Ipamorelin — pharmacology
Molecular targets, mechanism of action, pharmacokinetics and interactions as characterised in humans.
§2Pharmacology
§2.1Molecular targets
Table 2. Molecular targets recorded for Ipamorelin, with the character of the interaction and the potency where the Institute holds it.
| Target | Interaction | Note |
|---|---|---|
| Growth hormone secretagogue receptor (GHSR-1a, ghrelin receptor) | Agonist | Selective for growth-hormone release without the adrenocorticotropin, cortisol or prolactin elevation seen with earlier secretagogues such as GHRP-6 |
§2.2Mechanism of action
Ipamorelin activates the ghrelin receptor on pituitary somatotrophs, producing growth-hormone release through a pathway distinct from and complementary to GHRH receptor signalling. Its defining pharmacological characteristic, established in the original preclinical work, is selectivity: unlike GHRP-6 and hexarelin it does not meaningfully raise cortisol or prolactin, and unlike ghrelin itself it does not stimulate appetite at growth-hormone-releasing doses.[1,2]
§2.3Pharmacokinetics
- Terminal half-life
- ≈2 h
- Time to maximum concentration
- not reliably published in humans
- Volume of distribution
- not published
- Plasma protein binding
- not published
- Clearance
- not published
- Bioavailability
- not published
Assumed proteolytic and renal. Human pharmacokinetic data are sparse.
§2.4Interactions
- Not characterised
References cited on this page
References are numbered in order of first citation in this document. Each superscript in the text links to its entry below.
- Raun K, Hansen BS, Johansen NL, Thøgersen H, Madsen K, Ankersen M, Andersen PH. Ipamorelin, the first selective growth hormone secretagogue. European Journal of Endocrinology 1998;139(5):552–561. doi:10.1530/eje.0.1390552 · PMID 9849822
- Teichman SL, Neale A, Lawrence B, Gagnon C, Castaigne JP, Frohman LA. 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. Journal of Clinical Endocrinology & Metabolism 2006;91(3):799–805. doi:10.1210/jc.2005-1536 · PMID 16352683
Identifiers are reproduced only where the Institute holds them. Where a digital object identifier or PubMed identifier is not shown, the Institute has recorded the journal and year and has not constructed an identifier.