GHRP-6 5mg

Description

GHRP-6

Benefit Key take-aways
1 Robust GH pulse + IGF-1 rise Reproducible dose-dependent GH surges with IGF-1 increases over weeks; greater peaks when co-dosed with GHRH analogs versus either alone.
2 Appetite restoration & weight in catabolic states Strong orexigenic effect increases intake/weight in cachexia, COPD/CHF rehab pilots; must balance with glycaemic control.
3 Sleep & recovery signals Bedtime dosing can augment slow-wave sleep (SWS) and nocturnal GH pulsatility, supporting recovery; effects vary by age and baseline sleep.
4 Tendon/ligament & collagen turnover GH/IGF-1–mediated increases in type-I collagen synthesis and tenocyte activity suggest utility in overuse/repair contexts (preclinical → translational).
5 Bone-formation markers Up-shifts P1NP/osteocalcin and improves bone micro-anabolism in hyposecretory states; fracture outcomes untested.
6 Cardiometabolic & vascular Ghrelin-pathway agonism shows endothelial and LV function benefits and sympathetic dampening in models of HF/ischemia; human data are early.
7 GI motility and mucosal protection Improves gastric emptying, supports epithelial integrity, and reduces mucosal cytokines in injury models.
8 Neuroendocrine & mood Ghrelin signalling can reduce anhedonia and support neuroplasticity; limited pilot data with GHRP-class agents show fatigue/mood improvements.
9 Rehab synergy Additive benefits on lean mass/strength when paired with progressive resistance training and adequate protein intake.

2. Molecular Mechanism of Action

2.1 Receptor Pharmacodynamics

  • Primary target: GHSR-1a (ghrelin receptor) on hypothalamic neurons and pituitary somatotrophs → Gq/PLC → IP₃/Ca²⁺ → GH exocytosis.

  • Axis biology: Synergizes with GHRH; blunted by somatostatin; preserves physiologic pulsatility versus continuous GH.

  • Central effects: Activates NPY/AgRP (orexigeny), modulates sleep circuits, and affects autonomic tone.

2.2 Down-stream Biology

Pathway Functional outcome Context
GH → GHR–JAK2–STAT5 → IGF-1 ↑ Protein synthesis, recovery, lipolysis Muscle, liver, adipose
NPY/AgRP activation ↑ Appetite, ↑ GI motility Hypothalamus/GI
Collagen & ECM turnover ↑ Type-I collagen synthesis Tendon/ligament, skin
Bone remodelling ↑ Formation markers (P1NP/OCN) Skeleton
Endothelial signalling Improved NO bioavailability, LV support (models) Cardiovascular

3. Pharmacokinetics

  • Route: SC (research/clinical physiology).

  • Onset/peak: GH peaks ~20–45 min post-dose; returns to baseline by ~2–3 h.

  • Half-life: Short (≈15–30 min) for peptide; biological effects exceed plasma residence.

  • Dosing in studies: ~1–2 µg/kg SC per pulse; common research use 100–200 µg 1–3×/day. Co-administration with GHRH analogs (e.g., CJC-1295-no-DAC/sermorelin) potentiates GH/IGF-1.

4. Pre-clinical and Translational Evidence

4.1 GH Axis & Body Composition

Repeated dosing elevates IGF-1 and fat-free mass signals; fat-mass effects depend on dietary intake (orexigeny can offset lipolysis without nutrition control).

4.2 Musculoskeletal/Repair

Animal and human physiology show collagen synthesis up-regulation and improved tendon matrix organisation with GH/IGF-1 signalling; targeted trials with GHRP-6 are still limited.

4.3 Cardiometabolic

Ghrelin-mimetic actions may improve endothelial function and LV performance in HF/ischemia models; confirmatory human data for GHRP-6 specifically are pending.

Evidence quality note: Strong physiology and class-level data for GH pulsatility and orexigeny; specific randomized human outcomes with GHRP-6 are limited. Extrapolate with caution.

5. Emerging Clinical Interests

Field Rationale Current status
Sarcopenia/frailty Oral intake ↑ + GH/IGF-1 support Early translational
Cachexia/rehab Appetite + anabolism for weight/FFM regain Pilot concepts
Tendon/ligament repair Collagen anabolism Preclinical → feasibility
Bone health (adjunct) Formation markers ↑ Exploratory
Sleep/SWS deficits Nocturnal GH pulses PoC needed
HF/ischemia Endothelial/LV signalling Preclinical/early human physiology
GI motility/mucositis Pro-motility, epithelial protection Preclinical

6. Safety and Tolerability

  • Common: Marked hunger, flushing/warmth, transient lightheadedness, peripheral edema, carpal-tunnel-like paresthesias, headache, injection-site irritation, reflux/heartburn.

  • Endocrine: Prolactin and cortisol can rise acutely; IGF-1 elevation depends on frequency/co-therapy.

  • Metabolic: Ghrelin-like signalling may raise fasting glucose/insulin; manage diet and monitor in prediabetes/diabetes.

  • CV/Renal: Sodium/water retention → BP drift in susceptible patients.

  • Neuropsych: Vivid dreams/insomnia in a minority (timing dependent).

  • Contraindications/Caution: Active malignancy, proliferative retinopathy, uncontrolled diabetes, severe OSA, pregnancy.

  • Drug interactions: Additive effects with other GH secretagogues; theoretical interactions with dopamine/prolactin modulators and acid-suppressants (for reflux).

Comparative safety matrix

Feature GHRP-6 GHRP-2 Hexarelin MK-677 (oral GHSR agonist)
Appetite drive High Moderate Low–moderate Very high
GH/IGF-1 rise (per pulse) High; ↑ with GHRH High; slightly less orexigeny High; stronger PRL/Cort↑ Sustained daily ↑
Edema/CTS-like Moderate Moderate Moderate Moderate–high
Prolactin/Cortisol ↑ (acute) ↑ (moderate) ↑↑ Mild ↑
Route/PK SC; t½ ~15–30 min SC; short t½ SC; short t½ Oral; t½ 4–6 h
GI symptoms Reflux/GERD more common Similar Similar Nausea, GERD

7. Regulatory Landscape

  • Approvals: None for any indication.

  • Sport: WADA-prohibited (S2, GH-releasing substances).

  • Supply quality: Research-chemical products vary; ensure GMP-grade material in any formal study.

8. Future Directions

  • Chronopharmacology: Optimize bedtime vs pre-training pulses for SWS and recovery while managing reflux.

  • Combination therapy: Pair GHRP-6 + GHRH analogs to lower dose burden and enhance physiologic pulsatility; consider GLP-1/GIP co-therapy to temper orexigeny in weight-sensitive populations.

  • Indication-focused trials: Sarcopenia/rehab (DXA, stair-climb power), tendon healing (MRI/US elastography), bone (DXA + turnover markers), HFpEF/HFrEF physiology (VO₂, endothelial function).

  • Safety program: Glycaemic outcomes, BP/edema, PRL/Cort monitoring, and sleep metrics; standardized reflux mitigation.

  • Formulation science: Stabilized or depot analogs for consistent, lower-dose pulsatility with fewer GI effects.

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