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Chemical Compound Review

Pralmorelin     (2S)-6-amino-2-[[(2R)-2- [[(2S)-2-[[(2S)-2...

Synonyms: GHRP 2, GHRP-2 Acetate, SureCN3055328, AC1NUU5W, KP 102, ...
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Disease relevance of Pralmorelin


Psychiatry related information on Pralmorelin


High impact information on Pralmorelin

  • However, antagonism of the GHRH-receptor and of protein kinase A with (N-Ac-Tyr1,D-Arg2)GRF-(1-29)-NH2 and Rp-adenosine-3',5'-cyclic monophosphothioate, respectively, did not alter the stimulatory effects of GHRP-2 and GHRP-6 on GH secretion [6].
  • The effect of GHRP-2 and/or GHRP-6 on cAMP production was studied in 15 tumors, seven of which possessed constitutive adenylyl cyclase activity as evidenced by presence of gsp oncogenes [6].
  • The effects of the synthetic GH-releasing peptides, GHRP-2 and GHRP-6, on phosphatidylinositol (PI) hydrolysis and cAMP production have been examined in human pituitary somatotropinomas with and without adenylyl cyclase-activating gsp oncogenes [6].
  • As expected, serum GH levels rose significantly during GHRP-2 infusion (AUC 5550 +/- 1090 microg/L/240 min vs. 412 +/- 161 microg/L/240 min, p = 0.003) [1].
  • Growth hormone releasing peptide-2 (GHRP-2), like ghrelin, increases food intake in healthy men [1].

Chemical compound and disease context of Pralmorelin


Biological context of Pralmorelin


Anatomical context of Pralmorelin


Associations of Pralmorelin with other chemical compounds

  • To this end, seven healthy postmenopausal women underwent frequent (10-min) blood sampling for 24 h during simultaneous i.v. infusion of GHRH and GHRP-2 each at a rate of 1 microg/kg x h on d 10 of randomly ordered placebo or 17beta-estradiol (E2) (1 mg orally twice daily) replacement [15].
  • As an indirect probe of estrogen-regulated hypothalamic somatostatin restraint, the present study monitors the ability of short-term oral E2 supplementation to modulate GH secretion during combined continuous stimulation by recombinant human GHRH [GHRH-(1-44)-amide] and the potent and selective synthetic GH-releasing peptide, GHRP-2 [15].
  • Estrogen's disruption of the orderliness of sequential GH pulse-mass values during fixed GHRH/GHRP-2 feedforward would be consistent with a subtle reduction in the release and/or actions of hypothalamic somatostatin or an (unexpected) direct pituitary action of the sex steroid [15].
  • In conclusion, our results demonstrate that, in man, GHRP-2 and HEX have similar, 2 and HEX is not fully specific, as they induce similar increases in PRL, ACTH and cortisol levels [16].
  • The effect of a newly developed growth hormone (GH)-releasing hexapeptide (KP-102) on GH secretion was studied in urethan-anesthetized adult male rats [17].

Gene context of Pralmorelin

  • In contrast, ApEn analysis of the evolution of successive GH secretory burst-mass values over 24 h disclosed that E2 replacement disrupts the serial regularity of pulsatile GH output (elevates the ApEn ratio) during combined GHRH/GHRP-2 stimulation (P = 0.004) [15].
  • Because such adiposity was thought to be mediated by hypothalamic NPY neurons, we investigated by which mechanism a synthetic ghrelin receptor agonist, GHRP-2, would generate a positive energy balance in NPY-deficient [Npy(-/-) mice] and wild-type controls [18].
  • Hypothalamic mRNA levels of agouti- related protein (AGRP), an orexigenic melanocortin receptor antagonist, increased after GHRP-2 treatment [18].
  • KP-102 (GHRP-2: pralmorelin) is a synthetic growth hormone releasing peptide (GHRP) that powerfully stimulates the release of GH by acting (i.v.) at both hypothalamic and pituitary sites [14].
  • Conversely, a CRF antagonist markedly inhibited KP-102-induced ACTH release in conscious rats, whereas an AVP antagonist or anti-AVP antiserum did not [14].

