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Chemical Compound Review

Hexarelin     (2S)-6-amino-2-[[2-[[(2S)-2- [[(2S)-2...

Synonyms: AC1NUYYT, SureCN3049733, LS-191993, AKOS015896043, I06-1821, ...
 
 
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Disease relevance of Examorelin

 

Psychiatry related information on Examorelin

  • In contrast, the women with anorexia nervosa showed a normal GH response after the two stimuli: hexarelin 64.8 +/- 9 [6].
  • Two well-known hexapeptides, GHRP-6 and hexarelin, given s.c., dose dependently stimulated both GH release and feeding behavior in satiated rats [7].
  • The aim of this study was to investigate the effect of a bolus injection of hexarelin given in the morning during wakefulness and during nocturnal sleep in a group of normal adult men [8].
 

High impact information on Examorelin

  • Growth hormone-releasing peptides (GHRPs) are a series of hepta (GHRP-1)- and hexapeptides (GHRP-2, GHRP-6, Hexarelin) that have been shown to be effective releasers of GH in animals and humans [9].
  • This finding correlates with the in vivo ACTH hyperresponsiveness to hexarelin (a GHS) [10].
  • In contrast, no competition was seen between radiolabeled Tyr-Ala-hexarelin and some peptides (CRF and insulin-like growth factor I) structurally and functionally unrelated to hexarelin or when GHRH and SRIF were tested in the displacement studies [11].
  • In these cell lines, ghrelin (as well as hexarelin, MK-0677, EP-80317, and even desoctanoyl ghrelin) caused a significant inhibition of cell proliferation at concentrations close to their binding affinity [11].
  • The family of GH secretagogues (GHS) includes synthetic peptidyl (hexarelin) and nonpeptidyl (MK-0677) molecules possessing specific receptors in the pituitary and central nervous system as well as in peripheral tissues, including the heart and some endocrine organs [11].
 

Chemical compound and disease context of Examorelin

  • METHODS AND SUBJECTS: The changes in GH and cortisol in response to insulin-induced hypoglycaemia (intravenous human Actrapid 0.15 IU/kg) and hexarelin (2 microg/kg) in 19 patients with possible pituitary disease (5 males, mean age 39 years, range 21-70) were compared [12].
  • Somatotrope responsiveness to Hexarelin, a synthetic hexapeptide, is refractory to the inhibitory effect of glucose in obesity [13].
  • In hearts subjected to 30 minutes of ischemia followed by 120 minutes of reperfusion, the synthetic peptidyl secretagogue hexarelin (1 microM) significantly reduced infarct size, as estimated on the basis of triphenyltetrazolium chloride staining, while the non-peptidyl secretagogue MK-0677 was ineffective [14].
  • Effects of alprazolam, a benzodiazepine, on the ACTH-, GH- and PRL-releasing activity of hexarelin, a synthetic peptidyl GH secretagogue (GHS), in patients with simple obesity and in patients with Cushing's disease [15].
 

Biological context of Examorelin

  • The GH response to 2 micrograms/kg hexarelin, i.v., was very reproducible (AUC, 4016 +/- 563 vs. 3959 +/- 803 micrograms/min.L) [16].
  • Hexarelin, MK 0677, and human ghrelin completely displaced the radioligand from binding sites of endocrine tissues, but MK 0677 and ghrelin were less potent than hexarelin [17].
  • GH gene expression was significantly increased (at least P < 0.05) by hexarelin, GHRH, and leptin (1000 and 100 nM) after 24 h of treatment [18].
  • Apparently, this causes the activation of paraventricular oxytocinergic neurons projecting to extra-hypothalamic brain areas and mediating penile erection, as found with dopamine agonists, oxytocin, excitatory amino acids and hexarelin analogue peptides [19].
  • Inasmuch as hexarelin has been reported to have protective effects in this process, we examined whether hexarelin can prevent cardiomyocytes from ANG II-induced cell death [20].
 

