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Gene Review

Ghsr  -  growth hormone secretagogue receptor

Rattus norvegicus

Synonyms: GH-releasing peptide receptor, GHRP, GHS-R, Ghrelin receptor, Growth hormone secretagogue receptor type 1
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Disease relevance of Ghsr


Psychiatry related information on Ghsr


High impact information on Ghsr


Chemical compound and disease context of Ghsr


Biological context of Ghsr

  • A full-length contiguous cDNA from rat hypothalamus was isolated and shown to be identical in its nucleotide and deduced amino acid sequence to the rat pituitary GHS-R [9].
  • A single intron of approximately 2 kb divides the open reading frame into two exons encoding TM 1-5 and TM 6-7, thus placing the GHS-R into the intron-containing class of GPC-Rs [9].
  • In addition, determination of the nucleotide sequence for the human GHS-R gene confirmed the position of an intron in the human GHS-R gene at this position [9].
  • Hypothalamic GHS-R mRNA levels increased with age but exhibited no significant sex difference at each age tested [11].
  • These results suggest that GHRH-R is vital for GHRH-induced GH secretion but only partially involved in GHRP-2-stimulated GH secretion under the condition of down-regulation of GHS-R gene transcription [12].

Anatomical context of Ghsr

  • GHS-R mRNA is prominently expressed in arcuate (ARC) and ventromedial nuclei (VMN) and in hippocampus, but not in the periventricular nucleus [13].
  • In conclusion, the expression of GHS-R in rat adipocytes increases with the age and during adipogenesis [14].
  • The levels of GHS-R mRNA increased by up to 4-fold in adipose tissue from epididymal and parametrial regions as the rat aged from 4-20 wk and were significantly elevated during the differentiation of preadipocytes in vitro [14].
  • In addition, cellular distribution of GHS-R within adult testis tissue was assessed [15].
  • Reverse transcription-polymerase chain reaction demonstrated the expression of ghrelin and GHS-R in the rat adrenal cortex, and high adrenal concentrations of immunoreactive ghrelin were detected by radioimmune assay (RIA) [16].

Associations of Ghsr with chemical compounds

  • In addition, GH-releasing peptides, such as GHRP-6 and the nonpeptide mimetics, L-692,429 and MK-0677, stimulate GH release through their activation of a distinct receptor, the GH secretagogue receptor (GHS-R) [9].
  • Taken together, these data demonstrate that changes in the levels of pituitary GHS-R mRNA, but not GHRH-R mRNA, are associated with changes in the gonadal steroid environment, thereby implicating the GHS/GHS-R signalling system as a control point in the establishment and maintenance of sexually dimorphic patterns of GH secretion [11].
  • In the present study, the effect of i.c.v. injection of different ghrelins including chicken and bullfrog ghrelin, and synthetic GH-releasing peptide (GHRP) on feeding of neonatal chicks was investigated [17].
  • Although the actions of dermorphin, 2549, and GHRP on GH release are GHRH dependent, release of endogenous GHRH does not explain how GH is released synergistically by the combination of these peptides [18].
  • Hexarelin modulates the expression of growth hormone secretagogue receptor type 1a mRNA at hypothalamic and pituitary sites [19].

Regulatory relationships of Ghsr


Other interactions of Ghsr

  • GH secretagogue (GHS)/ghrelin stimulates GH secretion by binding mainly to its receptor (GHS-R) on GHRH neurons in the arcuate nucleus (Arc) of the hypothalamus [1].
  • GHRH-R mRNA levels were comparable in males and females within each age while GHS-R mRNA levels were gender dependent [11].
  • These results indicate that the chicken GHS receptor is affected by several forms of GHS, and that food intake of neonatal chicks is inhibited by GHS receptor agonists [17].
  • Taken together, these results indicate that GHRH-induced up-regulation of pituitary GHS-R synthesis in vivo is indirect and independent of both somatostatin and GH [25].
  • Stimulation of the arcuate NPY neurons via GHS-R may explain the increased appetite and the cortisol release seen after administration of some GHS compounds [21].

Analytical, diagnostic and therapeutic context of Ghsr

  • We demonstrate that our lead compound, L-NOX-B11, binds ghrelin with low-nanomolar affinity and inhibits ghrelin-mediated GHS-receptor activation in cell culture with an IC(50) of 5 nM. l-NOX-B11 is highly specific for the bioactive, n-octanoylated form of ghrelin [26].
  • Serum was analyzed for GH, pituitaries were collected, and GHS-R and GHRH receptor (GHRH-R) messenger RNA (mRNA) levels were determined by RT-PCR [25].
  • Accordingly, we examined the effects of GHRP and PACAP on GH secretion at the single cell level using the reverse hemolytic plaque assay which allows distinction of effects on the number of secreting cells and the amount of hormone each cell secretes [27].
  • The calcium response of cardiocytes to GHRP was visualized using confocal microscopy [28].
  • At these times, the mean log pituitary GHS-R mRNA contents were significantly lower in the GC rat group than in the control group [29].


