Histrelin acetate 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: 10-101-21
CAS No:76712-82-8 (net)
Synonyms/Alias:Histrelin acetate;220810-26-4;Vantas;Supprelin;DTXSID30176580;Histrelin (acetate);MFCD00918679;Histrelin (acetate)?;SCHEMBL18715;CHEMBL1200509;AKOS040764197;FD110400;TS-10572;(Des-Gly10,D-His(Bzl)6,Pro-NHEt9)-LHRH Acetate;(Des-Gly10,D-His(Bzl)6,Pro-NHEt 9)-LHRH acetate;
Chemical Name:acetic acid;(2S)-N-[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2R)-3-(1-benzylimidazol-4-yl)-1-[[(2S)-1-[[(2S)-5-(diaminomethylideneamino)-1-[(2S)-2-(ethylcarbamoyl)pyrrolidin-1-yl]-1-oxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-1-oxopropan-2-yl]amino]-3-(4-hydroxyphenyl)-1-oxopropan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-3-(1H-indol-3-yl)-1-oxopropan-2-yl]amino]-3-(1H-imidazol-5-yl)-1-oxopropan-2-yl]-5-oxopyrrolidine-2-carboxamide
Histrelin Acetate is a synthetic nonapeptide analog of gonadotropin-releasing hormone (GnRH), engineered for enhanced stability and receptor affinity. As a potent GnRH agonist, it plays a significant role in modulating the secretion of luteinizing hormone (LH) and follicle-stimulating hormone (FSH) by acting on the anterior pituitary. Its structural modifications confer increased resistance to enzymatic degradation, making it highly valuable for studies requiring sustained receptor activation. The compound's unique biochemical profile has established it as an indispensable tool in neuroendocrine research, reproductive biology, and peptide signaling investigations.
Endocrine Regulation Research: Histrelin Acetate is widely employed in laboratory studies investigating the regulation of the hypothalamic-pituitary-gonadal (HPG) axis. By serving as a GnRH agonist, it enables researchers to control and modulate the release of gonadotropins in in vitro and in vivo models. This capability is particularly useful for dissecting the feedback mechanisms involved in hormone secretion, elucidating the dynamics of pituitary signaling, and advancing the understanding of endocrine homeostasis.
Reproductive Biology Studies: The compound is instrumental in exploring the physiological and molecular mechanisms underlying reproductive function. Its ability to induce downregulation of GnRH receptors through continuous stimulation provides a robust model for examining the suppression of gonadotropin release. Scientists utilize it to probe the regulation of gametogenesis, gonadal steroidogenesis, and the effects of altered hormonal environments on reproductive tissues, thereby deepening insights into fertility and developmental biology.
Peptide Receptor Pharmacology: Histrelin Acetate serves as a reference ligand in the characterization of GnRH receptor pharmacodynamics. Its high potency and specificity make it an ideal candidate for competitive binding assays, receptor desensitization studies, and signal transduction analyses. These applications are critical for the development of novel GnRH analogs, screening of receptor modulators, and mapping of downstream signaling pathways in neuroendocrine cells.
Peptide Synthesis and Analytical Method Development: Due to its well-defined structure and stability, Histrelin Acetate is utilized as a standard or control in peptide synthesis protocols and analytical method validation. Laboratories leverage its properties to optimize chromatographic separation techniques, refine mass spectrometry detection parameters, and calibrate quantitative assays for peptide-based compounds. Such applications are essential for ensuring accuracy and reproducibility in peptide research workflows.
Mechanistic Studies of Hormone-Dependent Pathways: The compound's ability to precisely modulate hormonal signaling cascades makes it a valuable probe for dissecting the molecular basis of hormone-dependent cellular processes. Researchers employ it to investigate gene expression changes, protein phosphorylation events, and cellular responses following GnRH receptor activation or suppression. This facilitates a detailed understanding of the intricate networks governing endocrine physiology and supports the development of new research models in systems biology.
The once-yearly histrelin implant maintained testosterone suppression for repeated treatment cycles and was generally well tolerated. The histrelin implant provides a clinically attractive option for long-term androgen deprivation therapy in patients with advanced prostate cancer seeking fewer office visits and repeated injections.
Shore, N., Cookson, M. S., & Gittelman, M. C. (2012). Long‐term efficacy and tolerability of once‐yearly histrelin acetate subcutaneous implant in patients with advanced prostate cancer. BJU international, 109(2), 226-232.
The LHRH agonist histrelin acetate is the only available sustained-release hydrogel implant for once-yearly administration. The once-yearly implant allows patients to receive fewer cycles of implanting and replanting to maintain continuous ADT therapy. The histrelin acetate implant is 3.5 cm long, is 3 mm in diameter, and is administered subcutaneously into the inner aspect of the upper arm or abdomen. The inner aspect of the upper arm can clinically be difficult for the surgeon as it is a mobile insertion site and difficult for elderly patients limited by strength/arthritis to maintain the necessary abducted and extended arm position. Thus, the arm compared to the abdomen site is more difficult for surgeon and is less tolerated by patients.
Woolen, S., Holzmeyer, C., Nesbitt, E., & Siami, P. F. (2014). Long-term efficacy and tolerability of abdominal once-yearly histrelin acetate subcutaneous implants in patients with advanced prostate cancer. Prostate cancer, 2014.
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