Description

Hexarelin Acetate – Advanced Biochemical Mechanism Profile

(Growth Hormone Secretagogue; GHSR-1a Agonist; Peptide Analog)

Hexarelin is a synthetic growth hormone secretagogue (GHS) that selectively activates the GHSR-1a receptor, a G-protein–coupled receptor expressed in pituitary and hypothalamic cell models. It is structurally related to ghrelin mimetics, but engineered for increased receptor affinity and metabolic stability.

✅ 1. Primary Receptor Target

GHSR-1a (Growth Hormone Secretagogue Receptor 1a)

• Class: Gq/11-coupled GPCR

• Location: pituitary somatotrophs, hypothalamus, cardiac tissue, immune cells

• Outcome: stimulation of intracellular Ca²⁺ mobilization and PKC activation

Upon binding:

1. GHSR-1a → Gq/11

2. Phospholipase Cβ (PLCβ) activation

3. PIP₂ → IP₃ + DAG hydrolysis

4. IP₃ → Ca²⁺ release from ER stores

5. DAG → PKC activation

6. Membrane depolarization → GH exocytosis in endocrine studies

✅ 2. Secondary Signaling Pathways

A. cAMP / PKA (Gs-linked cross-activation)

Some cell models show additional Gs coupling:

• ↑ adenylate cyclase

• ↑ cAMP

• PKA phosphorylation of calcium channels

• Enhanced GH-secretory vesicle fusion

B. ERK1/2 MAPK Pathway

GHSR-1a activation stimulates:

• Ras → Raf → MEK1/2 → ERK1/2

• Upregulation of growth-signaling transcription factors

C. PI3K / Akt Pathway

Cardiac and metabolic research models show:

• PI3K → Akt phosphorylation

• Anti-apoptotic gene signaling

• Mitochondrial membrane stabilization

✅ 3. Second Messengers and Enzymes

✅ 4. Gene Targets Commonly Studied in Research

Certain studies also track cardiac metabolic genes due to GHSR expression in cardiomyocytes.

✅ 5. Receptor Kinetics

• High affinity for GHSR-1a

• Resistant to peptidase degradation relative to native ghrelin

• Sustained intracellular Ca²⁺ activity

• Rapid induction of GH-releasing vesicle exocytosis in pituitary cell lines

Research-Only Use Classification

Hexarelin Acetate is supplied solely for laboratory research and in-vitro experimentation.
It is not approved for human or animal use, consumption, injection, ingestion, therapeutic application, or diagnostic procedures.