Skip to main content
PepStack

Gonadorelin

Hormonal Axis
GnRHGonadotropin-Releasing HormoneFactrel

Overview

Gonadorelin, also known as GnRH or Gonadotropin-Releasing Hormone, is a decapeptide hormone that plays a crucial role in the regulation of the reproductive system. It is synthesized in the hypothalamus and is responsible for the release of two key gonadotropins: luteinizing hormone (LH) and follicle-stimulating hormone (FSH) from the anterior pituitary gland. The structure of gonadorelin consists of ten amino acids, and it is typically synthesized using solid-phase peptide synthesis techniques for research and clinical applications. Researchers have investigated gonadorelin primarily in the context of reproductive health and endocrinology. It has been observed to influence the onset of puberty, fertility treatments, and the management of reproductive disorders. Additionally, gonadorelin is used in diagnostic tests to assess pituitary function and in the treatment of hormone-responsive cancers. The mechanism of action of gonadorelin involves binding to specific GnRH receptors on the pituitary gland, which triggers a signaling cascade leading to the secretion of LH and FSH. These hormones then act on the gonads to stimulate the production of sex steroids and gametes. Pharmacokinetically, gonadorelin has a short half-life, with intravenous administration resulting in a half-life of approximately 2 to 4 minutes. Its stability and bioavailability vary depending on the route of administration, with subcutaneous and intramuscular routes providing more sustained effects. Currently, gonadorelin is approved for use in specific diagnostic and therapeutic contexts. It is regulated by health authorities in various countries, with its use primarily confined to clinical and research settings. Researchers continue to explore its potential applications in reproductive medicine and oncology.

Mechanism of Action

Gonadorelin acts by binding to GnRH receptors located on the surface of pituitary gonadotroph cells. This binding activates the phospholipase C pathway, leading to the release of calcium ions and the subsequent secretion of luteinizing hormone (LH) and follicle-stimulating hormone (FSH). These hormones are critical for the regulation of the reproductive system.

Molecular Data

FormulaC55H75N17O13
Molecular Weight1182.3 g/mol
CAS Number33515-09-2
PubChem CID638793

Half-Life

SubcutaneousData limited
IntramuscularData limited
Intravenous~2 to 4 minutes
IntranasalData limited
OralPoor bioavailability

Gonadorelin is rapidly metabolized and cleared from the circulation, necessitating specific routes of administration for sustained effects.

Storage

Lyophilized

Stable for 2+ years at -20°C, 12 months at 4°C

Reconstituted

Use within 14 days when refrigerated at 4°C

Avoid

Avoid repeated freeze-thaw cycles, direct light

Solvent

Bacteriostatic water or sterile saline recommended

Solubility

Gonadorelin is soluble in water and aqueous buffers but has limited solubility in organic solvents like acetonitrile and DMSO.

Legal Status

🇩🇪DE

Not approved as a medicinal product. Not a controlled substance. Sale as research chemical is a legal grey area.

🇺🇸US

Approved by the FDA for specific diagnostic and therapeutic uses. Not a controlled substance.

🇦🇺AU

Listed in the Australian Register of Therapeutic Goods for specific uses. Not a controlled substance.

🇬🇧UK

Approved by the MHRA for specific medical uses. Not a controlled substance.

Legal status information is provided for general reference only and may not reflect the most current regulatory changes. Always verify with official government sources before making any decisions.

9 Research Publications

Gonadotropin-Releasing Hormone (GnRH)/GnRH Receptors and Their Role in the Treatment of Endometriosis.

Review

Cureus · 2023

Researchers reviewed the role of gonadotropin-releasing hormone (GnRH) and its receptors in the treatment of endometriosis, a common condition where tissue similar to the uterine lining grows outside the uterus. They highlighted the potential of GnRH analogs and antagonists as innovative treatment options, emphasizing the need for further research in this area.

  • Endometriosis affects 6%-10% of women in the general population and 35%-50% of those with pain or infertility.
  • GnRH I, released by the hypothalamus, plays various roles in the body, including in the nervous system.
  • The study suggests that new treatments using GnRH II or antagonists of the GnRH I receptor could be promising for managing endometriosis.
PubMed

Gonadotropin-releasing hormone (GnRH) measurements in pituitary portal blood: A history.

Review

Journal of neuroendocrinology · 2022

Researchers reviewed the history of measuring gonadotropin-releasing hormone (GnRH) and luteinizing hormone (LH) to better understand reproductive control. They found that while LH levels in blood are often used as indicators of GnRH release, this method has limitations and does not always accurately reflect GnRH patterns.

  • Researchers observed that LH measurements in peripheral blood may not accurately represent the release of GnRH from the hypothalamus.
  • The study highlighted the development of portal blood collection methods to directly measure GnRH levels.
  • Researchers found that under certain conditions, the pituitary gland does not effectively indicate GnRH release patterns.
PubMed

Hypothalamic mechanisms of obesity-associated disturbance of hypothalamic-pituitary-ovarian axis.

