Gonadotropin hormone releasing hormones (GnRH) set a flow in the secretion of gonadotropins, i.e. follicle stimulating hormone (FSH) and luteinizing hormone (LH), both of which are considered to manage and regulate the endocrine functioning and maturation of the gonads (1).
Gonadorelin is a synthetic peptide composed of ten amino acids, all joined to one another in a sequential form (3). Gonadorelin is structurally similar to the endogenous GnRH, except for 1-2 amino acid changes in the sequence (4). Structurally identical to the endogenous GnRH hormones, Gonadorelin has been dubbed a GnRH agonist by researchers and exhibits some potential in regulating the levels of gonadotropins and maintaining regular reproductive functions (3).
The peptide has been suggested to stimulate the synthesis and release of gonadotropins luteinizing hormone and follicle stimulating hormone by possibly stimulating the anterior pituitary gland (5). This is mainly the reason why Gonadorelin is referred to by researchers as a “GnRH agonist”, as it may possibly induce the same action as GnRH.
Researchers have suggested that Gonadorelin may induce downregulation of the GnRH receptors located at the pituitary gland. This is the peptide hormone that binds to the receptors, which at first, for a short period, may stimulate the secretion of the gonadotropins. Eventually, scientists believe the receptors become less sensitive towards this peptide, aka downregulation of the receptors, which then reversibly inhibits the release of luteinizing hormone and follicle stimulating hormone (5). Research on this peptide and other GnRH analogs are underway, and several research hypotheses have been presented, some summarized below (7):
- Gonadorelin may help researchers meter hypothalamus and pituitary gland functions
- The peptide may possibly induce ovulation
- May be a potential anti-carcinogen agent
- May reduce the likelihood of neurological deterioration
Research and Clinical Studies
Gonadorelin Peptide and Cancer Cells
Research in cancer cell proliferation in both clinical and animal studies suggest that excessive exposure of breast cells to mitogens, namely estrogen and progesterone, may increase the risk of developing cancer in those cells. Potentially blocking the action of these mitogens, and thereby reducing the exposure of the healthy cells to them, may reduce the risk of cancer development (8). Researchers are suggesting that GnRH agonists such as Gonadorelin may exhibit some potential in mitigating the action of mitogens in healthy cells. Studies (9) examining test subjects with high testosterone levels, a marker for hyperandrogenemia (a condition characterized by excessive androgen synthesis), are at higher risk of developing breast cancer. The source of androgen, and thereby the potential source of breast cancer, may possibly be counteracted with GnRH analogs, as researchers are hypothesizing that the peptide may induce a reduction in the substrate for estrogen synthesis, but may not necessarily inhibit the synthesis of estrogen completely.
Researchers have also explored the potential of Gonadorelin in experimental studies intended to inhibit the production of luteinizing hormones. The researchers suggested that due to the downregulation potential of GnRH receptors, it may induce a decline in the testosterone and dihydrotestosterone production. Development of carcinogenic cells in male test subjects may depend on these testosterone levels, which, by the use of GnRH analogs, might be inhibited. (10)
Gonadorelin Peptide and Spermatogenesis, Gonadotropins
In this clinical trial (11), seven male test subjects were presented a GnRH analogue every day for up to 16 weeks, and a compound of testosterone enanthate bimonthly. Basal serum follicle stimulating hormone, luteinizing hormones and testosterone levels were monitored throughout the study period. After 14 to 16 weeks, it was noted by the researchers that the average sperm count in the test subjects had reportedly reduced by an average 93%, also causing azoospermia in three of the subjects, which is characterized by a complete absence of sperms in the ejaculate. Subsequently, once the study was completed, the average sperm count returned to normal indicating that the possible action of the peptide hormone may be reversible.
Gonadorelin Peptide and Neurological Deterioration
Research (12) has suggested that luteinizing hormones may have some impact on the brain, primarily the hippocampus, which is the memory center of the brain, and in some scenarios may possibly induce some dysfunction. These researchers posited that one way of mitigating neurological dysfunction may be to block the production and release of luteinizing hormones, which may possibly be achieved through introduction of GnRH analogs such as Gonadorelin. Testosterone has also been studied by scientists for its potential to preserve memory function and may be beneficial to brain function. Hence, inhibiting the entire gonadal axis in test models may not be fully beneficial. This is why GnRH, which researchers suggest only induces selective inhibitory action on luteinizing hormones, may show potential for future research studies (13).
