Description

Gonadorelin Acetate

1. Basic Overview

Gonadorelin Acetate (also known as GnRH / LHRH) is a synthetic decapeptide, structurally identical to endogenous gonadotropin-releasing hormone secreted by the hypothalamus.

Amino Acid Sequence: pyroGlu-His-Trp-Ser-Tyr-Gly-Leu-Arg-Pro-Gly-NH₂
CAS: 71447-49-9
Molecular Weight: 1182.3 Da
Form: Lyophilized white crystalline powder
Plasma Half-life: 2–4 minutes (intravenous); 10–40 minutes (subcutaneous)

Gonadorelin acts as the master upstream regulator of the Hypothalamic-Pituitary-Gonadal (HPG) axis. A critical pharmacological feature: pulsatile administration stimulates gonadotropin release, while continuous exposure causes receptor desensitization and suppresses the HPG axis.

2. Mechanism of Action

Selectively binds GnRH receptors on gonadotroph cells within the anterior pituitary gland.
Activates intracellular calcium signaling pathways, triggering secretion of Luteinizing Hormone (LH) and Follicle-Stimulating Hormone (FSH).
LH and FSH travel to gonads to regulate testosterone synthesis in males, estrogen / progesterone production and follicle development in females.
Intermittent pulsatile dosing maintains receptor sensitivity and preserves normal reproductive endocrine function.
Sustained non-pulsatile administration leads to GnRH receptor downregulation, reducing LH/FSH and lowering circulating sex hormone levels.

3. Main Observed Research Effects

Stimulate endogenous LH & FSH secretion to maintain HPG axis activity
Support testicular function and preserve spermatogenesis in male research models
Induce follicle maturation and ovulation in female fertility research
Used for GnRH stimulation tests to evaluate pituitary gonadotropic function
Investigate protection of reproductive function during long-term hormone intervention
Research for treatment of hypogonadotropic hypogonadism

4. Reconstitution Instructions (Lyophilized Vial)

Common specifications: 2mg / 5mg / 10mg per vial

Equilibrate the vial to room temperature; disinfect the rubber stopper with alcohol.
Slowly inject Bacteriostatic Water (BAC water) along the inner glass wall. Avoid direct impact onto lyophilized powder.

Standard mixing scheme: 2mg powder + 2mL BAC water → Final concentration = 1 mg/mL

Gently rotate the vial to dissolve powder. DO NOT shake violently to avoid peptide denaturation. The finished solution is clear and colourless.
Storage Requirements

Unreconstituted lyophilized powder: Store sealed at -20°C, protected from light. Shelf life up to 24 months.
Reconstituted peptide solution: Refrigerate 2°C ~ 8°C, stable within 28 days. Avoid repeated freeze-thaw cycles.

5. Research Administration Protocols

Primary Route: Subcutaneous Injection

Reference Experimental Dosage

Low research dose: 100 mcg per injection
Standard research dose: 200 mcg – 500 mcg per injection
Frequency: 1–2 times daily (intermittent pulsatile style recommended)
Injection site: Lower abdomen subcutaneous tissue; rotate injection sites regularly

Cycle Reference

8–12 weeks continuous experimental cycle; follow with 2–4 weeks observation period before repeating cycles.

Alternative Route: Intravenous Injection

Typical diagnostic research dose: 100 mcg single bolus for pituitary stimulation testing.

6. Precautions

Pure laboratory research reagent. Not approved for human medical use.
Strict sterile operation required during reconstitution to prevent contamination.
If turbidity, precipitation or persistent local irritation occurs, discard the solution immediately.
Dosing schedule is critical. Improper continuous administration may suppress reproductive hormone secretion.
Limited large-scale independent long-term clinical research data; all effects are summarized from preclinical and in-vivo animal experiments.

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