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Gonadorelin

Extensively Studied FDA Approved

Gonadotropin-Releasing Hormone | GnRH Agonist

Dose 100-200 mcg for single injections; 5-20 mcg per pulse for pulsatile therapy
Frequency 2-3 times weekly for fertility/TRT support; every 90-120 minutes for pulsatile therapy; single dose for diagnostic
Cycle Varies - diagnostic single use, fertility therapy ongoing, TRT support continuous
Storage Lyophilized: 2-8°C refrigerated; Reconstituted: 2-8°C refrigerated, use within 14 days due to short stability
Accumulation Plotter

Gonadorelin is a synthetic form of the naturally occurring gonadotropin-releasing hormone (GnRH). It stimulates the pituitary gland to release follicle-stimulating hormone (FSH) and luteinizing hormone (LH), which in turn regulate testosterone production in men and ovulation in women. It is FDA-approved for diagnostic testing and fertility treatment. The pulsatile nature of GnRH secretion is critical for proper reproductive function.

Mechanism of Action

Gonadorelin acts as an agonist of the GnRH receptor in the anterior pituitary. When administered in pulses (mimicking natural secretion patterns every 60-120 minutes), it stimulates release of FSH and LH. LH then stimulates Leydig cells in the testes to produce testosterone, or triggers ovulation in women. Continuous exposure paradoxically causes receptor downregulation and suppressed hormone production.

Key Benefits

  • Stimulates natural testosterone production
  • Maintains testicular function during hormone therapy
  • Supports fertility in hypogonadal conditions
  • FDA-approved for diagnostic and therapeutic use
  • Can restore LH and FSH pulsatility
  • Alternative to hCG for testicular stimulation
  • Preserves endogenous hormone production
Molecular Weight
1,182.3 Da
Chain Length
10 amino acids
Type
Decapeptide
Amino Acid Sequence
One-letter: ?HWSYGLRPG?
H₂N
H
? 1
O ‖ C
N
H 2
O ‖ C
N
W 3
O ‖ C
N
S 4
O ‖ C
N
Y 5
O ‖ C
N
H
G 6
O ‖ C
N
L 7
O ‖ C
N
R 8
O ‖ C
N
P 9
O ‖ C
N
H
G 10
O ‖ C
N
H
? 11
COOH
pGl
1

pGlu

Position 1

His
2

Histidine

Position 2

Trp
3

Tryptophan

Position 3

Ser
4

Serine

Position 4

Tyr
5

Tyrosine

Position 5

Gly
6

Glycine

Position 6

Leu
7

Leucine

Position 7

Arg
8

Arginine

Position 8

Pro
9

Proline

Position 9

Gly
10

Glycine

Position 10

NH2
11

NH2

Position 11

N-terminus C-terminus
Hydrophobic
Polar
Positive (+)
Negative (-)
Modified

Fertility & Reproductive

  • Hypogonadotropic Hypogonadism

    Treatment of conditions like Kallmann syndrome where GnRH deficiency causes low testosterone and infertility.

  • Ovulation Induction

    Induces ovulation in women with hypothalamic amenorrhea who don't ovulate regularly.

  • Male Fertility

    Stimulates testosterone and sperm production by restoring LH/FSH pulsatility.

  • Delayed Puberty

    Treatment of delayed puberty due to hypothalamic-pituitary dysfunction.

Diagnostic

  • Pituitary Function Testing

    Used to assess hypothalamic-pituitary function and diagnose GnRH deficiency.

  • LH/FSH Response Assessment

    Evaluates pituitary reserve and responsiveness to GnRH stimulation.

Hormone Optimization

  • TRT Support

    Maintains testicular function and fertility during testosterone replacement therapy.

  • Post-Cycle Therapy

    Helps restore natural testosterone production after anabolic steroid use.

  • Cryptorchidism

    Treatment of undescended testes in pediatric patients.

Can be administered as single injections or via pulsatile infusion pump. Single injections are used for diagnostic testing, while pulsatile administration mimics natural GnRH secretion for therapeutic purposes. Very short half-life (10-40 minutes) requires careful dosing strategy.

GoalDoseFrequencyRoute
Diagnostic testing100 mcgSingle injectionSubQ or IV
Fertility support50-100 mcg2-3x weeklySubQ
Pulsatile therapy5-20 mcg per pulseEvery 90-120 minSubQ pump
TRT adjunct100-200 mcg2-3x weeklySubQ

Reconstitution Instructions

Materials Needed:
  • Bacteriostatic water (BAC)
  • Insulin syringes (0.5-1 mL)
  • Alcohol swabs
  • Peptide vial
  • Sterile work surface
  1. 1 Clean work area and hands thoroughly
  2. 2 Calculate required BAC water volume
  3. 3 Draw BAC water into syringe
  4. 4 Inject slowly down vial side (not directly onto powder)
  5. 5 Gently swirl until dissolved (never shake)
  6. 6 Store in refrigerator, use within 14 days
hCG

Often used as alternative to hCG for testicular stimulation during TRT.

compatible
Testosterone

Used alongside TRT to maintain testicular function and fertility.

synergistic
Clomiphene

Can be combined in fertility and PCT protocols.

compatible
Kisspeptin

Kisspeptin stimulates GnRH release; can work together for hormone optimization.

synergistic
Within minutes

LH and FSH release begins

Hours

Testosterone increase in response to LH

Week 1-2

Improved hormonal markers on blood tests

Week 2-4

Restoration of natural hormone pulsatility

Ongoing

Maintained testicular function and fertility

Common Side Effects

  • Injection site reactions
  • Headache
  • Flushing
  • Nausea
  • Abdominal discomfort

Stop Signs - Discontinue if:

  • Signs of allergic reaction (rash, difficulty breathing)
  • Severe headaches
  • Unusual abdominal pain

Contraindications

  • Hormone-sensitive tumors
  • Pregnancy
  • Hypersensitivity to GnRH or analogs
  • Conditions worsened by sex hormone release

Good Signs

  • White lyophilized powder
  • Clear solution after reconstitution
  • Intact vacuum seal

Warning Signs

  • Slight clumping that dissolves easily

Bad Signs

  • Discolored powder
  • Cloudy or particulate solution
  • Broken seal
  • Gonadorelin in Hypogonadotropic Hypogonadism
    Journal of Clinical Endocrinology & Metabolism (2018)

    Pulsatile GnRH administration effectively restores fertility in patients with hypothalamic hypogonadism.

  • GnRH Pulsatility and Reproductive Function
    Frontiers in Endocrinology (2020)

    Pulsatile GnRH secretion (every 60-120 min) is essential for proper FSH/LH release and reproductive function.

  • Gonadorelin for Ovulation Induction
    Fertility and Sterility (2015)

    Effective treatment for ovulation induction in women with hypothalamic amenorrhea.

Disclaimer

This information is for educational and research purposes only. Consult a healthcare professional before use.