Gonadorelin
Also known as: GnRH
Molecular Identifiers
Overview
Gonadotropin-releasing hormone (GnRH). Stimulates LH and FSH release from the pituitary gland. Research on the HPG axis. Pulsatile administration may be beneficial.
FDA-approved as Factrel for diagnostic use of gonadotropic function and as Lutrepulse for therapeutic pulsatile administration in the treatment of hypogonadotropic hypogonadism and infertility.
The main clinical interest around gonadorelin is restoring hypothalamic-pituitary-gonadal (HPG) axis function in cases of hypogonadotropic hypogonadism and infertility. When delivered in a pulsatile fashion, it mimics endogenous GnRH secretion and triggers physiological LH and FSH release, with effects on male and female fertility and on ovulation induction.
Today gonadorelin is prescribed mainly in reproductive medicine and endocrinology clinics, often through compounding pharmacies for off-label uses such as pituitary reserve testing and post-cycle therapy protocols associated with anabolic steroid use. It is FDA-approved as Factrel (diagnostic use) and Lutrepulse (therapeutic pulsatile administration).
Within the HPG axis, gonadorelin is essentially endogenous GnRH itself, with a very short half-life — useful for pulsatile physiological stimulation. It differs from triptorelin (long-acting agonist that, after the initial flare, desensitizes the receptor and suppresses LH/FSH) and from cetrorelix (antagonist, immediate suppression without a flare, standard in IVF); it sits downstream of kisspeptin-10 (which acts on hypothalamic neurons to trigger GnRH release); and it acts via the pituitary, unlike hCG (which mimics LH directly at the Leydig cells).
QHWSYGLRPG pGlu-His-Trp-Ser-Tyr-Gly-Leu-Arg-Pro-Gly-NH2 First residue is pyroglutamic acid (pGlu), not glutamine. C-terminus is amidated.
Half-life
~2-4 minutes
Administration Route
Subcutaneous or intravenous
Category
Hormonal Regulation
Mechanism of Action
- Stimulation of LH and FSH release from the anterior pituitary
- Regulation of the hypothalamic-pituitary-gonadal (HPG) axis
- Pulsatile administration mimics endogenous secretion
Dosage Protocol
Data compiled from the literature. This does not constitute medical advice.
| Parameter | Value |
|---|---|
| Dose | 100-200 mcg per injection |
| Frequency | 2-3 times per week |
| Timing | Any time of day |
| Duration | As per research protocol |
Reported Side Effects
Adverse effects described in the literature. Severity and frequency vary between individuals.
- Headache
- Facial flushing
- Nausea
- Injection site pain
- Hot flashes
Product Properties
| Purity | >99% |
| Appearance | White lyophilized powder |
| Solubility | Soluble in water and bacteriostatic water |
| Source | Solid-phase peptide synthesis (SPPS) |
| Storage | Lyophilized: -20°C for up to 2 years, 2-8°C for up to 6 months. Reconstituted: 2-8°C for up to 4 weeks. Protect from light and moisture. Avoid repeated freeze-thaw cycles. |
Presentations & Preparation
Vials of Gonadorelin found in the research market:
Reconstitution
- Diluent: Bacteriostatic water
- Volume: 2 ml per vial
- Slowly inject the diluent against the vial wall
- Gently swirl until fully dissolved
- Never shake
Storage
- Lyophilized: Refrigerated 2-8°C
- Reconstituted: Refrigerated 2-8°C (up to 30 days)
- Protect from direct light
- Do not freeze after reconstitution
Scientific Studies
Published studies on Gonadorelin.
The pulsatile gonadorelin pump induces earlier spermatogenesis than cyclical gonadotropin therapy in congenital hypogonadotropic hypogonadism men
Zhang L, Cai K, Wang Y, Ji W, Cheng Z, Chen G, Liao Z
Predictors of outcome of long-term GnRH therapy in men with idiopathic hypogonadotropic hypogonadism
Pitteloud N, Hayes FJ, Dwyer A, Boepple PA, Lee H, Crowley WF Jr
Related Peptides
Argipressin
5-20 IU or 1-4 mcg/kg · As clinically needed
Cetrorelix
0.25-3 mg per injection · Once daily (0.25 mg) or single dose (3 mg)
HCG
250-500 IU per injection · 2-3 times per week
Kisspeptin-10
1-10 mcg per injection · Per research protocol
α-MSH
0.5-2 mg per injection · Once daily or every other day
Oxytocin
10-40 IU intranasal or 50-200 mcg subcutaneous · 1-2 times daily