Page data last changed: . Registry refreshes and identity assessments are separate from scientific content review.
The reproductive axis's master switch, ten residues long: pulsed, it turns the gonads on; given continuously, its analogues turn them off.
Also known as: GnRH · GnRH-I · LHRH · gonadorelin acetate · gonadorelin hydrochloride · Fertagyl (veterinary)
Part of the Foundational & therapeutic peptides cluster
Overview
Gonadorelin is the synthetic form of gonadotropin-releasing hormone (GnRH, also LHRH), the hypothalamic decapeptide pGlu-His-Trp-Ser-Tyr-Gly-Leu-Arg-Pro-Gly-NH2 that drives pituitary release of luteinising and follicle-stimulating hormone. It is chemically identical to the human hormone, has a half-life of minutes, and is used as a diagnostic stimulation test, in pulsatile-pump fertility treatment, and extensively in veterinary reproduction. Its long-acting agonist and antagonist analogues — leuprolide, triptorelin, ganirelix and others — are separate profiles.
Source & context
Biological / chemical source: Synthetic form identical to endogenous gonadotropin-releasing hormone
Primary research or clinical context: Approved in various markets as a diagnostic agent for pituitary function and, by pulsatile pump, for fertility; widely approved in veterinary medicine; not a research-only compound
What gonadorelin is
Gonadorelin is the synthetic, chemically identical form of gonadotropin-releasing hormone (GnRH), the ten-residue peptide that hypothalamic neurons release in pulses to tell the pituitary to secrete luteinising hormone (LH) and follicle-stimulating hormone (FSH). Historically it was called luteinising-hormone-releasing hormone (LHRH), and PubChem lists it under both names and under the veterinary brand Fertagyl. Formula C55H75N17O13, average mass about 1,182 Da, CAS 33515-09-2. Because it is the native hormone rather than an analogue, everything about its behaviour — a half-life of minutes, and opposite effects depending on whether it is pulsed or sustained — is the physiology of the reproductive axis itself.
Sequence and chemistry
The sequence is pGlu-His-Trp-Ser-Tyr-Gly-Leu-Arg-Pro-Gly-NH2. The N-terminal pyroglutamate (a cyclised glutamine) and the C-terminal glycinamide are native features that already protect the ends from exopeptidases; what limits the hormone's life is endopeptidase cleavage at the Gly6–Leu7 and Pro9–Gly10 bonds. Every long-acting agonist analogue — leuprolide, triptorelin, buserelin, nafarelin — substitutes a D-amino acid at position 6 and modifies or replaces glycine 10 for exactly that reason, while antagonists such as ganirelix rebuild the N-terminus as well. Gonadorelin is the reference point those profiles are measured against.
Mechanism: pulse frequency is the message
GnRH acts on a single receptor on pituitary gonadotrophs, but the outcome depends on timing. The hypothalamus releases it roughly hourly; each pulse triggers LH and FSH release, and the pulse frequency encodes which gonadotropin dominates. Continuous exposure does the opposite: the receptor is internalised and desensitised within days and gonadotropin output collapses. That single fact explains the whole drug family. Gonadorelin, with its minutes-long half-life, is used when a physiological pulse is wanted; agonist analogues with hours-long half-lives are used precisely because their sustained signal shuts the axis down, which is how they treat prostate cancer, endometriosis and precocious puberty.
| Signal | Receptor response | Effect on LH / FSH | Used for |
|---|---|---|---|
| Pulsatile (gonadorelin by pump) | Normal activation | Physiological release | Hypothalamic amenorrhoea, ovulation induction |
| Single bolus (gonadorelin) | Acute activation | LH surge measured | Pituitary stimulation test |
| Continuous (agonist analogues) | Desensitisation | Suppressed after initial flare | Prostate cancer, endometriosis, puberty suppression |
| Blockade (antagonists) | Competitive inhibition | Suppressed immediately | IVF, prostate cancer |
Human uses
Gonadorelin's human uses follow from its short action. As a diagnostic, a single dose provokes a measurable LH and FSH response that tests pituitary gonadotroph function. In fertility medicine it can be delivered by a portable pump that mimics the natural pulse to induce ovulation in women whose own hypothalamic signal is absent. Availability differs by country and formulation, and the human products have been discontinued or replaced in some markets, so approval status should be checked locally. The literature returned for the name is dominated by reviews of GnRH-analogue therapy in endometriosis, heavy menstrual bleeding and breast disease, which concern the long-acting analogues rather than gonadorelin itself.
Veterinary use
Gonadorelin is far more widely used in animals than in people. Products such as Fertagyl are approved for cattle to treat cystic ovaries and to synchronise ovulation in timed-insemination programmes, and it is used in other livestock and companion-animal reproduction. That veterinary market is one reason the peptide is inexpensive and widely available, and one reason it appears in grey-market listings alongside human research peptides.
