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Compound Evidence InstituteEvidence synthesis · established 2023Graded assessments of compounds, trials, methods and supply
Document set current to 30 July 2026
Compound monograph · §2

GHRP-2 — pharmacology

Molecular targets, mechanism of action, pharmacokinetics and interactions as characterised in humans.

Document identifier
CEI-MN-026/2
Series
Compound monograph
Version
4.0
Published
17 Oct 2023
Last reviewed
17 Apr 2024
Next review
17 Apr 2026
Identifier
10.71829/cei.mono.26
Certainty
Low
Cycle
2023 Q4

§2Pharmacology

§2.1Molecular targets

Table 2. Molecular targets recorded for GHRP-2, with the character of the interaction and the potency where the Institute holds it.

TargetInteractionNote
Growth hormone secretagogue receptor (GHSR-1a)AgonistPotent; also raises cortisol and prolactin, though less than hexarelin

§2.2Mechanism of action

Ghrelin receptor agonism producing growth-hormone release. Its approved use is a single-dose provocative diagnostic test, for which the acute pharmacodynamic effect is the entire basis of the indication and questions of chronic administration do not arise.[1,2]

§2.3Pharmacokinetics

Terminal half-life
≈45–60 min
Time to maximum concentration
≈15 min (intravenous)
Volume of distribution
not published
Plasma protein binding
not published
Clearance
not published
Bioavailability
not published

Proteolytic degradation with renal excretion of fragments.

Reconstructed plasma concentration–time profilePlasma concentration plotted against time after dosing, reconstructed from published pharmacokinetic parameters.0.00.20.40.60.801234Time after first dose (hours)Relative concentrationt max ≈ 1 ht½ ≈ 1 h
Modelled profileSimulated observationsDose administration
Figure 2. Illustrative. Plasma concentration–time profile reconstructed by the Institute from the published half-life and time-to-maximum-concentration parameters using a one-compartment model with first-order absorption. The curve is not digitised from a published figure and its vertical scale is relative. It is published to convey the shape of the profile and the approach to steady state, not to supply a concentration at any time point.

§2.4Interactions

  • Glucocorticoids and somatostatin analogues confound the diagnostic response

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.

  1. 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
  2. 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.

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