GHRP-6 — pharmacology
Molecular targets, mechanism of action, pharmacokinetics and interactions as characterised in humans.
§2Pharmacology
§2.1Molecular targets
Table 2. Molecular targets recorded for GHRP-6, with the character of the interaction and the potency where the Institute holds it.
| Target | Interaction | Note |
|---|---|---|
| Growth hormone secretagogue receptor (GHSR-1a) | Agonist | The original synthetic ligand for this receptor, characterised before the endogenous ligand ghrelin was identified |
§2.2Mechanism of action
Ghrelin receptor agonism with pronounced growth-hormone release, marked appetite stimulation, and concomitant elevation of cortisol and prolactin. Its historical importance is substantial — it was the pharmacological tool that led to the discovery of the ghrelin receptor and subsequently of ghrelin itself — but its selectivity profile makes it the least attractive member of the class for any practical purpose.[1,2]
§2.3Pharmacokinetics
- Terminal half-life
- ≈20 min
- Time to maximum concentration
- ≈15 min
- Volume of distribution
- not published
- Plasma protein binding
- not published
- Clearance
- not published
- Bioavailability
- not published
Rapid proteolytic degradation. Tachyphylaxis with continued dosing is documented.
§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
- Thevis M, Thomas A, Schänzer W. Detecting peptidic drugs, drug candidates and analogs in sports doping: current status and future directions. Expert Review of Proteomics 2019;11(6):663–673. doi:10.1586/14789450.2014.965158
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.