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Growth hormone secretagogue (revision 3)

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Growth hormone secretagogue
Two receptor familiesGHRH receptor; ghrelin receptor (GHS-R1a)
GHRH analoguesSermorelin, CJC-1295, Tesamorelin
Ghrelin-receptor agonistsIpamorelin, and related compounds
Approved exampleTesamorelin, for a specific indication
Topic infobox · conventions

Growth hormone secretagogues are compounds that stimulate release of endogenous growth hormone, in contrast to administration of growth hormone itself. Two receptor families are involved: the receptor for growth hormone-releasing hormone, and the ghrelin receptor GHS-R1a.[1]

GHRH analogues — sermorelin, CJC-1295, tesamorelin — mimic the hypothalamic releasing hormone. Ghrelin-receptor agonists such as ipamorelin act at a separate receptor and by a partly complementary mechanism.[1]

Mechanisms

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GHRH-receptor agonism at somatotroph cells raises cAMP and promotes synthesis and release of growth hormone. Native GHRH has a very short half-life; the analogues are modified to extend it, and CJC-1295 uses a linker permitting covalent binding to albumin for a much longer duration.[1]

Ghrelin-receptor agonism acts through a different pathway and also suppresses somatostatin tone, so the two mechanisms combine more than additively in some experimental settings — the rationale for combining them that appears in community discussion.[1]

References

  1. ^ a b c d Sigalos JT, Pastuszak AW. "The safety and efficacy of growth hormone secretagogues." Sexual Medicine Reviews 6(1):45–53 (2018). PMID 28526632.