The grey-market context
Gonadorelin is sold online to men using exogenous testosterone in the belief that it will maintain testicular function, on the model of human chorionic gonadotropin. The physiology above explains the difficulty: a peptide with a half-life of minutes produces a brief pulse, and the effect of intermittent self-injection on LH output has not been studied in controlled trials. The registered-trial count on ClinicalTrials.gov for the term “gonadorelin” — over a thousand — reflects analogue trials that match the name, not studies of this use. This profile is educational and does not offer guidance on any regimen.
Status
Gonadorelin is an approved active substance in human diagnostic and fertility products in various jurisdictions and in veterinary products in most, with the specific human products varying by country. It is not a controlled substance. Material sold as a research chemical for human self-administration is outside any approval and of unverified content. This page is not medical advice.
Sequence of the selected reference form
Sequence backbone for the reference form: Gonadorelin parent GnRH-I amide. Termini, stereochemistry and modifications are described below.
XHWSYGLRPG
X1 is L-pyroglutamate; Gly10 is amidated.. X marks a noncanonical residue; see the expanded sequence and reference chemistry below.
Analyze sequences in the playground →Structure & chemistry
Molecular identity & reference confidence
Source-supported reference
The selected mammalian GnRH-I parent has pyroglutamate1 and Gly10 amidation. Official labels distinguish this parent from acetate/HCl salts. The old linked CID returns a different molecular formula, not the selected gonadorelin formula.
- Molecular form
- Gonadorelin parent GnRH-I amide
- Species
- Mammalian GnRH-I sequence; bovine endogenous identity is explicitly documented in the veterinary label
- Termini (N / C)
- L-pyroglutamyl lactam / Glycinamide (Gly10-NH2)
Average reference mass · Molecular identity assessment: 2026-10-05
Reference policy updated: 2026-10-05
- PubChem PUG REST selected parent properties · 2026-10-05
- PubChem selected-parent biologic notation · 2026-10-05
- PubChem selected-parent identifiers with depositor attribution · 2026-10-05
- NIH GSRS independently selected parent record · 2026-10-05
- Official product label chemical description, selected parent distinguished from formulation · 2026-10-05
H-Pyr-His-Trp-Ser-Tyr-Gly-Leu-Arg-Pro-Gly-NH2
- Molecular formula
- C55H75N17O13
- Average reference mass
- ≈ 1,182.3
- Plasma half-life
- Minutes — rapidly cleaved by peptidases at Gly6-Leu7 and Pro9-Gly10; the reason its analogues substitute those positions
- Receptors
- GnRH receptor (GnRHR), a Gq-coupled receptor on pituitary gonadotrophs; pulsatile activation releases LH and FSH, continuous activation desensitises the receptor
- Backbone
- Gonadorelin parent GnRH-I amide
- C-terminus
- Glycinamide (Gly10-NH2)
- Status
- Approved: diagnostic and pulsatile-fertility use in various human markets; veterinary products (e.g. Fertagyl) widely approved
- PubChem CID: 638793
- CAS RN: 33515-09-2
- UNII: 9O7312W37G
Chemistry values: curated profile, PubChem.
Clinical development snapshot
ClinicalTrials.gov lists 1,162 registered studies with “Gonadorelin” as an intervention (snapshot 2026-10-01). A registry footprint is not evidence of efficacy or approval.
| NCT | Title | Phase | Status | Updated |
|---|---|---|---|---|
| NCT07460752 | Evaluation of Alternative Site Goserelin Acetate Injection for Ovarian Function Suppression (OFS) in Local and | Phase 2 | recruiting | 2026-10-01 |
| NCT02115282 | Exemestane With or Without Entinostat in Treating Patients With Recurrent Hormone Receptor-Positive Breast Can | Phase 3 | active not recruiting | 2026-10-01 |
| NCT07235917 | A Study to Investigate Mibavademab in Adult Women With Functional Hypothalamic Amenorrhea | Phase 2 | recruiting | 2026-10-01 |
| NCT05161195 | Roll-over Study to Allow Continued Access to Ribociclib | Phase 4 | active not recruiting | 2026-10-01 |
| NCT05827081 | Phase IIIb Study of Ribociclib + ET in Early Breast Cancer | Phase 3 | recruiting | 2026-10-01 |
| NCT01630967 | Efficacy Study of Switching to a Lutenizing Hormone-releasing Hormone (LHRH) Antagonist From a LHRH Agonist to | Phase 2 | withdrawn | 2026-10-01 |
Gonadorelin — reconstitution calculator
Enter how much peptide is in the vial and how much diluent (e.g. bacteriostatic water) is added. The tool returns the resulting solution concentration — and, for any amount you type, the volume it corresponds to. This is educational arithmetic, not a dosing recommendation.
Reference form: Gonadorelin parent GnRH-I amideAverage reference mass: 1,182.32 Da
Enter an amount to see the volume it corresponds to.
Educational concentration mathematics only. This tool does not recommend a dose, amount, or protocol, and nothing here is medical advice. Many peptides are not authorized by Health Canada for human use — see our reconstitution and bacteriostatic-water guides for context.
Change log
Dated observations from the data pipeline (registry flags, trial footprints, identifiers) and editorial reviews of this profile.