  1. Growth hormone-releasing hormone (GHRH) neurons in the arcuate nucleus (Arc) of the hypothalamus are decreased in transgenic rats whose expression of ghrelin receptor is attenuated: Evidence that ghrelin receptor is involved in the up-regulation of GHRH expression in the arc. Mano-Otagiri, A., Nemoto, T., Sekino, A., Yamauchi, N., Shuto, Y., Sugihara, H., Oikawa, S., Shibasaki, T. Endocrinology (2006) [Pubmed]
  2. Upregulation of cardiovascular ghrelin receptor occurs in the hyperdynamic phase of sepsis. Wu, R., Zhou, M., Cui, X., Simms, H.H., Wang, P. Am. J. Physiol. Heart Circ. Physiol. (2004) [Pubmed]
  3. Antiproliferative and GH-inhibitory activity of chimeric peptides consisting of GHRP-6 and somatostatin. Dasgupta, P., Singh, A.T., Mukherjee, R. Biochem. Biophys. Res. Commun. (1999) [Pubmed]
  4. Identification and characterization of a new growth hormone-releasing peptide receptor in the heart. Bodart, V., Bouchard, J.F., McNicoll, N., Escher, E., Carrière, P., Ghigo, E., Sejlitz, T., Sirois, M.G., Lamontagne, D., Ong, H. Circ. Res. (1999) [Pubmed]
  5. Ghrelin plays a minor role in the physiological control of cardiac function in the rat. Torsello, A., Bresciani, E., Rossoni, G., Avallone, R., Tulipano, G., Cocchi, D., Bulgarelli, I., Deghenghi, R., Berti, F., Locatelli, V. Endocrinology (2003) [Pubmed]
  6. Ghrelin induces fasted motor activity of the gastrointestinal tract in conscious fed rats. Fujino, K., Inui, A., Asakawa, A., Kihara, N., Fujimura, M., Fujimiya, M. J. Physiol. (Lond.) (2003) [Pubmed]
  7. The role of the gastric afferent vagal nerve in ghrelin-induced feeding and growth hormone secretion in rats. Date, Y., Murakami, N., Toshinai, K., Matsukura, S., Niijima, A., Matsuo, H., Kangawa, K., Nakazato, M. Gastroenterology (2002) [Pubmed]
  8. Regulation of growth hormone secretagogue receptor gene expression in the arcuate nuclei of the rat by leptin and ghrelin. Nogueiras, R., Tovar, S., Mitchell, S.E., Rayner, D.V., Archer, Z.A., Dieguez, C., Williams, L.M. Diabetes (2004) [Pubmed]
  9. Molecular analysis of rat pituitary and hypothalamic growth hormone secretagogue receptors. McKee, K.K., Palyha, O.C., Feighner, S.D., Hreniuk, D.L., Tan, C.P., Phillips, M.S., Smith, R.G., Van der Ploeg, L.H., Howard, A.D. Mol. Endocrinol. (1997) [Pubmed]
  10. GH-releasing peptides improve cardiac dysfunction and cachexia and suppress stress-related hormones and cardiomyocyte apoptosis in rats with heart failure. Xu, X.B., Pang, J.J., Cao, J.M., Ni, C., Xu, R.K., Peng, X.Z., Yu, X.X., Guo, S., Chen, M.C., Chen, C. Am. J. Physiol. Heart Circ. Physiol. (2005) [Pubmed]
  11. Growth hormone-releasing hormone receptor (GHRH-R) and growth hormone secretagogue receptor (GHS-R) mRNA levels during postnatal development in male and female rats. Kamegai, J., Wakabayashi, I., Kineman, R.D., Frohman, L.A. J. Neuroendocrinol. (1999) [Pubmed]
  12. Is GHRH receptor essential to GHRP-2-induced GH secretion in primary cultured rat pituitary cells? Roh, S.G., Chen, C., Choi, K.C., Shrestha, Y., Sasaki, S. Endocrinology (2002) [Pubmed]
  13. Hypothalamic growth hormone secretagogue-receptor (GHS-R) expression is regulated by growth hormone in the rat. Bennett, P.A., Thomas, G.B., Howard, A.D., Feighner, S.D., van der Ploeg, L.H., Smith, R.G., Robinson, I.C. Endocrinology (1997) [Pubmed]
  14. The role of ghrelin and growth hormone secretagogues receptor on rat adipogenesis. Choi, K., Roh, S.G., Hong, Y.H., Shrestha, Y.B., Hishikawa, D., Chen, C., Kojima, M., Kangawa, K., Sasaki, S. Endocrinology (2003) [Pubmed]
