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Gonadorelin

peptide · headlineFDA-approved

Acts as a GnRH receptor agonist on the anterior pituitary

Overview

Gonadorelin is a synthetic gonadotropin-releasing hormone (GnRH) used for diagnostic and therapeutic purposes in reproductive and endocrine medicine. It stimulates the anterior pituitary to release LH and FSH and is used in fertility restoration, hormone replacement, and hypothalamic amenorrhea treatment.

How it works

  • Acts as a GnRH receptor agonist on the anterior pituitary
  • Induces secretion of luteinizing hormone (LH) and follicle-stimulating hormone (FSH)
  • Requires pulsatile administration to mimic physiological GnRH signaling
  • Used in evaluating pituitary response and stimulating gonadal steroid production

Dosing

Standard diagnostic dose: 0.1 mg IV as a single bolus. Therapeutic pulsatile use: 5–20 mcg IV or SubQ every 90–120 minutes for HRT or fertility.

Intravenous (IV)0.1 mg standardrange 0.050.2 mg· Single dose (diagnostic) or pulsatile dosing (therapeutic)

Caution: Typical clinical research doses are 50–100 μg per injection. Gonadorelin is only approved for use in select diagnostic procedures.

Cycling

  • For diagnostic use: 0.1 mg IV as a single bolus. For therapeutic use: administered every 90–120 min in pulsatile infusion pumps over 7–14 days.

Side effects

Common
  • Transient headache or flushing shortly after injection

Stacking & combinations

With

GHK-Cu

Benefit

Used with HCG or Kisspeptin-10 in fertility and HPTA restoration protocols

Lifestyle support

Diet

Balanced nutrition. Avoid excessive alcohol.

Sleep

Adequate sleep (7–9 hours) supports hormonal rhythms. Stress management.

Timing

Consistent injection schedule to support hormonal rhythms.

Exercise

Resistance training.

Research studies

Studies summarized for educational purposes only. Inclusion does not imply human use; referenced research was conducted in vitro, in animal models, or in regulated clinical trials.

Research study

Induction of puberty in men by long-term pulsatile administration of low-dose gonadotropin-releasing hormone

Hoffman AR, Crowley WF Jr New England Journal of Medicine, 1982 View source ↗

Scientific findings

Six men with idiopathic hypogonadotropic hypogonadism received low-dose GnRH delivered subcutaneously in episodic (pulsatile) pulses via a portable infusion pump, mimicking physiologic hypothalamic secretion. Serum gonadotropins normalized within one week and rose above normal by two weeks, and testosterone increased from a markedly suppressed baseline (77 +/- 13 ng/dL) into the adult range. Four patients showed testicular growth and three achieved spermatogenesis by 43 weeks, demonstrating that pulsatile, rather than continuous, GnRH delivery reverses the pituitary-gonadal defect.

Plain English

In men whose bodies never triggered puberty because the brain fails to release the hormone that starts it, doctors used a small pump to deliver GnRH in tiny timed bursts like the body normally would. Within weeks the men's hormone levels became normal and testosterone climbed to adult levels. Several developed larger testes and began producing sperm, showing this pump approach can jump-start delayed puberty and fertility.

Research study

Induction of puberty by pulsatile gonadotropin releasing hormone

Stanhope R, Brook CG, Pringle PJ, Adams J, Jacobs HS Lancet, 1987 View source ↗

Scientific findings

Fifteen girls and seventeen boys with delayed or arrested puberty were treated with subcutaneous pulsatile GnRH at 90-minute intervals (1-2 micrograms/pulse for girls, 2-4 micrograms/pulse for boys). Clinical features, growth acceleration, endocrine profiles, and ovarian ultrasound morphology reproduced those of normal spontaneous puberty. Measurement of spontaneous gonadotropin pulsatility after treatment withdrawal distinguished 20 patients with hypogonadotropic hypogonadism from 12 with constitutional delay of growth and puberty, confirming that normal puberty is GnRH-dependent.

Plain English

Children with delayed puberty were given GnRH through a pump that released a small dose every 90 minutes, matching the body's natural rhythm. Their growth, hormone changes, and physical development matched what normally happens in puberty. Stopping the treatment and rechecking hormone patterns also helped doctors tell apart kids who were simply late bloomers from those with a permanent hormone deficiency.

Research study

Role of Gonadotropin-releasing Hormone Stimulation Test in Diagnosing Gonadotropin Deficiency in Both Males and Females with Delayed Puberty

Sun QH, Zheng Y, Zhang XL, Mu YM Chinese Medical Journal (English), 2015 View source ↗

Scientific findings

Investigators compared GnRH (gonadorelin) stimulation test responses across 91 patients with idiopathic hypogonadotropic hypogonadism, 27 with constitutional delay of growth and puberty, 6 prepubertal children, and 20 pubertal adults to derive diagnostic cut-offs. In males, a serum basal LH <0.6 IU/L or peak LH <9.74 IU/L yielded moderate sensitivity (73.8%/80.0%) and specificity (90.9%/86.4%); in females, basal LH <0.85 IU/L or basal FSH <2.43 IU/L gave sensitivities of 80.0%/100.0% and specificities of 75.0%/50.0%. The authors concluded the test alone adequately differentiates hypogonadotropic hypogonadism from constitutional delay in males, with basal or peak LH being the most useful predictor.

Plain English

Doctors gave a GnRH injection and measured how much the pituitary gland released the hormones LH and FSH, then compared results between patients with a true hormone deficiency and those who were just late to enter puberty. They identified LH threshold levels that reliably separated the two groups, especially in boys. This helps clinicians decide whether a teenager with delayed puberty needs treatment or will develop normally on their own.

Verified citations

2 · PubMed-checked
  • GnRH agonists: gonadorelin, leuprolide and nafarelin.reviewPMID 1835275
  • Effect of gonadorelin (GnRH) products on pregnancy rates in postpartum dairy cows.clinicalPMID 25979657

Reconstitution calculator

Intravenous (IV)
Draw to2 units

= 0.02 mL on a U-100 insulin syringe

Concentration5 mg/mL
Doses / vial100

Assumes a U-100 insulin syringe (100 units = 1 mL). This is a preparation aid, not a protocol — dose and route are the prescriber's decision. Refrigerate at 2–8 °C (35.6–46.4 °F); use within 4 weeks and avoid freeze–thaw

Chemistry & PK

Sequence
Pyr-His-Trp-Ser-Tyr-Gly-Leu-Arg-Pro-Gly-NH2
Half Life
2–4 minutes
Degradation
Rapid degradation by plasma proteases and renal clearance
Molecular Weight
1182
Molecular Formula
C55H75N17O13
Tissue Specificity
Targets anterior pituitary GnRH receptors

Bioavailability

Oral
Very poor; not viable orally
Subq
Low due to enzymatic degradation; typically not used subcutaneously

Storage & handling

Lyophilized

store at −20 °C (−4 °F); after reconstitution, refrigerate at 2–8 °C (35.6–46.4 °F); avoid freeze–thaw cycles

Reconstituted

Refrigerate at 2–8 °C (35.6–46.4 °F); use within 4 weeks and avoid freeze–thaw

Legal / compounding

FDA-approved
EU
Approved
FDA
Approved
Canada
Approved
Australia
Approved

Legal status is a hard gate: non-compoundable or delisted agents cannot be filled and are blocked from protocol export. Keep 503A status current.