- ChemistryPubChem formula updated to C55H75N17O13.
- Trials6 registered studies added on ClinicalTrials.gov (now 1162).
- EditorialProfile content reviewed and updated by the editorial team.
FAQ about Gonadorelin
What is Gonadorelin?+
Gonadorelin is the synthetic form of gonadotropin-releasing hormone (GnRH, also LHRH), the hypothalamic decapeptide pGlu-His-Trp-Ser-Tyr-Gly-Leu-Arg-Pro-Gly-NH2 that drives pituitary release of luteinising and follicle-stimulating hormone. It is chemically identical to the human hormone, has a half-life of minutes, and is used as a diagnostic stimulation test, in pulsatile-pump fertility treatment, and extensively in veterinary reproduction. Its long-acting agonist and antagonist analogues — leuprolide, triptorelin, ganirelix and others — are separate profiles.
What Canadian product status is recorded for Gonadorelin?+
Canadian product status for Gonadorelin has not been verified in this profile. No verified record here does not mean no authorization exists. Status depends on the product, formulation and use; consult Health Canada's product records.
What is the length of the selected reference form for Gonadorelin?+
The selected reference form (Gonadorelin parent GnRH-I amide) has 10 residues or residue-derived units in its backbone. Other forms in this family may have a different length.
What is gonadorelin?+
The synthetic form of gonadotropin-releasing hormone (GnRH/LHRH), the ten-residue hypothalamic peptide that triggers pituitary release of LH and FSH. It is identical to the human hormone.
How does gonadorelin work?+
It activates the pituitary GnRH receptor. Given in pulses it releases LH and FSH; given continuously, GnRH signalling desensitises the receptor and suppresses them — which is how its long-acting analogues work.
What is gonadorelin used for?+
Pituitary stimulation testing, pulsatile-pump ovulation induction, and, widely, veterinary reproduction (cattle ovulation synchronisation).
What is the sequence of gonadorelin?+
pGlu-His-Trp-Ser-Tyr-Gly-Leu-Arg-Pro-Gly-NH2; formula C55H75N17O13, mass about 1,182 Da.
Gonadorelin vs HCG — are they the same?+
No. HCG is a large glycoprotein that acts directly on the gonads like LH; gonadorelin is a decapeptide that acts on the pituitary to release LH and FSH, and only for minutes per dose.
Is gonadorelin approved?+
Yes, as a diagnostic and pulsatile-fertility agent in various human markets and in veterinary products; specific human products vary by country.
Further reading
- PK conceptsWhy Peptides Have Short Half-Lives (And How Engineers Fix It)Proteases, renal clearance, DPP-4, PEGylation, lipidation, cyclization—educational guide to peptide pharmacokinetics concepts.
- FoundationsWhat Are Research Peptides? A Clear Educational GuideLearn what “research peptides” means, how they differ from approved peptide drugs, quality markers (COA, purity), and how to study them responsibly.
- CanadaAre Peptides Legal in Canada? A Regulatory GuideAn educational overview of how Health Canada regulates peptides—drug authorization, DINs, the “research use only” gray area, and import ambiguity. Not legal advice.
Related peptides
References & further reading
- 1.Hashem et al. (2020). Reproductive performance of goats treated with free gonadorelin or nanoconjugated gonadorelin at estrus. Domest Anim Endocrinol
- 2.Akın et al. (2015). Anaphylaxis to gonadorelin acetate in a girl with central precocious puberty. J Pediatr Endocrinol Metab
- 3.Chenault et al. (1990). LH and FSH response of Holstein heifers to fertirelin acetate, gonadorelin and buserelin. Theriogenology
- 4.Silva et al. (2017). A comparative study of the effects of intramuscular administration of gonadorelin, mating and intrauterine infusion of either raw seminal plasma or seminal plasma purified β-NGF on luteal development in llamas. Reprod Domest Anim
- 5.Picard-Hagen et al. (2015). Effect of gonadorelin, lecirelin, and buserelin on LH surge, ovulation, and progesterone in cattle. Theriogenology
- 6.Kesler et al. (1999). Gonadorelin-induced testosterone release: a biological assay for quality assurance of gonadorelin in veterinary medicine. Drug Dev Ind Pharm
- 7.Wong et al. (1990). Stability and purity profile of gonadorelin acetate: a high-purity gonadotropin-releasing hormone. Int J Fertil
- 8.Janakiram et al. (2014). Raloxifene and antiestrogenic gonadorelin inhibits intestinal tumorigenesis by modulating immune cells and decreasing stem-like cells. Cancer Prev Res (Phila)
- 9.IUPHAR/BPS Guide to Pharmacology — gonadotrophin-releasing hormone receptor and GnRH ligands
- 10.PubChem — Gonadorelin (CID 638793)
- 11.Ferrero et al. (2010). Endometriosis. BMJ Clinical Evidence (GnRH-analogue therapy review)
- 12.Duckitt & McCully (2012). Menorrhagia. BMJ Clinical Evidence (GnRH-analogue therapy review)
- 13.Wikipedia — Gonadorelin