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TRIPTORELIN PEPTIDE

Triptorelin inhibits the release of estrogen and causes a profound hypogonadism “chemical castration” in animal test subjects. It is used predominantly as an androgen deprivation therapy of advanced prostate cancer. Its research shows that it could be used to treat benign conditions responsive to hormonal inhibition such as endometriosis, uterine fibroids, precocious puberty, and infertility. However in lower dosed administrations GnRH or triptorelin has been shown to have the reverse effect on the HPTA and actually work to jump start FSH and LH.

If you are looking for where to buy triptorelin for your research, we have it stocked at Loti Labs. This peptide is of the highest purity and we can guarantee a 100% satisfaction or your money back.

WHAT IS TRIPTORELIN?

Triptorelin is also known as 6-­D­-Tryptophan. It is a synthetic agonist analog of the naturally occurring Gonadotropin-releasing hormone produced in the hypothalamus. It acts on the Gonadotropin-releasing hormone receptors in the pituitary gland stimulating the release of Luteinizing hormone (LH) and Follicular stimulating hormone (FSH) stimulating the production and release of testosterone by the male testes and estrogen by the female ovaries and placenta. It is a decapeptide containing the amino acids in the sequence H-Pyr-His-Trp-Ser-Tyr-D-Trp-Leu-Arg-Pro-Gly-NH2. It is a more potent form of GnRH.

Animal studies comparing triptorelin to native GnRH found that triptorelin had 13 fold higher releasing activity for luteinizing hormone, and 21-fold higher releasing activity for follicle-stimulating hormone.

STRUCTURE OF TRIPTORELIN

Sequence: H-Pyr-His-Trp-Ser-Tyr-D-Trp-Leu-Arg-Pro-Gly-NH2

Molecular Formula: C₆₄H₈₂N₁₈O₁₃

Molecular weight: 1311.4 g/mol

CAS number: 57773-63-4

MECHANISM OF ACTION

Triptorelin has a strong affinity for Gonadotropin-Releasing Hormone Receptor than native GnRH. When it binds to the receptors on gonadotropes following intravenous administration, it causes gonadotropin release (flare-up effect). After several days, this is followed by a dramatic drop in the circulating concentrations of FSH and LH, through a desensitization mechanism, which results in a decline in testosterone and estrogen production.

The metabolism of triptorelin is not well understood; however, metabolism likely does not involve hepatic enzymes such as cytochrome P450. Triptorelin has no identified metabolites. It is eliminated through the kidneys and the liver and has a strong resistance to enzymatic breakdown and a prolonged half-life of 3 hours compared to native GnRH of about 2 to 4 minutes.

TRIPTORELIN USES

Circulating levels of testosterone in men and estrogen in women regulate the synthesis of GnRH is typically produced in a pulsatile manner. Triptorelin infusions produce a transient increase in sex hormones, but with continued non-pulsatile stimulation, LH and FSH synthesis are inhibited causing a decline in estrogen and testosterone levels. Triptorelin’s benefits and side effects are due to this phenomenon. Below are its uses:

• Palliation of prostate cancer
• Chemical castration
• Improving endometriosis
• Breast cancer management
• Improving precocious puberty in male rats

TRIPTORELIN SIDE EFFECTS

Along with its benefits, triptorelin may cause some unwanted effects typical of androgen deprivation in animal test studies. They include:

• Hot flushes
• Skeletal pains
• Impotence
• Headaches
• Fatigue
• Hypertension
• Diarrhea and vomiting
• Insomnia
• Urinary retention and urinary tract infections
• Anemia
• Embryo-fetal toxicity

LOOKING FOR WHERE TO BUY PEPTIDES

You can purchase triptorelin from Loti Labs. Buy peptides which are USA-made for the integrity of your research. It is tested through HPLC and Mass spectrometry to ensure quality. Triptorelin is commonly sold in 100mcg vials and is available in lyophilized powder form.

References

1. National Center for Biotechnology Information. PubChem Database. Triptorelin, CID=25074470, https://pubchem.ncbi.nlm.nih.gov/compound/Triptorelin (accessed on Dec. 20, 2019)

1. LiverTox: Clinical and Research Information on Drug-Induced Liver Injury [Internet]. Bethesda (MD): the National Institute of Diabetes and Digestive and Kidney Diseases; 2012-. Triptorelin. [Updated 2018 Mar 22]. Available from: https://www.ncbi.nlm.nih.gov/books/NBK548756/

1. Merseburger, A.S. & Hupe, M.C. Adv Ther (2016) 33: 1072. https://doi.org/10.1007/s12325-016-0351-4

1. Leschek EW, Flor AC, Bryant JC, Jones JV, Barnes KM, Cutler GB Jr. Effect of Antiandrogen, Aromatase Inhibitor, and Gonadotropin-releasing Hormone Analog on Adult Height in Familial Male Precocious Puberty. J Pediatr. 2017;190:229–235. doi:10.1016/j.jpeds.2017.07.047