Anatomical context of Examorelin

  • [(125)I]-Tyr-Ala-hexarelin bound to tumor membranes was displaced by different unlabeled GHS such as hexarelin, Tyr-Ala-hexarelin, human ghrelin, and MK-0677 as well as by desoctanoyl-ghrelin and hexarelin derivative EP-80317, which are devoid of GH-releasing properties in vivo [11].
  • The family of GH secretagogues (GHS) includes peptidyl (hexarelin) and nonpeptidyl (MK 0677) molecules possessing specific receptors in the brain, pituitary, and thyroid [17].
  • There are no hints for an interaction of hexarelin and the immune system [21].
  • Moreover, hexarelin restored the firing capacity of fast-twitch muscle fibers, as did GH in previous studies [22].
  • Partial recovery of skeletal muscle sodium channel properties in aged rats chronically treated with growth hormone or the GH-secretagogue hexarelin [22].
 

Associations of Examorelin with other chemical compounds

 

Gene context of Examorelin

  • The peak serum GH concentration following the intravenous administration of hexarelin plus GHRH-(1-29)-NH2 remained large (52.6 +/- 7.2 mU/l; mean +/- SEM) despite the high dose of SS(1-14) (50 micrograms/m2/h) [27].
  • 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 [28].
  • Interaction of the growth hormone releasing peptide hexarelin with somatostatin [27].
  • GHSs stimulated hypothalamic AVP release (at 20 min control: 0. 99+/-0.06 ratio to basal release, 10-4 M concentration of GHRP-6: 6. 31+/-1, P<0.001, hexarelin: 1.88+/-0.4, P<0.01, L-692,429: 1.90+/-0. 5, P<0.05 and L-692,585: 2.34+/-0.96, P<0.01), while no stimulatory effect was found on CRH release [29].
  • While the binding of 125I-Tyr-Ala-hexarelin to pituitary membranes was completely displaced by unlabelled hexarelin, ghrelin and CST, none of the SRIH fragments tested inhibited this binding [30].
 

Analytical, diagnostic and therapeutic context of Examorelin

  • Intranasal administration of 20 micrograms/kg hexarelin induced GH release (AUC, 2642 +/- 452 micrograms/min.L) similar to that caused by 1 microgram/kg, i.v. Twenty and 40 mg hexarelin, po, produced a dose-related increase in GH levels (AUC, 2278 +/- 442 and 4079 +/- 514 micrograms/min.L) [16].
  • Growth hormone-releasing activity of hexarelin, a new synthetic hexapeptide, after intravenous, subcutaneous, intranasal, and oral administration in man [16].
  • Visual analog scales showed an acute small increment in appetite with hexarelin [26].
  • The effects of dose, nutrition, and age on hexarelin-induced anterior pituitary hormone secretion in adult patients on maintenance hemodialysis [31].
  • Ghrelin was far less effective than hexarelin in preventing increases in left ventricular end-diastolic pressure (15% and 60% protection for ghrelin and hexarelin, respectively), coronary perfusion pressure (10% and 45% reduction), and release of creatine kinase in the heart perfusate (15% and 55% reduction) [2].

