Growth hormone secretagogue

Growth hormone secretagogues or GH secretagogues (GHSs) are a class of drugs which act as secretagogues (i.e., induce the secretion) of growth hormone (GH).^[1] They include agonists of the ghrelin/growth hormone secretagogue receptor (GHSR), such as ghrelin (lenomorelin), pralmorelin (GHRP-2), GHRP-6, examorelin (hexarelin), ipamorelin, and ibutamoren (MK-677),^[1][2] and agonists of the growth hormone-releasing hormone receptor (GHRHR), such as growth hormone-releasing hormone (GHRH, somatorelin), CJC-1295,^[3] sermorelin,^[4] and tesamorelin.^[5]

Many of them also induce the secretion of insulin-like growth factor 1 (IGF-1),^[6] as well as of other hypothalamic-pituitary hormones such as prolactin and cortisol. The main clinical application of these agents is the treatment of growth hormone deficiency.^[7] They also see black market use, similarly to anabolic steroids, for bodybuilding purposes.

GHRH receptor agonists

Main article: Growth-hormone-releasing hormone receptor § Agonists

Peptide

• GHRH (Somatocrinin, GRF, GHRF)
• CJC-1295 (DAC:GRF)
• Modified GRF (1-29) (CJC without DAC)
• Dumorelin
• Rismorelin
• Sermorelin (Geref, Gerel; GHRH (1-29))
• Somatorelin
• Tesamorelin (Egrifta)

Ghrelin (GHS) receptor agonists

Main article: Growth hormone secretagogue receptor § Agonists

Peptide

• Ghrelin (Lenomorelin, GHRL)
• GHRP-1
• GHRP-2 (Pralmorelin; GHRP Kaken 100; GHRP-2; KP-102, GPA-748, WAY-GPA-748)
• GHRP-3
• GHRP-4
• GHRP-5
• GHRP-6 (SKF-110679)
• Alexamorelin
• Examorelin (hexarelin; EP-23905, MF-6003)
• Ipamorelin (NNC 26-0161)
• Relamorelin (RM-131, BIM-28131, BIM-28163)
• Tabimorelin (NN-703)

Non-peptide

• Adenosine
• Anamorelin (ONO-7643, RC-1291, ST-1291)
• Capromorelin (CP-424391)
• Ibutamoren (MK-677, MK-0677, L-163191, LUM-201)
• Macimorelin (AEZS-130, JMV 1843)
• SM-130686

Note that while ulimorelin is a ghrelin receptor agonist, it is not a GHS as it is peripherally selective and has little or no effect on GH secretion.^[8] Likewise, Adenosine is capable of eliciting hunger response as a ghrelin agonist but has little to no effect on GH secretion.

See also

• Hypothalamic–pituitary–somatic axis

References

1. Davenport AP, Bonner TI, Foord SM, Harmar AJ, Neubig RR, Pin JP, et al. (December 2005). "International Union of Pharmacology. LVI. Ghrelin receptor nomenclature, distribution, and function". Pharmacological Reviews. 57 (4): 541–6. doi:10.1124/pr.57.4.1. PMID 16382107. S2CID 11254096.
2. Camanni F, Ghigo E, Arvat E (January 1998). "Growth hormone-releasing peptides and their analogs". Frontiers in Neuroendocrinology. 19 (1): 47–72. doi:10.1006/frne.1997.0158. PMID 9465289. S2CID 31400577.
3. Teichman, SL; et al. (2006). "Prolonged stimulation of growth hormone (GH) and insulin-like growth factor I secretion by CJC-1295, a long-acting analog of GH-releasing hormone, in healthy adults". J Clin Endocrinol Metab. 91 (3): 799–805. doi:10.1210/jc.2005-1536. PMID 16352683.
4. Prakash A, Goa KL (August 1999). "Sermorelin: a review of its use in the diagnosis and treatment of children with idiopathic growth hormone deficiency". BioDrugs. 12 (2): 139–57. doi:10.2165/00063030-199912020-00007. PMID 18031173.
5. Mauss, Stefan; Schmutz, Günther (2001). "Das HIV-assoziierte Lipodystrophiesyndrom". Medizinische Klinik. 96 (7): 391–401. doi:10.1007/PL00002220. PMID 11494914.
6. Mutschler, Ernst (2013). Arzneimittelwirkungen (in German) (10 ed.). Stuttgart: Wissenschaftliche Verlagsgesellschaft. p. 353. ISBN 978-3-8047-2898-1.
7. Alexopoulou O, Abs R, Maiter D (2010). "Treatment of adult growth hormone deficiency: who, why and how? A review". Acta Clin Belg. 65 (1): 13–22. doi:10.1179/acb.2010.002. PMID 20373593. S2CID 24874132.
8. Fraser GL, Hoveyda HR, Tannenbaum GS (2008). "Pharmacological demarcation of the growth hormone, gut motility and feeding effects of ghrelin using a novel ghrelin receptor agonist". Endocrinology. 149 (12): 6280–8. doi:10.1210/en.2008-0804. PMID 18719021.