Gonadorelin
approvedAlso known as: GnRH, LHRH, Factrel
**Mechanism of Action** Gonadorelin is a synthetic decapeptide identical to endogenous gonadotropin-releasing hormone (GnRH). It binds to GnRH receptors on anterior pituitary gonadotroph cells, stimulating the synthesis and pulsatile release of luteinizing hormone (LH) and follicle-stimulating hormone (FSH). This action is dose- and frequency-dependent: pulsatile administration mimics physiological GnRH release, promoting gonadal steroidogenesis and gametogenesis, while continuous exposure paradoxically suppresses gonadotropin secretion via receptor desensitization. **Key Research Findings** Clinical studies confirm that intravenous or subcutaneous gonadorelin reliably induces LH/FSH peaks within 30 minutes, making it a standard diagnostic tool for hypothalamic-pituitary-gonadal axis integrity (e.g., in delayed puberty or hypogonadotropic hypogonadism). Research also demonstrates its efficacy in controlled ovarian stimulation protocols for assisted reproduction, though pulsatile delivery systems are required to avoid downregulation. Long-term continuous use is not recommended due to desensitization effects. **Clinical Relevance** Gonadorelin is FDA-approved for diagnostic testing of pituitary function and for induction of ovulation in select anovulatory women with intact pituitary function. Its therapeutic use is limited by short half-life (~4 minutes) and need for precise pulsatile administration. Off-label applications include male hypogonadism and cryptorchidism, though newer GnRH analogs with longer half-lives are often preferred. For research purposes only — not medical advice.
Key data
C55H75N17O13Research & studies
Bremelanotide and Tesamorelin are the most clinically established peptides, with defined dosing and regulatory approval for selected indications.; Kisspeptin shows early promise but remains investigational; Oxytocin has biologic plausibility but limited efficacy data; PnPP-19 remains preclinical.; Growth hormone secretagogues reliably increase GH and IGF-1 concentrations, but evidence for improved sexual function, physical performance, or quality of life remains limited.; Melanotan II, Ibutamoren, CJC-1295, and related agents remain accessible through unregulated markets, raising concerns about product quality, dosing variability, and incompletely characterized adverse effects.
Kp10 induced ovulation in 87.5% of does, comparable to gonadorelin, with similar corpora lutea counts per ovulated doe (12.9 vs 14.6 CL/doe).; Day 7 plasma progesterone was significantly higher in GnRH-treated ovulated does than Kp10-treated ones (25.12 vs 9.47 ng/mL; p < 0.0211), while non-ovulated controls had minimal P4 (0.86 ng/mL).; Plasma estradiol showed no significant differences across days or groups (mean 32.74 pg/mL on day 0 and 37.27 pg/mL on day 7).; Histology confirmed Kp10 promoted preovulatory follicle development and CL formation mirroring GnRH, and enhanced angiogenesis via increased VEGF expression in more developed follicles and CL.
The model identified 2991 new DDIs involving 192 drugs used in female reproductive conditions and other unrelated treatments.; Most new DDIs involved estradiol, acetaminophen, bupivacaine, risperidone, and follitropin, with follitropin having the highest discovery rate at 42%.; Predicted 12 DDIs between oral contraceptives and HIV drugs that could compromise efficacy.; Among new DDIs, 23 were expected to improve therapies and 11 to cause harmful effects.
Efficient extraction of peptidic analytes from urine was achieved for insulins, growth hormone-releasing hormones, insulin-like growth factors, synacthen, gonadorelin, and mechano growth factors.; Five internal standards were used to cover all five included peptide drug categories.; The method fulfills nearly all WADA technical document requirements for minimum required performance levels.; Proof of principle was demonstrated using authentic post-administration urine samples for insulins and gonadorelin.
Bioanalytical methods have evolved toward simpler, on-site techniques with reduced time and costs.; Affinity reagent production has advanced from natural receptors to biomimetic, animal-free options like aptamers and MIPs.; Peptide hormone analysis remains challenging in biomedical, pharmaceutical, and anti-doping contexts.; Gonadorelin is highlighted as a neuropeptide misused in doping, driving interest in its detection.
A detection limit of 277 pmol L-1 for gonadorelin was achieved.; Reproducibility was good with average CV% of 4.07% in standard solutions and 5.24% in urine samples.; The assay showed adequate selectivity against non-specific control peptides.; Results were successfully validated by mass spectrometry, the reference anti-doping platform.
GnRH at AI did not improve ovulation rate, plasma progesterone 7 days post-AI, or pregnancy per AI in cows detected by traditional estrus detection or AAM.; No treatment effects were observed for pregnancy at P1 (32-45 days) or P2 (60-115 days) in either experiment.; High-activity cows in the AAM system had greater pregnancy per AI and lower pregnancy loss compared to low-activity cows, with no interaction with GnRH treatment.; The study does not support routine use of GnRH at estrus detection to enhance reproductive outcomes.
Both GnRH and NGnRH increased corpora lutea number and twinning rate compared to control.; GnRH treatment increased serum estradiol and progesterone concentrations more than NGnRH and control.; NGnRH achieved similar fertility and prolificacy to GnRH at a quarter of the dose.; Both treatments reduced estrus duration and pregnancy losses compared to control.
Frequently asked questions
What is Gonadorelin?
**Mechanism of Action** Gonadorelin is a synthetic decapeptide identical to endogenous gonadotropin-releasing hormone (GnRH). It binds to GnRH receptors on anterior pituitary gonadotroph cells, stimulating the synthesis and pulsatile release of luteinizing hormone (LH) and follicle-stimulating hormone (FSH). This actio
How does Gonadorelin work?
Synthetic GnRH decapeptide that stimulates pituitary LH and FSH release; used diagnostically and to support gonadal function.
What is the research status of Gonadorelin?
Gonadorelin is currently classified as approved, with 298 research references on record. This is for research purposes only and is not medical advice.
What is the molecular weight of Gonadorelin?
Gonadorelin has a molecular weight of approximately 1182.3 g/mol (formula C55H75N17O13).
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