Triptorelin pamoate is a potent LHRH agonist. After a transient increase, continuous administration results in downregulation of LH and FSH levels followed by a suppression of ovarian and testicular steroid biosynthesis.
CAT No: 10-101-101
CAS No:57773-63-4 (net), 124508-66-3 (pamoate salt)
Synonyms/Alias:5-Oxo-L-prolyl-L-histidyl-L-tryptophyl-L-seryl-L-tyrosyl-D-tryptophyl-L-leucyl-L-arginyl-L-prolylglycine amide, 4,4'-methylenebis(3-hydroxy-2-naphthoate) (salt); Decapeptyl; Diphereline; Gonapeptyl; Luteinizing hormone-releasing factor (swine), 6-D-tryptophan-, 4,4'-methylenebis(3-hydroxy-2-naphthalenecarboxylate) (salt); Pamorelin; Trelstar; Trelstar depot; Trelstar LA; Triptorelin embonate; UNII-08AN7WA2G0
Triptorelin Pamoate is a synthetic decapeptide analog of gonadotropin-releasing hormone (GnRH), formulated as a pamoate salt to enable sustained-release properties in research settings. As a member of the peptide compound category, it exhibits high affinity for the GnRH receptor, making it a valuable tool for probing the regulation of the hypothalamic-pituitary-gonadal axis. Its capacity to modulate gonadotropin secretion through receptor agonism renders it particularly important in studies of endocrine function, reproductive biology, and neuroendocrine signaling. The pamoate formulation is specifically designed to facilitate extended release, which is advantageous for experimental protocols requiring prolonged peptide exposure.
Endocrine research: Triptorelin Pamoate is widely employed in laboratory investigations focused on elucidating the mechanisms of gonadotropin regulation and pituitary gland function. The decapeptide structure allows for precise receptor targeting, enabling researchers to simulate or suppress endogenous GnRH activity in a controlled manner. By modulating luteinizing hormone (LH) and follicle-stimulating hormone (FSH) release, it provides a robust model for studying hormonal feedback loops and the downstream effects on steroidogenesis, gametogenesis, and reproductive physiology.
Reproductive biology studies: The compound's ability to induce sustained GnRH receptor activation is particularly valuable in experimental models of reproductive axis suppression or stimulation. Investigators utilize the extended-release properties of the pamoate salt to maintain stable peptide concentrations over time, allowing for the assessment of long-term effects on gonadal function, sexual maturation, and fertility endpoints. This facilitates the exploration of molecular pathways underlying puberty, estrous cycling, and gonadal atrophy or hyperactivity under various experimental conditions.
Neuroendocrine signaling analysis: Researchers leverage Triptorelin Pamoate in studies examining the complex interplay between the central nervous system and peripheral endocrine organs. Its potent and sustained agonistic action enables detailed analysis of neuropeptide signaling cascades, receptor desensitization, and downstream gene expression changes in neuronal and pituitary tissues. Such investigations are critical for understanding the neurochemical regulation of reproductive and metabolic processes at both cellular and systemic levels.
Peptide drug delivery research: The pamoate formulation serves as an instructive model for the development and evaluation of long-acting peptide delivery systems. By studying the pharmacokinetic and pharmacodynamic profiles of this depot-formulated GnRH analog, scientists gain insights into the factors influencing peptide stability, release kinetics, and bioavailability. These findings inform the design of novel sustained-release strategies for other peptide-based research compounds, with applications in optimizing dosing regimens and minimizing experimental variability.
Peptide-receptor interaction studies: The high specificity of Triptorelin Pamoate for the GnRH receptor makes it an excellent probe for structure-activity relationship (SAR) analyses and receptor binding assays. Researchers utilize it to dissect the molecular determinants of ligand-receptor affinity, receptor activation, and intracellular signaling pathways. Such studies advance the understanding of peptide-receptor dynamics, providing a foundation for rational design of next-generation analogs and for mapping the functional domains critical to receptor engagement and signal transduction.
Gonadotropin-releasing hormone agonists are widely used as androgen deprivation therapy in many men with locally advanced or metastatic prostate cancer. Gonadotropin-releasing hormone agonists are delivered by intramuscular injection every 1, 3 or 6 months, but in some patients subcutaneous injection may be more appropriate. This study assessed the efficacy and safety profile of the gonadotropin-releasing hormone agonist, triptorelin pamoate, when administered by the subcutaneous route.
Lebret, T., Rouanne, M., Hublarov, O., Jinga, V., Petkova, L., Kotsev, R., ... & Dutailly, P. (2015). Efficacy of triptorelin pamoate 11.25 mg administered subcutaneously for achieving medical castration levels of testosterone in patients with locally advanced or metastatic prostate cancer. Therapeutic advances in urology, 7(3), 125-134.
To compare the efficacy of monthly administrations of the luteinizing hormone-releasing hormone agonists triptorelin pamoate and leuprolide acetate to induce and maintain castrate levels of serum testosterone in men with advanced prostate cancer. Triptorelin reduced testosterone concentrations less rapidly, but maintained castration as effectively as leuprolide. There was no evidence that the slower onset of castration caused deleterious effects.
Heyns, C. F., Simonin, M. P., Grosgurin, P., Schall, R., & Porchet, H. C. (2003). Comparative efficacy of triptorelin pamoate and leuprolide acetate in men with advanced prostate cancer. BJU international, 92(3), 226-231.
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