Review

Trends in endocrinology and metabolism: TEM · 2022

Researchers reviewed how obesity affects the hormonal regulation of ovulation in women. They found that the hypothalamus, which plays a crucial role in ovulation, is influenced by metabolic signals and inflammation, leading to ovulatory disorders commonly seen in obese women. The study highlights the need for further research to develop new treatments for these hormonal imbalances.

  • Researchers observed that ovulatory disorders are prevalent among obese women due to disruptions in the hypothalamic-pituitary-ovarian axis.
  • The hypothalamus receives metabolic signals that regulate the release of gonadotropin-releasing hormone (GnRH), essential for ovulation.
  • Inflammation in the hypothalamus can also impact ovulation independently of obesity.
PubMed

Role of Gonadotropin-Releasing Hormone (GnRH) in Ovarian Cancer.

Review

Cells · 2021

Researchers reviewed the role of gonadotropin-releasing hormone (GnRH) in ovarian cancer. They found that GnRH is involved in the growth and spread of ovarian tumors, acting both directly on cancer cells and indirectly through the hormonal regulation system in the body.

  • GnRH receptors are present not only in the pituitary gland but also in the ovaries and ovarian tumors.
  • GnRH influences ovarian cancer cell growth and metastasis through both direct and indirect mechanisms.
  • The study provides insights into how GnRH could be linked to ovarian cancer development and potential treatment strategies.
PubMed

The Role of Gonadotropin-Releasing Hormone (GnRH) in Endometrial Cancer.

Review

Cells · 2021

Researchers reviewed the role of Gonadotropin-Releasing Hormone (GnRH) in endometrial cancer, a common type of cancer in women. They found that many endometrial cancer cells express GnRH and its receptor, which may influence cell growth and death. The study also highlighted that certain GnRH-based treatments showed promise in early-stage cancer but had limited effectiveness in advanced cases.

  • Researchers observed that most endometrial cancer cells express GnRH and its receptor, suggesting a role in regulating cancer cell behavior.
  • The study found that GnRH agonists can inhibit cancer cell growth and induce cell death in laboratory models.
  • Researchers noted that while some GnRH treatments showed potential in early-stage endometrial cancer, they were less effective in advanced or recurrent cases.
PubMed

Gonadotropin-Releasing Hormone and GnRH Receptor: Structure, Function and Drug Development.

Review

Current medicinal chemistry · 2020

Researchers reviewed the role of Gonadotropin-Releasing Hormone (GnRH) and its receptor in human reproduction and how their dysfunction can lead to various cancers and disorders. They highlighted the development of drugs targeting this system, including agonists and antagonists, which could improve treatment options. This study provides insights into the complex functions of GnRH and its receptor, paving the way for new drug designs.

  • Researchers observed that GnRH is crucial for sexual maturation and reproductive regulation in humans.
  • They found that dysfunctions in the GnRH-GnRHR complex can lead to cancer and other disorders.
  • The study highlighted the potential of GnRHR as a drug target, leading to the development of various therapeutic molecules.
PubMed

Gonadotropin-releasing hormone analog therapeutics.

Review

Minerva ginecologica · 2018

Researchers reviewed the role of gonadotropin-releasing hormone (GnRH) analogs in managing hormone-related health issues, such as puberty disorders, infertility, and certain cancers. They found that these analogs are effective in regulating the hypothalamic-pituitary-gonadal axis and have potential in assisted reproductive therapies.

  • GnRH dysregulation can lead to various hormone-dependent diseases.
  • GnRH analogs are effective in treating conditions related to the HPG axis.
  • These analogs also play a significant role in assisted reproductive technologies.
PubMed

Gonadotropin-releasing hormone antagonists.

Review

Current opinion in pharmacology · 2003

Researchers observed that gonadotropin-releasing hormone (GnRH) antagonists can block the hormone's action, which may lead to new treatments for various hormone-related conditions. These compounds are currently being tested for use in assisted reproduction and could potentially be used for male contraception and to inhibit certain cancers. The study highlights the expanding role of GnRH antagonists in medicine.

  • GnRH antagonists inhibit the hormone from binding to its receptor, effectively reducing hormone activity.
  • These compounds are in clinical trials for assisted reproduction and may soon be available for broader applications.
  • Potential future uses include hormonal male contraception and targeting specific cancer cells.
PubMed

Gonadotropin-releasing hormone.

In Vitro

The New England journal of medicine · 1977

Researchers studied gonadotropin-releasing hormone (GnRH) and its effect on luteinizing hormone (LH) release in a lab setting. They found that LH can still be released in the absence of calcium, suggesting that calcium is not essential for this process. Additionally, the study proposes that GnRH receptors may have different forms that can affect how cells respond to hormonal signals.

  • Researchers found that luteinizing hormone (LH) can be released in response to GnRH even without calcium.
  • The absence of calcium prevented LH release in response to other stimuli, indicating a specific role for GnRH.
  • The study suggests that GnRH receptor proteins may exist in different forms that influence cell signaling and hormone release.
PubMed

Track Gonadorelin in PepStack

Log your research cycles, set reminders and visualize serum levels.

This page is for informational and research purposes only. All information is based on published scientific literature. Nothing on this page constitutes medical advice or replaces consultation with a qualified healthcare professional.