Lowl
involves: C57BL/6J
MGI:2441906  MP:0001402 hypoactivity PMID: 16322794 
Ghsrtm1Lowl Ghsrtm1Lowl/Ghsrtm1Lowl
involves: C57BL/6J
MGI:2441906  MP:0005659 increased resistance to diet-induced obesity PMID: 16322794 
Clinically-Relevant Mutations and Pathophysiology Click here for help
Disease:  Growth hormone deficiency, isolated partial; GHDP
Synonyms: Short stature due to GHSR deficiency [Orphanet: ORPHA314811]
OMIM: 615925
Orphanet: ORPHA314811
Biologically Significant Variants Click here for help
Type:  Splice variant
Species:  Human
Description:  GHSR1(b) is derived from the GHSR gene by alternative splicing. The splice variant has only five transmembrane domains and does not bind or is activated by ghrelin or other growth hormone secretagogues. GHSR1(b) mRNA however is widely expressed.
References:  26,33
General Comments
The role of endothelial vasodilators in mediating ghrelin-induced vasodilatation is not clear.

References

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1. Baldanzi G, Filigheddu N, Cutrupi S, Catapano F, Bonissoni S, Fubini A, Malan D, Baj G, Granata R, Broglio F et al.. (2002) Ghrelin and des-acyl ghrelin inhibit cell death in cardiomyocytes and endothelial cells through ERK1/2 and PI 3-kinase/AKT. J Cell Biol, 159 (6): 1029-37. [PMID:12486113]

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