Gonadorelin Peptide and Diagnostics
In this clinical study (14), the synthetically developed peptide Gonadorelin was presented in 11 female test subjects during the middle of the follicular phase of the menstrual cycle. All subjects exhibited an apparent increase in the basal levels of gonadotropins following peptide presence. In addition, 10 test subjects with amenorrhea were presented with the peptide. Amenorrhea is characterized by irregular menstruation. After the study, researchers reported that basal levels of gonadotropins, particularly the luteinizing hormone levels, appeared to increase in the short term, but remained steady in the long term. This study suggested that the pituitary secretion of luteinizing hormones and follicle stimulating hormones by Gonadorelin may not not depend on the basal levels of these hormones, however, it may possibly depend on the functioning of the hypothalamic and pituitary axis. Researchers suggested that as a result of this study, there may be a positive correlation between the two, possibly that higher severity of the hypothalamic and pituitary axis disturbance, the more the secretion of the gonadotropins.
Gonadorelin peptide is available for research and laboratory purposes only. Please review and adhere to our Terms and Conditions before ordering.
1. Marques P, Skorupskaite K, George JT, et al. Physiology of GNRH and Gonadotropin Secretion. [Updated 2018 Jun 19]. In: Feingold KR, Anawalt B, Boyce A, et al., editors. Endotext. South Dartmouth (MA): MDText.com, Inc. https://www.ncbi.nlm.nih.gov/books/NBK279070/
2. Hypogonadotropic Hypogonadism. https://www.pennmedicine.org/for-patients-and-visitors/patient-information/conditions-treated-a-to-z/hypogonadotropic-hypogonadism
3. National Center for Biotechnology Information. PubChem Compound Summary for CID 638793, Gonadorelin. https://pubchem.ncbi.nlm.nih.gov/compound/Gonadorelin.
4. Philip GA Thomas, Alain Fontbonne, Drugs and reproduction. https://www.sciencedirect.com/topics/pharmacology-toxicology-and-pharmaceutical-science/gonadorelin-acetate
5. Lepor, Herbert. “Comparison of single-agent androgen suppression for advanced prostate cancer.” Reviews in urology vol. 7 Suppl 5,Suppl 5 (2005): S3-S12. https://www.ncbi.nlm.nih.gov/pmc/articles/PMC1477619/
7. Gonadorelin (Intravenous Route, Injection Route). https://www.mayoclinic.org/drugs-supplements/gonadorelin-intravenous-route-injection-route/description/drg-20067426
8. Spicer DV, Pike MC. Sex steroids and breast cancer prevention. J Natl Cancer Inst Monogr. 1994;(16):139-47. https://pubmed.ncbi.nlm.nih.gov/7999456/
9. Secreto G, Sieri S, Agnoli C, Grioni S, Muti P, Zumoff B, Sant M, Meneghini E, Krogh V. A novel approach to breast cancer prevention: reducing excessive ovarian androgen production in elderly women. Breast Cancer Res Treat. 2016 Aug;158(3):553-61. https://pubmed.ncbi.nlm.nih.gov/27393623/
10. Zerbib M. Analogues de la GnRH dans le traitement du cancer de la prostate [GnRH analogs and prostate cancer treatment]. Ann Urol (Paris). 2005 Oct;39 Suppl 3:S66-72. French. doi: 10.1016/s0003-4401(05)80011-7. https://pubmed.ncbi.nlm.nih.gov/16302714/
11. Bhasin S, Yuan QX, Steiner BS, Swerdloff RS. Hormonal effects of gonadotropin-releasing hormone (GnRH) agonist in men: effects of long term treatment with GnRH agonist infusion and androgen. J Clin Endocrinol Metab. 1987 Sep;65(3):568-74. https://pubmed.ncbi.nlm.nih.gov/3114307/
12. Rao CV. Involvement of Luteinizing Hormone in Alzheimer Disease Development in Elderly Women. Reprod Sci. 2017 Mar;24(3):355-368. https://pubmed.ncbi.nlm.nih.gov/27436369/
13. R.L Bowen, et al, Not All Androgen Deprivation Therapies Are Created Equal: Leuprolide and the Decreased Risk of Developing Alzheimer’s Disease, J. Clin. Oncol., vol 34, no. 23, p.2800, Aug 2016. https://ascopubs.org/doi/full/10.1200/JCO.2015.66.3997
14. Vesper B, Rohde W, Groot-Wassink T. Ein Beitrag zur klinischen Anwendung von Gonadorelin als Diagnostikum im Einfach- und Doppelbelastungstest [Clinical use of Gonadorelin as a diagnostic agent in one- and two-step tests]. Zentralbl Gynakol. 1986;108(23):1442-52. https://pubmed.ncbi.nlm.nih.gov/3103350/
15. Gonadorelin. https://go.drugbank.com/drugs/DB00644
NOTE: These products are intended for laboratory research use only. Gonadorelin for sale (10mg) is not intended for personal use. Please review and adhere to our Terms and Conditions before ordering.
Dr. Marinov (MD, Ph.D.) is a researcher and chief assistant professor in Preventative Medicine & Public Health. Prior to his professorship, Dr. Marinov practiced preventative, evidence-based medicine with an emphasis on Nutrition and Dietetics. He is widely published in international peer-reviewed scientific journals and specializes in peptide therapy research.