  15. Developmental, stage-specific, and hormonally regulated expression of growth hormone secretagogue receptor messenger RNA in rat testis. Barreiro, M.L., Suominen, J.S., Gaytán, F., Pinilla, L., Chopin, L.K., Casanueva, F.F., Diéguez, C., Aguilar, E., Toppari, J., Tena-Sempere, M. Biol. Reprod. (2003) [Pubmed]
  16. Ghrelin and growth hormone secretagogue receptor are expressed in the rat adrenal cortex: Evidence that ghrelin stimulates the growth, but not the secretory activity of adrenal cells. Andreis, P.G., Malendowicz, L.K., Trejter, M., Neri, G., Spinazzi, R., Rossi, G.P., Nussdorfer, G.G. FEBS Lett. (2003) [Pubmed]
  17. Chicken ghrelin and growth hormone-releasing peptide-2 inhibit food intake of neonatal chicks. Saito, E.S., Kaiya, H., Takagi, T., Yamasaki, I., Denbow, D.M., Kangawa, K., Furuse, M. Eur. J. Pharmacol. (2002) [Pubmed]
  18. On the actions of the growth hormone-releasing hexapeptide, GHRP. Bowers, C.Y., Sartor, A.O., Reynolds, G.A., Badger, T.M. Endocrinology (1991) [Pubmed]
  19. Hexarelin modulates the expression of growth hormone secretagogue receptor type 1a mRNA at hypothalamic and pituitary sites. Bresciani, E., Nass, R., Torsello, A., Gaylinn, B., Avallone, R., Locatelli, V., Thorner, M.O., Müller, E.E. Neuroendocrinology (2004) [Pubmed]
  20. Expression of growth hormone secretagogue-receptors by growth hormone-releasing hormone neurons in the mediobasal hypothalamus. Tannenbaum, G.S., Lapointe, M., Beaudet, A., Howard, A.D. Endocrinology (1998) [Pubmed]
  21. Co-localization of growth hormone secretagogue receptor and NPY mRNA in the arcuate nucleus of the rat. Willesen, M.G., Kristensen, P., Rømer, J. Neuroendocrinology (1999) [Pubmed]
  22. Insulin-like growth factor-I down-regulates ghrelin receptor (growth hormone secretagogue receptor) expression in the rat pituitary. Kamegai, J., Tamura, H., Shimizu, T., Ishii, S., Sugihara, H., Oikawa, S. Regul. Pept. (2005) [Pubmed]
  23. Adipogenic and orexigenic effects of the ghrelin-receptor ligand tabimorelin are diminished in leptin-signalling-deficient ZDF rats. Holm, A.M., Johansen, P.B., Ahnfelt-Rønne, I., Rømer, J. Eur. J. Endocrinol. (2004) [Pubmed]
  24. Ghrelin receptor agonist GHRP-2 prevents arthritis-induced increase in E3 ubiquitin-ligating enzymes MuRF1 and MAFbx gene expression in skeletal muscle. Granado, M., Priego, T., Martín, A.I., Villanúa, M.A., López-Calderón, A. Am. J. Physiol. Endocrinol. Metab. (2005) [Pubmed]
  25. Growth hormone (GH)-releasing hormone (GHRH) and the GH secretagogue (GHS), L692,585, differentially modulate rat pituitary GHS receptor and GHRH receptor messenger ribonucleic acid levels. Kineman, R.D., Kamegai, J., Frohman, L.A. Endocrinology (1999) [Pubmed]
  26. Inhibition of ghrelin action in vitro and in vivo by an RNA-Spiegelmer. Helmling, S., Maasch, C., Eulberg, D., Buchner, K., Schröder, W., Lange, C., Vonhoff, S., Wlotzka, B., Tschöp, M.H., Rosewicz, S., Klussmann, S. Proc. Natl. Acad. Sci. U.S.A. (2004) [Pubmed]
  27. Pituitary adenylate cyclase activating polypeptide, growth hormone (GH)-releasing peptide and GH-releasing hormone stimulate GH release through distinct pituitary receptors. Goth, M.I., Lyons, C.E., Canny, B.J., Thorner, M.O. Endocrinology (1992) [Pubmed]
  28. The positive inotropic and calcium-mobilizing effects of growth hormone-releasing peptides on rat heart. Xu, X.B., Cao, J.M., Pang, J.J., Xu, R.K., Ni, C., Zhu, W.L., Asotra, K., Chen, M.C., Chen, C. Endocrinology (2003) [Pubmed]
  29. High plasma growth hormone (GH) levels inhibit expression of GH secretagogue receptor messenger ribonucleic acid levels in the rat pituitary. Nass, R., Gilrain, J., Anderson, S., Gaylinn, B., Dalkin, A., Day, R., Peruggia, M., Thorner, M.O. Endocrinology (2000) [Pubmed]
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