Growth hormone secretagogue explained

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),^[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

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

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

Notes and References

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