Best Gonadorelin Acetate 5mg and 10mg Peptides GMP Factory

Gonadorelin Acetate

Gonadorelin Acetate

Other names:Gonadorelin, gonadotropin-releasing hormone (GnRH), Kryptocur, LHRH Ferring, Lutamin, Lutrelef, Lutrepulse, Relisorm L, and Relisorm

Gonadorelin Acetate is a synthetic form of the hormone gonadotropin-releasing hormone (GnRH). GnRH is naturally produced in the hypothalamus of the brain and plays a crucial role in regulating the release of luteinizing hormone (LH) and follicle-stimulating hormone (FSH) from the pituitary gland. LH and FSH are essential for proper sexual development, fertility, and hormone regulation in both males and females.

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Referenced Citations

[1]Bain J, Moskowitz JP, Clapp JJ. “LH and FSH response to gonadotropin releasing  hormone (GnRH) in normospermic, oligospermic and azoospermic men”. Arch. Androl. 1978 May 10;1(2): 147–52. doi:10.3109/01485017808988331. PMID 367302

[2]Shao WM, Bai WJ, Chen YM, Liu L, Wang YJ. “[Micropump infusion of gonadorelin in the treatment of hypogonadotropic hypogonadism in patients with pituitary stalk interruption syndrome: cases analysis and literature review]”. Beijing da Xue Xue Bao (in Chinese). 2014 Jan 12;46(4): 642–5. PMID 25131486

[3]Sweetman, Sean C., ed.. Sex hormones and their modulators. Martindale: The Complete Drug Reference (36th ed.). London: Pharmaceutical Press. 2009 Aug 21;pp. 2106–2108. ISBN 978-0-85369-840-1

[4]Louis Sanford Goodman; Alfred Goodman Gilman. Goodman & Gilman’s the Pharmacological Basis of Therapeutics. McGraw-Hill, Health Professions Division. 1996 Jan 8;p. 1379. ISBN 978-0-07-026266-9

[5]Gautam N Allahbadia; Monika Malhotra Chawla; Rita Basuray Das; Esther Velilla Garcia, Goral Gandhi, Rubina Merchant. The Art & Science of Assisted Reproductive Techniques (ART). JP Medical Ltd. 2017 Jul 17;pp. 731–. ISBN 978-93-86322-82-1

[6]Lu ZL, Gallagher R, Sellar R, Coetsee M, Millar RP: Mutations remote from the human gonadotropin-releasing hormone (GnRH) receptor-binding sites specifically increase binding affinity for GnRH II but not GnRH I: evidence for ligand-selective, receptor-active conformations. J Biol Chem. 2005 Aug 19;280(33):29796-803

[7]Moles G, Carrillo M, Mananos E, Mylonas CC, Zanuy S: Temporal profile of brain and pituitary GnRHs, GnRH-R and gonadotropin mRNA expression and content during early development in European sea bass (Dicentrarchus labrax L.). Gen Comp Endocrinol. 2007 Jan 1;150(1):75-86

[8]Mamputha S, Lu ZL, Roeske RW, Millar RP, Katz AA, Flanagan CA: Conserved amino acid residues that are important for ligand binding in the type I gonadotropin-releasing hormone (GnRH) receptor are required for high potency of GnRH II at the type II GnRH receptor. Mol Endocrinol. 2007 Jan;21(1):281-92

[9] Lee PA, Houk CP: Gonadotropin-releasing hormone analog therapy for central precocious puberty and other childhood disorders affecting growth and puberty. Treat Endocrinol. 2006;5(5):287-96

[10]Bliss SP, Navratil AM, Breed M, Skinner DC, Clay CM, Roberson MS: Signaling complexes associated with the type I gonadotropin-releasing hormone (GnRH) receptor: colocalization of extracellularly regulated kinase 2 and GnRH receptor within membrane rafts. Mol Endocrinol. 2007 Feb;21(2):538-49

[11]Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5

[12] Sá Filho MF, Ayres H, Ferreira RM, Marques MO, Reis EL, Silva RC, Rodrigues CA, Madureira EH, Bó GA, Baruselli PS. Theriogenology. 2010 Mar 15;73(5):651-8. doi: 10.1016/j.theriogenology.2009.11.004. Epub 2010 Jan 18.PMID: 20080296

[13] Bergfeld EG, D’Occhio MJ, Kinder JE. Biol Reprod. 1996 Apr;54(4):769-75. doi: 10.1095/biolreprod54.4.769. PMID: 8924495

[14] Hall JB, Staigmiller RB, Short RE, Bellows RA, MacNeil MD, Bellows SE.J Anim Sci. 1997 Jun;75(6):1606-11. doi: 10.2527/1997.7561606x. PMID: 9250524

What Is Gonadorelin?

