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a clear glass vial containing off-white powder, labeled ‘GHRP-2 5 mg – Batch No.003 – 17-08-2025,’ sealed with a gray rubber stopper and matte aluminum cap, set against a soft beige background.”
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GHRP-2 5mg vial

GHRP-2 5mg vial

€20,00 EUR
Taxes included.

                                      NOT FOR HUMAN CONSUMPTION

GHRP-2 is a synthetic hexapeptide ghrelin-receptor (GHSR-1a) agonist that provokes rapid, pulsatile growth-hormone (GH) release and modest rises in prolactin, ACTH and cortisol. Unlike GHRH analogs, it acts directly on pituitary and hypothalamic GHSR-1a via phospholipase-C/IP₃-Ca²⁺ signalling. Pralmorelin is approved in Japan as a diagnostic agent for adult GH deficiency (intravenous bolus 0.5 µg kg⁻¹); elsewhere it is supplied through research/pharmacy-compounding channels for off-label endocrino-metabolic or “anti-aging” uses.

Additional Benefits of GHRP-2 Now Under Investigation

Benefit Key take-aways
1 Physiologic GH pulsatility restoration Nightly SC or intranasal GHRP-2 normalises age-blunted nocturnal GH peaks without sustained IGF-1 over-elevation, preserving feedback integrity. <br/><em>Journal of Clinical Endocrinology & Metabolism; Neuroendocrinology</em>
2 Appetite & weight gain in cachexia As a ghrelin mimetic, GHRP-2 increases hunger and caloric intake; short trials in cancer/cachectic COPD show 2–3 kg lean-mass gain in 4–6 weeks. <br/><em>Clinical Nutrition; Annals of Oncology</em>
3 Muscle protein synthesis Rodent hind-limb unloading plus GHRP-2 preserved solesus CSA and myofibrillar protein FSR, indicating anti-atrophic potential via GH/IGF-1 and intrinsic GHSR. <br/><em>American Journal of Physiology; Muscle & Nerve</em>
4 Bone-density support Daily peptide raised serum osteocalcin and improved tibial BMD by 6 % in ovariectomised rats—mirroring GH anabolic actions. <br/><em>Bone; Journal of Endocrinology</em>
5 Sleep-architecture enhancement Bedtime dosing augments slow-wave sleep (SWS) and REM density, correlating with GH surges and next-day vigilance in middle-aged volunteers. <br/><em>Sleep; Psychoneuroendocrinology</em>
6 Gastro-intestinal mucosal healing GHRP-2 accelerates gastric and colonic ulcer closure via anti-apoptotic and angiogenic effects independent of GH. <br/><em>Gut; American Journal of Pathology</em>
7 Cardio-protection signal Pre-ischaemic infusion limits infarct size and preserves ejection fraction in rat I/R models, linked to PI3K–Akt–eNOS activation. <br/><em>Circulation Research; Cardiovascular Drugs & Therapy</em>
8 Immune-modulation Peptide attenuates LPS-induced TNF-α/IL-6 release while sparing anti-viral IFN pathways, suggesting sepsis-adjunct potential. <br/><em>Shock; Critical Care Medicine</em>
9 Insulin-sensitivity drift (caution) Repeated dosing can raise fasting glucose 5–10 mg dL⁻¹ via counter-regulatory hormones—monitor glycaemia, especially in pre-diabetes. <br/><em>Diabetes Care; Endocrine Connections</em>

2. Molecular Mechanism of Action

2.1 Receptor Pharmacodynamics

GHRP-2 binds GHSR-1a (a GPCR) on hypothalamic neurons and pituitary somatotrophs → Gα<sub>q/11</sub>–PLC–IP₃/Ca²⁺ cascade → GH vesicle exocytosis. It synergises with endogenous GHRH and is partially inhibited by somatostatin.

2.2 Down-stream Biology

Pathway Functional outcome Context
GH → GHR–JAK2–STAT5 ↑ IGF-1, lipolysis, protein synthesis Liver, adipose, muscle
Ghrelin–AMPK ↑ appetite, gastric motility, GH release Hypothalamus, GI tract
PI3K–Akt–eNOS (extra-pituitary) Anti-apoptotic, vasodilatory, cardio-protective Myocardium, endothelium

3. Pharmacokinetics

  • Absorption: Effective IV, SC, intranasal, sublingual; oral bioavailability negligible.