Analytical, diagnostic and therapeutic context of Pralmorelin


  1. Growth hormone releasing peptide-2 (GHRP-2), like ghrelin, increases food intake in healthy men. Laferrère, B., Abraham, C., Russell, C.D., Bowers, C.Y. J. Clin. Endocrinol. Metab. (2005) [Pubmed]
  2. Pretreatment with growth hormone-releasing peptide-2 directly protects against the diastolic dysfunction of myocardial stunning in an isolated, blood-perfused rabbit heart model. Weekers, F., Van Herck, E., Isgaard, J., Van den Berghe, G. Endocrinology (2000) [Pubmed]
  3. KP-102 (growth hormone-releasing peptide-2) attenuates ischemia/reperfusion injury in isolated rat hearts. Furuta, S., Hori, T., Ohyama, T. Naunyn Schmiedebergs Arch. Pharmacol. (2006) [Pubmed]
  4. Growth hormone-releasing peptide-2 infusion synchronizes growth hormone, thyrotrophin and prolactin release in prolonged critical illness. Van den Berghe, G., Wouters, P., Bowers, C.Y., de Zegher, F., Bouillon, R., Veldhuis, J.D. Eur. J. Endocrinol. (1999) [Pubmed]
  5. Neurokinin receptor antagonists inhibit the binding of growth hormone-releasing peptide to EP-1 human neuroblastoma cells. Tai, S., Kaji, H., Okimura, Y., Abe, H., Chihara, K. Biochem. Biophys. Res. Commun. (1995) [Pubmed]
  6. Protein kinase C-dependent growth hormone releasing peptides stimulate cyclic adenosine 3',5'-monophosphate production by human pituitary somatotropinomas expressing gsp oncogenes: evidence for crosstalk between transduction pathways. Adams, E.F., Lei, T., Buchfelder, M., Bowers, C.Y., Fahlbusch, R. Mol. Endocrinol. (1996) [Pubmed]
  7. Pharmacological characteristics of KP-102 (GHRP-2), a potent growth hormone-releasing peptide. Doi, N., Hirotani, C., Ukai, K., Shimada, O., Okuno, T., Kurasaki, S., Kiyofuji, T., Ikegami, R., Futamata, M., Nakagawa, T., Ase, K., Chihara, K. Arzneimittel-Forschung. (2004) [Pubmed]
  8. Pharmacokinetics and pharmacodynamics of growth hormone-releasing peptide-2: a phase I study in children. Pihoker, C., Kearns, G.L., French, D., Bowers, C.Y. J. Clin. Endocrinol. Metab. (1998) [Pubmed]
  9. 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]
  10. The role of protein kinase C in GH secretion induced by GH-releasing factor and GH-releasing peptides in cultured ovine somatotrophs. Wu, D., Clarke, I.J., Chen, C. J. Endocrinol. (1997) [Pubmed]
  11. Effects of growth hormone-releasing peptide-2 (GHRP-2) on membrane Ca2+ permeability in cultured ovine somatotrophs. Chen, C., Clarke, I.J. J. Neuroendocrinol. (1995) [Pubmed]
  12. The growth hormone-releasing peptide KP-102 induces c-fos expression in the arcuate nucleus. Kamegai, J., Hasegawa, O., Minami, S., Sugihara, H., Wakabayashi, I. Brain Res. Mol. Brain Res. (1996) [Pubmed]
  13. Anti-inflammatory effect of the ghrelin agonist growth hormone-releasing peptide-2 (GHRP-2) in arthritic rats. Granado, M., Priego, T., Martín, A.I., Villanúa, M.A., López-Calderón, A. Am. J. Physiol. Endocrinol. Metab. (2005) [Pubmed]
  14. ACTH releasing activity of KP-102 (GHRP-2) in rats is mediated mainly by release of CRF. Hirotani, C., Oki, Y., Ukai, K., Okuno, T., Kurasaki, S., Ohyama, T., Doi, N., Sasaki, K., Ase, K. Naunyn Schmiedebergs Arch. Pharmacol. (2005) [Pubmed]
  15. Impact of estradiol supplementation on dual peptidyl drive of GH secretion in postmenopausal women. Veldhuis, J.D., Evans, W.S., Bowers, C.Y. J. Clin. Endocrinol. Metab. (2002) [Pubmed]
  16. Effects of GHRP-2 and hexarelin, two synthetic GH-releasing peptides, on GH, prolactin, ACTH and cortisol levels in man. Comparison with the effects of GHRH, TRH and hCRH. Arvat, E., di Vito, L., Maccagno, B., Broglio, F., Boghen, M.F., Deghenghi, R., Camanni, F., Ghigo, E. Peptides (1997) [Pubmed]
  17. Effect of D-Ala-D-beta Nal-Ala-Trp-D-Phe-Lys-NH2 (KP-102) on GH secretion in urethan-anesthetized rats. Sawada, H., Sugihara, H., Onose, H., Minami, S., Shibasaki, T., Wakabayashi, I. Regul. Pept. (1994) [Pubmed]
  18. GH-releasing peptide-2 increases fat mass in mice lacking NPY: indication for a crucial mediating role of hypothalamic agouti-related protein. Tschöp, M., Statnick, M.A., Suter, T.M., Heiman, M.L. Endocrinology (2002) [Pubmed]
  19. Joint mechanisms of impaired growth-hormone pulse renewal in aging men. Veldhuis, J.D., Iranmanesh, A., Bowers, C.Y. J. Clin. Endocrinol. Metab. (2005) [Pubmed]
  20. A five day treatment with daily subcutaneous injections of growth hormone-releasing peptide-2 causes response attenuation and does not stimulate insulin-like growth factor-I secretion in healthy young men. Nijland, E.A., Strasburger, C.J., Popp-Snijders, C., van der Wal, P.S., van der Veen, E.A. Eur. J. Endocrinol. (1998) [Pubmed]
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