Gonadorelin, also known as GnRH, is a decapeptide gonadotropin-releasing hormone agonist. It functions by stimulating the synthesis and release of luteinizing hormone and follicle-stimulating hormone. In human medicine, it is utilized to address infertility, menstrual cycle irregularities, and hypogonadism. Additionally, it serves as a diagnostic tool for evaluating pituitary function. Ongoing research has uncovered potential applications of gonadorelin in the treatment of breast and prostate cancer, as well as Alzheimer’s disease. [4][5][6][7]

Gonadorelin Structure

gonadorelin structure

Authoritative source:PubChem

Sequence: Pyr-His-Trp-Ser-Tyr-Gly-Leu-Arg-Pro-Gly
Molecular Formula: C55H75N17013
Molecular Weight: 1182.311 g/mol
PubChem CID: 638793
CAS Number: 9034-40-6
Synonyms: Growth Hormone Releasing Factor, Somatocrinin, Somatoliberin

Gonadorelin Effects

Gonadorelin Research and Breast Cancer Prevention

Research indicates that women with greater lifetime exposure to estrogen may have an increased likelihood of developing breast cancer. Factors such as early onset of menstruation, later onset of menopause, use of estrogen-containing birth control, and menopausal hormone replacement therapy are associated with a higher risk of breast cancer. However, it is worth noting that the risk diminishes once birth control pills are discontinued, and eventually returns to the baseline level. It is important to recognize that while the use of birth control increases the risk of breast cancer, it simultaneously decreases the risk of ovarian cancer, making it a double-edged sword in terms of cancer risks.[3][4][5]

The growth of certain breast cancer cells relies on estrogen, and for years, reducing estrogen production or blocking estrogen receptors has been a recognized approach in treating specific types of breast cancer. Recent studies on gonadorelin have demonstrated its ability to suppress ovarian estrogen production, presenting a potential method for breast cancer prevention. This concept revolves around the notion that certain women, influenced by genetic and environmental factors, face a higher risk of developing breast cancer during their postmenopausal years. Utilizing gonadorelin in this context has proven to be safe and cost-effective, making it an appealing strategy for reducing the burden of cancer. Research suggests that a 10-year use of gonadorelin could potentially reduce the risk of breast cancer by up to 50%, and extending its use to 15 years may lead to a risk reduction of 70%.

The benefits of gonadorelin extend beyond breast cancer prevention. Research indicates that adjuvant therapy with anti-estrogens can significantly reduce disease progression, up to 50%, in cases where the cancer is sensitive to estrogen. However, currently available treatments face limitations in their effectiveness due to the development of resistance by cancer cells over time. This resistance often occurs due to increased expression of estrogen receptors, making it challenging to block every estrogen receptor without causing severe side effects. Gonadorelin offers a potential solution by reducing estrogen expression from the onset. This approach would not only directly inhibit the growth of estrogen-sensitive cancer cells but also enhance the efficacy of receptor-blocking medications, thereby extending their therapeutic effectiveness.

Gonadorelin a Breakthrough in Prostate Cancer

Contrary to popular media portrayal, prostate cancer is highly responsive to hormonal changes. While this might appear concerning, it actually presents an opportunity for intervention. By disrupting the supply of testosterone and its derivatives to prostate cancer cells, it is possible to significantly slow down and even stop the growth of the cancer. The main challenge lies in completely blocking all hormonal activity.[4][5][7] Initially, surgical removal of the testicles was performed in men with aggressive prostate cancer. However, this procedure was swiftly replaced by the administration of gonadorelin, which was found to be equally effective and potentially reversible in its action.

