Growth hormone secretagogue (revision 2)
Old revision·03:08, 2 Nov 2024·SafetySignalSid
| Growth hormone secretagogue | |
|---|---|
| Two receptor families | GHRH receptor; ghrelin receptor (GHS-R1a) |
| GHRH analogues | Sermorelin, CJC-1295, Tesamorelin |
| Ghrelin-receptor agonists | Ipamorelin, and related compounds |
| Approved example | Tesamorelin, 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
[edit]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]