Gonadorelin (GnRH) (10mg)

What is the Gonadorelin (GnRH) Peptide?

Gonadorelin (GnRH) is a decapeptide gonadotropin-releasing hormone agonist.^[1] It appears to work by stimulating the synthesis and release of luteinizing hormone and follicle-stimulating hormone. It is being researched in human medicine to treat infertility, irregular menstrual cycles, and hypogonadism. It is also studied for its potential as a diagnostic tool to assess pituitary function. Ongoing research has uncovered potential uses for Gonadorelin in treating breast, prostate, and Alzheimer’s disease.^[2]

Specifications

AKA: Growth Hormone Releasing Factor, Somatocrinin, Somatoliberin

Sequence: Pyr-His-Trp-Ser-Tyr-Gly-Leu-Arg-Pro-Gly

Molecular Formula: C55H75N17O13

Molecular Weight: 1182.311 g/mol

PubChem: 638793

CAS Number: 9034-40-6

Reconstitution: Required

Research

Gonadorelin Research and Breast Cancer Prevention
Studies suggest that the higher the lifetime exposure to estrogen, the more likely a woman will develop breast cancer. Women who start menstruating at a young age, start estrogen-based contraceptives, start hormone replacement therapy during menopause, or have late-onset menopause are at risk of developing breast cancer. Fortunately, with oral contraceptives, your risk decreases when you stop taking the pill, and eventually, the increased risk returns to baseline. Of course, contraception is a double-edged sword because its use increases the risk of breast cancer but reduces the risk of ovarian cancer. Some breast cancer cells require estrogen to grow, and minimizing estrogen production or blocking estrogen receptors is an established method for treating certain forms of breast cancer. Gonadorelin’s studies suggest that it can be used to control ovarian cancer, Estrogen production, and exhibits potential to prevent breast cancer.^[3] Scientists report that “Fusion of GnRH to hpRNase1 structure produced an enzyme, which could specifically target tumor cells.” This hypothesis is based on the idea that some women are at increased risk of developing breast cancer in the postmenopausal year due to genetic and environmental factors. Gonadorelin appears to be a safe and inexpensive therapy to use in these situations, making it an attractive potential in reducing the burden of cancer.^[4] Studies show that ten years of use of Gonadorelin may reduce the risk of breast cancer by up to 50%, and 15 years of use of Gonadorelin can reduce the risk by 70%.^[5] Further research is required in this area, however. The potential benefits of Gonadorelin go beyond breast cancer prevention. Studies have suggested that adjuvant anti-estrogen therapy reduces disease progression by 50% if the cancer is estrogen-sensitive. Cancer cells tend to develop resistance to them over time, so their effectiveness is limited. This resistance usually results from increased expression of estrogen receptors. It is impossible to block all estrogen receptors without serious side effects. Gonadorelin may avoid this problem primarily by reducing the expression of estrogen. It appears to directly reduce the growth of estrogen-sensitive cancers and increases receptor efficacy, blocks the substance, and prolongs its lifespan.^[6] Studies of postmenopausal women with hyperandrogenism have suggested further that long-term GnRH treatment lowers total estrogen levels and reduces the risk of developing breast cancer. This occurs without serious side effects and therefore may provide an alternative to previous treatments, surgical removal of the ovaries.^[7]

Gonadorelin and Prostate Cancer
The use of GnRH in men with prostate cancer began in 1979 and was known as medical castration. However, this treatment eventually led to interesting discoveries. Some androgens are formed locally in the prostate through a mechanism called intracrinology.^[8] Of course, this means that GnRH blockade is only partially effective in treating prostate cancer. With deeper investigation into the potential benefits of Gonadorelin, scientists have developed new medications approved by the FDA for the treatment of castration-resistant prostate cancer (CRPC). These substances provide a new line of defense against the progression and metastasis of prostate cancer. They can also be used prophylactically in older men. The use of Gonadorelin and new topical medications in treating prostate cancer is known as complex androgen deprivation (CAB). CAB, which combines effective screening and early detection, is one of the few treatments in oncology that offers treatment and remission.^[9] CAB can cure 99% of all prostate cancers when used effectively and with early detection.

Gonadorelin and Dementia
Studies show that sex hormones, especially Luteinizing Hormone (LH), act on the brain in ways beyond the realm of sexual dimorphism and fertility. Indeed, increased menopausal-related LH correlates with an increased incidence of Alzheimer’s disease and reduced memory capacity in humans and animals. Rats treated with LH exhibited poor memory and hippocampal dysfunction. This was a defect that was apparently remedied by the administration of LH blockers.^[10] Further research on LH observe that higher hormone levels are associated with increased neuropathology. In particular, LH has been shown to promote the formation of plaques associated with Alzheimer’s disease.^[11] The researchers conclude that “Reducing the LH levels by treatment with gonadotropin-releasing hormone agonists could provide therapeutic benefits.” Therefore, it may be assumed that lowering LH levels will help slow the progression of Alzheimer’s disease. Testosterone is beneficial to brain health and helps maintain cognitive function. Therefore, blocking the entire hypothalamus-pituitary-gondola axis is not always effective for treating Alzheimer’s disease. For this reason, scientists have sought to test Gonadorelin derivatives to see if selective disruption of LH production is possible and has potential benefits.^[12] One ongoing study suggests that Leuprolide, a common substance used to treat uterine fibroids and GnRH receptor agonists, may effectively reduce the risk of Alzheimer’s disease compared to other Gonadotropin analogs. In this situation, Leuprolide may be used to offset the risk of CAB for Alzheimer’s disease. In particular, researchers studied the apparent ability of Leuprolide to downregulate serum gonadotropin levels (especially LH) and found it generally sufficient to offset the effects of decreased testosterone.^[13] Researchers are currently working to understand how the genetic interactions of Alzheimer’s disease can be disrupted to treat and prevent Alzheimer’s disease. Gonadorelin is an important peptide in this study.

The Future of Gonadorelin Research

Gonadorelin has long been researched for its potential for treating human and mammalian diseases. Still, researchers are constantly discovering new ways in which GnRH and GnRH analogs act in normal physiology and disease development. The discovery that Gonadorelin may play a role in treating prostate cancer is a breakthrough that has allowed physicians to develop highly effective treatments. When prostate cancer develops, 99% of people can be completely cured. Experimental studies report Gonadorelin to exhibit minimal side effects and low oral and excellent subcutaneous bioavailability in mice.

References