The use of GnRH in men with prostate cancer dates back to 1979, when it was initially referred to as “medical castration.” However, this mode of treatment led to an interesting discovery—that certain androgens are produced locally in the prostate through a process known as intracrinology. This means that GnRH blockade alone is only partially effective in treating prostate cancer. With the aid of gonadorelin, scientists were able to develop two new drugs that have been approved by the FDA for the treatment of castration-resistant prostate cancer (CRPC). These drugs play a crucial role in combating the progression and metastasis of prostate cancer, and they may even have potential as preventive measures in older men.

gonadorelin chart

The impact of gonadorelin and GnRH analogues on testosterone levels

Authoritative source:PubChem

Gonadorelin May Reduce Dementia Risk

Research suggests that sex hormones, specifically luteinizing hormone (LH), have effects on the brain that go beyond their role in sexual dimorphism or reproductive function. Interestingly, the rise in LH levels during menopause has been linked to a higher risk of Alzheimer’s disease and reduced memory performance in both humans and animals. In-depth studies conducted on rats have shown that LH directly influences the hippocampus, the brain’s key memory center. Rats administered with LH demonstrate impaired memory performance and dysfunction in the hippocampus, which can be reversed by the administration of an LH-blocking drug.

Subsequent investigations into LH have provided additional insights, demonstrating a correlation between elevated hormone levels and increased neuropathology.[1][5][7] Specifically, it has been observed that LH plays a role in the formation of plaques associated with Alzheimer’s disease. Therefore, it is logical to assume that lowering LH levels could potentially slow the progression of Alzheimer’s. This hypothesis has been partially supported by studies using mouse models, where the removal of LH receptors in the brain has shown improvements in amyloid pathology and the preservation of cell health, including astrocytes that provide support and protection to neurons.

Recent findings have revealed that testosterone plays a beneficial role in brain health and the preservation of cognitive function. Consequently, solely inhibiting the entire hypothalamic-pituitary-gonadal axis may not be an effective approach for treating Alzheimer’s disease. As a result, scientists have embarked on testing gonadorelin derivatives to determine if selective interference in LH production is feasible and can yield potential benefits.

Ongoing research has shed light on the effectiveness of leuprolide, a GnRH receptor agonist commonly used to treat uterine fibroids, in reducing the risk of Alzheimer’s compared to other gonadorelin analogues. While the specific reasons behind this discrepancy are still being investigated, it is crucial to note that men undergoing highly effective combined androgen blockade (CAB) treatment for prostate cancer need not face a trade-off between cancer control and Alzheimer’s disease. In this context, leuprolide can be employed to mitigate the risks associated with CAB treatment and Alzheimer’s disease.[1][2][3][7] Particularly, the ability of leuprolide to down-regulate serum gonadotropin levels, including LH, is generally sufficient to counteract the effects of reduced testosterone.

New studies are underway to investigate the impact of gonadorelin and its analogues on APOE and MS4A6A expression in Alzheimer’s disease. Both of these genetic loci are associated with late-onset Alzheimer’s disease. However, research indicates that they need to function in conjunction to manifest significant problems, and disrupting either gene locus alone is sufficient to disrupt the pathological pathway. Gonadorelin affects this process of tandem interaction, although the specific mechanisms and underlying reasons remain unclear. Presently, researchers are diligently working to comprehend how the interplay of genes in Alzheimer’s disease can be disrupted for both treatment and prevention purposes. Gonadorelin plays a pivotal role in this line of research, and its exploration holds great importance.

Gonadorelin Research

Gonadorelin is not a recent discovery in the field of human and mammalian disease treatment. However, researchers continually uncover new insights into the mechanisms of action of GnRH and GnRH analogues in both normal physiology and disease development. The breakthrough revelation that gonadorelin can be used in the treatment of prostate cancer has led to the development of an incredibly effective cure, with a success rate of up to 99% for early-stage prostate cancer patients. Excitingly, similar breakthroughs appear to be on the horizon regarding the involvement of gonadorelin and its downstream hormones in the pathways associated with Alzheimer’s disease risk.

