Cetrorelix is a synthetic gonadotropin-releasing hormone (GnRH) antagonist (IC50 = 1.21nM) [1]. Cetrorelix Acetate inhibits the GnRH signaling pathway, thereby reducing the secretion of follicle-stimulating hormone (FSH) and luteinizing hormone (LH) [2-3]. Cetrorelix Acetate is used to treat premature ovulation [4].
In epithelial cells, treatment with Cetrorelix Acetate (1-20ng/mL; 10d) significantly reduced cell growth rate [5]. In HTOA cells, Cetrorelix Acetate (10nM-10μM; 24-96h) treatment showed a dose-dependent anti-proliferative effect on cells [6].
In C57BL/6J mice, Cetrorelix Acetate (5µg/kg; ip; 7d) improves superovulation efficacy in aged mice without compromising oocyte quality [7]. In CFLP male mice, Cetrorelix Acetate (2µg; 2µL; intraventricular injection; single injection) attenuates the effects of beta-amyloid 25-35 [8].
References:
[1]. Beckers T, Reiländer H, Hilgard P. Characterization of gonadotropin-releasing hormone analogs based on a sensitive cellular luciferase reporter gene assay[J]. Analytical biochemistry, 1997, 251(1): 17-23.
[2]. Britten J L, Malik M, Levy G, et al. Gonadotropin-releasing hormone (GnRH) agonist leuprolide acetate and GnRH antagonist cetrorelix acetate directly inhibit leiomyoma extracellular matrix production[J]. Fertility and sterility, 2012, 98(5): 1299-1307.
[3]. Jiang J, Gao S, Xu J. Efficacy and safety of gonadotropin-releasing hormone (GnRH) agonists triptorelin acetate and cetrorelix acetate in assisted reproduction[J]. Medical Science Monitor: International Medical Journal of Experimental and Clinical Research, 2018, 24: 7996.
[4]. Steward R G, Gill I, Williams D B, et al. Cetrorelix lowers premature luteinization rate in gonadotropin ovulation induction–intrauterine insemination cycles: a randomized-controlled clinical trial[J]. Fertility and sterility, 2011, 95(1): 434-436.
[5]. Castellón E, Clementi M, Hitschfeld C, et al. Effect of leuprolide and cetrorelix on cell growth, apoptosis, and GnRH receptor expression in primary cell cultures from human prostate carcinoma[J]. Cancer investigation, 2006, 24(3): 261-268.
[6]. Tang X, Yano T, Osuga Y, et al. Cellular mechanisms of growth inhibition of human epithelial ovarian cancer cell line by LH-releasing hormone antagonist Cetrorelix[J]. The Journal of Clinical Endocrinology & Metabolism, 2002, 87(8): 3721-3727.
[7]. Kanda A, Nobukiyo A, Sotomaru Y. Effect of Cetrorelix administration on ovarian stimulation in aged mice[J]. Experimental Animals, 2021, 70(1): 31-36.
[8]. Telegdy G, Tanaka M, Schally A V. Effects of the LHRH antagonist Cetrorelix on the brain function in mice[J]. Neuropeptides, 2009, 43(3): 229-234.
Cetrorelix是一种合成的促性腺激素释放激素（GnRH）拮抗剂（IC50 = 1.21nM) [1]。Cetrorelix Acetate可抑制GnRH信号通路，从而减少促卵泡激素（FSH）和促黄体生成素（LH）的分泌 [2-3]。Cetrorelix Acetate用于治疗早产排卵 [4]。
在上皮细胞中，Cetrorelix Acetate（1-20ng/mL；10d）处理显著降低细胞生长率 [5]。在HTOA细胞中，Cetrorelix Acetate（10nM-10μM；24-96h）处理显示出剂量依赖性的抗细胞增殖作用 [6]。
在C57BL/6J小鼠中，Cetrorelix Acetate（5µg/kg；ip；7d）可提高老年小鼠的超排卵效果，且不影响卵母细胞质量 [7]。在CFLP雄性小鼠中，Cetrorelix Acetate（2µg；2µL；脑室内注射；单次注射）可减弱β-淀粉样蛋白25-35的作用 [8]。