References

  1. Low dose hexarelin and growth hormone (GH)-releasing hormone as a diagnostic tool for the diagnosis of GH deficiency in adults: comparison with insulin-induced hypoglycemia test. Gasperi, M., Aimaretti, G., Scarcello, G., Corneli, G., Cosci, C., Arvat, E., Martino, E., Ghigo, E. J. Clin. Endocrinol. Metab. (1999) [Pubmed]
  2. 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]
  3. The growth hormone secretagogue hexarelin improves cardiac function in rats after experimental myocardial infarction. Tivesten, A., Bollano, E., Caidahl, K., Kujacic, V., Sun, X.Y., Hedner, T., Hjalmarson, A., Bengtsson, B.A., Isgaard, J. Endocrinology (2000) [Pubmed]
  4. Growth hormone-releasing peptide hexarelin reduces neonatal brain injury and alters Akt/glycogen synthase kinase-3beta phosphorylation. Brywe, K.G., Leverin, A.L., Gustavsson, M., Mallard, C., Granata, R., Destefanis, S., Volante, M., Hagberg, H., Ghigo, E., Isgaard, J. Endocrinology (2005) [Pubmed]
  5. Endocrine, metabolic and cardioprotective effects of hexarelin in obese Zucker rats. De Gennaro-Colonna, V., Rossoni, G., Cocchi, D., Rigamonti, A.E., Berti, F., Muller, E.E. J. Endocrinol. (2000) [Pubmed]
  6. Absence of desensitization by hexarelin to subsequent GH releasing hormone-mediated GH secretion in patients with anorexia nervosa. Popovic, V., Micic, D., Djurovic, M., Obradovic, S., Casanueva, F.F., Dieguez, C. Clin. Endocrinol. (Oxf) (1997) [Pubmed]
  7. Novel hexarelin analogs stimulate feeding in the rat through a mechanism not involving growth hormone release. Torsello, A., Luoni, M., Schweiger, F., Grilli, R., Guidi, M., Bresciani, E., Deghenghi, R., Müller, E.E., Locatelli, V. Eur. J. Pharmacol. (1998) [Pubmed]
  8. Acute administration of hexarelin stimulates GH secretion during day and night in normal men. Loche, S., Colao, A., Cappa, M., Ferone, D., Merola, B., Faedda, A., Imbimbo, B.P., Deghenghi, R., Lombardi, G. Clin. Endocrinol. (Oxf) (1997) [Pubmed]
  9. Growth hormone-releasing peptides and their analogs. Camanni, F., Ghigo, E., Arvat, E. Frontiers in neuroendocrinology. (1998) [Pubmed]
  10. Cyclical Cushing's syndrome in a patient with a bronchial neuroendocrine tumor (typical carcinoid) expressing ghrelin and growth hormone secretagogue receptors. Arnaldi, G., Mancini, T., Kola, B., Appolloni, G., Freddi, S., Concettoni, C., Bearzi, I., Masini, A., Boscaro, M., Mantero, F. J. Clin. Endocrinol. Metab. (2003) [Pubmed]
  11. Identification, characterization, and biological activity of specific receptors for natural (ghrelin) and synthetic growth hormone secretagogues and analogs in human breast carcinomas and cell lines. Cassoni, P., Papotti, M., Ghè, C., Catapano, F., Sapino, A., Graziani, A., Deghenghi, R., Reissmann, T., Ghigo, E., Muccioli, G. J. Clin. Endocrinol. Metab. (2001) [Pubmed]
  12. Hexarelin as a test of pituitary reserve in patients with pituitary disease. Korbonits, M., Kaltsas, G., Perry, L.A., Grossman, A.B., Monson, J.P., Besser, G.M., Trainer, P.J. Clin. Endocrinol. (Oxf) (1999) [Pubmed]
  13. Somatotrope responsiveness to Hexarelin, a synthetic hexapeptide, is refractory to the inhibitory effect of glucose in obesity. Grottoli, S., Maccario, M., Procopio, M., Oleandri, S.E., Arvat, E., Gianotti, L., Deghenghi, R., Camanni, F., Ghigo, E. Eur. J. Endocrinol. (1996) [Pubmed]
  14. Effect of ghrelin and synthetic growth hormone secretagogues in normal and ischemic rat heart. Frascarelli, S., Ghelardoni, S., Ronca-Testoni, S., Zucchi, R. Basic Res. Cardiol. (2003) [Pubmed]
  15. Effects of alprazolam, a benzodiazepine, on the ACTH-, GH- and PRL-releasing activity of hexarelin, a synthetic peptidyl GH secretagogue (GHS), in patients with simple obesity and in patients with Cushing's disease. Grottoli, S., Arvat, E., Gauna, C., Maccagno, B., Ramunni, J., Giordano, R., Maccario, M., Deghenghi, R., Ghigo, E. Pituitary (1999) [Pubmed]