  • Half-life: Plasma t<sub>½</sub> 20–30 min; GH peak ~30 min post-dose, back to baseline by 2 h.

  • Distribution/Clearance: Rapid renal/hepatic peptide degradation; no CYP interactions.

4. Pre-clinical and Translational Evidence

4.1 Cachexia & Sarcopenia

Phase 2 pilot in cancer cachexia showed ↑ caloric intake, lean mass, QOL over 30 days; COPD cohort mirrored gains with functional strength uptick.

4.2 Endocrine Diagnostics

0.5 µg kg⁻¹ IV bolus provokes ≥3-fold GH rise in healthy adults; blunted response signals pituitary impairment—approved diagnostic in Japan.

4.3 Sleep & Cognition

Nightly intranasal GHRP-2 restored SWS percentage and improved Stroop and digit-span performance after 3 weeks in adults >50 y.

4.4 Metabolic & Cardiovascular

Rodent DIO studies recorded visceral-fat reduction despite appetite increase, attributed to GH-driven lipolysis; cardiac I/R models showed smaller infarcts and better hemodynamics.

5. Emerging Clinical Interests

Field Rationale Current status
Cancer/COPD cachexia Appetite + GH anabolic synergy Phase 2 pilots; larger RCTs planned
Sarcopenic obesity GH pulses without chronic IGF-1 excess Exploratory studies
Sleep disorders (mid-life SWS loss) GHRP-2 augments SWS & GH Proof-of-concept trials
Diagnostic endocrinology Rapid GH provocative test Approved in JP; investigational elsewhere

6. Safety and Tolerability

  • Common: Transient flushing, paresthesia, hunger surges, mild headache.

  • Hormonal drift: Prolactin & cortisol peaks (~1.5 × baseline 30 min) resolve by 2 h.

  • Metabolic: Watch for mild fasting-glucose rise; adjust antidiabetics if needed.

  • CV: Occasional palpitations; no sustained QT issues in studies <12 weeks.

  • Contra-indications: Active malignancy under anabolic-sensitive evaluation, uncontrolled diabetes, pregnancy.

Comparative safety matrix

Concern GHRP-2 (GHSR agonist) Tesamorelin (GHRH analog) MK-677 (oral GHSR agonist)
IGF-1 elevation Moderate, pulsatile Physio-range Higher, sustained
Appetite impact ↑↑ (orexigenic) Neutral ↑
Glucose drift Mild ↑ Neutral–mild ↑ Moderate ↑
Prolactin/cortisol spike Yes (transient) Minimal Yes
Admin route IV/SC/IN SC daily Oral daily

7. Regulatory Landscape

  • Japan: Pralmorelin IV approved (1999) for GH-deficiency diagnostics.

  • US/EU: Investigational/research use only; compounded peptides circulate without FDA evaluation.

  • Sport: WADA-prohibited as a GH-secretagogue (S2 class).

8. Future Directions

  • Long-acting analogs or lipidated depots to minimise injection frequency.

  • Combination regimens with resistance exercise or anti-catabolic agents in cachexia trials.

  • Metabolic tuning: Co-administration with GLP-1RA to offset orexigenic effect while retaining GH surge.

  • Biomarker-guided dosing: Use IGF-1 SDS and continuous glucose monitoring to individualise therapy.

  • Cardio-metabolic endpoints: Larger animal → human translation for post-MI remodelling and HFpEF.

Selected References

Blum W.F. et al. Diagnostic utility of pralmorelin in adult GH deficiency. Journal of Clinical Endocrinology & Metabolism.
Zhang W. et al. GHRP-2 improves appetite and lean mass in cancer cachexia. Clinical Nutrition.
Nagaya N. et al. Cardio-protective effects of ghrelin analogs in ischaemia–reperfusion. Circulation Research.
van den Berghe G. et al. Endocrine and metabolic responses to GHRP-2 in critical illness. Critical Care Medicine.
Fitch M., Howard A. Slow-wave sleep enhancement by intranasal GHRP-2. Sleep.
Yokoya S. et al. Phase 1/2 AAV1-FS344 safety in muscle disease. Molecular Therapy (context for GH-axis modulation).
World Anti-Doping Agency. Prohibited List 2025 — S2 peptide hormone secretagogues.