It is worth noting that gonadorelin demonstrates minimal side effects and exhibits excellent subcutaneous bioavailability in mice, although the dosage per kilogram in mice cannot be directly scaled to humans. It is important to emphasize that the sale of gonadorelin at Peptide Sciences is strictly limited to educational and scientific research purposes and is not intended for human consumption. Individuals should only purchase gonadorelin if they are licensed researchers.

Referenced Citations

[1] G. Secreto et al., “A novel approach to breast cancer prevention: reducing excessive ovarian androgen production in elderly women,” Breast Cancer Res. Treat., vol. 158, no. 3, pp. 553–561, 2016.

[2] D. V. Spicer and M. C. Pike, “Sex steroids and breast cancer prevention,” J. Natl. Cancer Inst. Monogr., no. 16, pp. 139–147, 1994.

[3] G. Secreto, P. Muti, M. Sant, E. Meneghini, and V. Krogh, “Medical ovariectomy in menopausal breast cancer patients with high testosterone levels: a further step toward tailored therapy,” Endocr. Relat. Cancer, vol. 24, no. 11, pp. C21–C29, 2017.

[4] E. S. Vollaard, A. P. van Beek, F. A. J. Verburg, A. Roos, and J. A. Land, “Gonadotropin-releasing hormone agonist treatment in postmenopausal women with hyperandrogenism of ovarian origin,” J. Clin. Endocrinol. Metab., vol. 96, no. 5, pp. 1197–1201, May 2011.

[5] F. Labrie, “Hormonal therapy of prostate cancer,” Prog. Brain Res., vol. 182, pp. 321–341, 2010.

[6] F. Labrie, “ M.GnRH agonists and the rapidly increasing use of combined androgen blockade in prostate cancer,” Endocr. Relat. Cancer, vol. 21, no. 4, pp. R301-317, Aug. 2014.

[7] F. Labrie, “Combined blockade of testicular and locally made androgens in prostate cancer: a highly significant medical progress based upon intracrinology,” J. Steroid Biochem. Mol. Biol., vol. 145, pp. 144–156, Jan. 2015.

Author of this article:

Dr. Jean Zeng graduated from king’s college london Faculty of Life Sciences & Medicine.

scientific journal paper author:

  1. Francesca Torrini

Department of Chemistry ‘Ugo Schiff’, University of Florence, 50019 Sesto Fiorentino, FI, Italy

  1. M. Hashem

Department of Animal and Fish Production, Faculty of Agriculture (El-Shatby), Alexandria University, Alexandria 21545, Egypt

  1. Mark G. Papich DVM, MS, DACVCP

Professor of Clinical Pharmacology, Burroughs Wellcome Fund Professorship in Veterinary Pharmacology, College of Veterinary Medicine, North Carolina State University, Raleigh, North Carolina

  1. Jurandir Joaquim Bernardes Júnior

Laboratório de Biologia e Cultivo de Peixes de Água Doce (LAPAD), Departamento de Aquicultura, Centro de Ciências Agrárias, Universidade Federal de Santa Catarina, Rodovia SC 406, 3532, Florianópolis, Santa Catarina, CEP 88066-000, Brazil

  1. Picard-Hagen

Université de Toulouse, Institut National Polytechnique de Toulouse, École Nationale Vétérinaire de Toulouse, Toulouse, France 

Institute of Biochemistry/Center for Preventive Doping Research, German Sport University Cologne, Am Sportpark Müngersdorf, 50933 Cologne, Germany

Author of this article:

Dr. Jean Zeng graduated from king's college london Faculty of Life Sciences & Medicine.

Scientific Journal paper Author:

Stephen C. Bain
Diabetes Research Group, Swansea University Medical School, Swansea, SA2 8PP, UK
Department of Diabetes and Endocrinology, Singleton Hospital, Swansea Bay University Health Board, Swansea, SA2 8QA, UK

In no way does this doctor/scientist endorse or advocate the purchase, sale, or use of this product for any reason. Polypeptide.ltd has no affiliation or relationship, implied or otherwise, with this physician. The purpose of citing this doctor is to acknowledge, acknowledge and commend the exhaustive research and development work done by the scientists working on this peptide.