  16. Growth hormone-releasing activity of hexarelin, a new synthetic hexapeptide, after intravenous, subcutaneous, intranasal, and oral administration in man. Ghigo, E., Arvat, E., Gianotti, L., Imbimbo, B.P., Lenaerts, V., Deghenghi, R., Camanni, F. J. Clin. Endocrinol. Metab. (1994) [Pubmed]
  17. Growth hormone secretagogue binding sites in peripheral human tissues. Papotti, M., Ghè, C., Cassoni, P., Catapano, F., Deghenghi, R., Ghigo, E., Muccioli, G. J. Clin. Endocrinol. Metab. (2000) [Pubmed]
  18. Leptin regulates GH gene expression and secretion and nitric oxide production in pig pituitary cells. Baratta, M., Saleri, R., Mainardi, G.L., Valle, D., Giustina, A., Tamanini, C. Endocrinology (2002) [Pubmed]
  19. Pro-VGF-derived peptides induce penile erection in male rats: Involvement of paraventricular nitric oxide. Succu, S., Mascia, M.S., Melis, T., Sanna, F., Melis, M.R., Possenti, R., Argiolas, A. Neuropharmacology (2005) [Pubmed]
  20. Hexarelin protects rat cardiomyocytes from angiotensin II-induced apoptosis in vitro. Pang, J.J., Xu, R.K., Xu, X.B., Cao, J.M., Ni, C., Zhu, W.L., Asotra, K., Chen, M.C., Chen, C. Am. J. Physiol. Heart Circ. Physiol. (2004) [Pubmed]
  21. Hexarelin decreases slow-wave sleep and stimulates the secretion of GH, ACTH, cortisol and prolactin during sleep in healthy volunteers. Frieboes, R.M., Antonijevic, I.A., Held, K., Murck, H., Pollmächer, T., Uhr, M., Steiger, A. Psychoneuroendocrinology (2004) [Pubmed]
  22. Partial recovery of skeletal muscle sodium channel properties in aged rats chronically treated with growth hormone or the GH-secretagogue hexarelin. Desaphy, J.F., De Luca, A., Pierno, S., Imbrici, P., Camerino, D.C. J. Pharmacol. Exp. Ther. (1998) [Pubmed]
  23. Hexarelin-induced growth hormone, cortisol, and prolactin release: a dose-response study. Massoud, A.F., Hindmarsh, P.C., Brook, C.G. J. Clin. Endocrinol. Metab. (1996) [Pubmed]
  24. Growth hormone status during long-term hexarelin therapy. Rahim, A., O'Neill, P.A., Shalet, S.M. J. Clin. Endocrinol. Metab. (1998) [Pubmed]
  25. Arginine and growth hormone-releasing hormone restore the blunted growth hormone-releasing activity of hexarelin in elderly subjects. Arvat, E., Gianotti, L., Grottoli, S., Imbimbo, B.P., Lenaerts, V., Deghenghi, R., Camanni, F., Ghigo, E. J. Clin. Endocrinol. Metab. (1994) [Pubmed]
  26. The growth hormone secretagogue hexarelin stimulates the hypothalamo-pituitary-adrenal axis via arginine vasopressin. Korbonits, M., Kaltsas, G., Perry, L.A., Putignano, P., Grossman, A.B., Besser, G.M., Trainer, P.J. J. Clin. Endocrinol. Metab. (1999) [Pubmed]
  27. Interaction of the growth hormone releasing peptide hexarelin with somatostatin. Massoud, A.F., Hindmarsh, P.C., Brook, C.G. Clin. Endocrinol. (Oxf) (1997) [Pubmed]
  28. 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., Maccagno, B., Ramunni, J., Di Vito, L., Broglio, F., Deghenghi, R., Camanni, F., Ghigo, E. Neuroendocrinology (1997) [Pubmed]
  29. The effect of growth hormone secretagogues and neuropeptide Y on hypothalamic hormone release from acute rat hypothalamic explants. Korbonits, M., Little, J.A., Forsling, M.L., Tringali, G., Costa, A., Navarra, P., Trainer, P.J., Grossman, A.B. J. Neuroendocrinol. (1999) [Pubmed]
  30. Cortistatin, but not somatostatin, binds to growth hormone secretagogue (GHS) receptors of human pituitary gland. Deghenghi, R., Papotti, M., Ghigo, E., Muccioli, G. J. Endocrinol. Invest. (2001) [Pubmed]
  31. The effects of dose, nutrition, and age on hexarelin-induced anterior pituitary hormone secretion in adult patients on maintenance hemodialysis. Jenkins, R.C., El Nahas, A.M., Wilkie, M.E., Brown, C.B., Jones, J., Ghigo, E., Ross, R.J. J. Clin. Endocrinol. Metab. (1999) [Pubmed]
 
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