Alarelin Acetate is a synthetic gonadotropin-releasing hormone (GnRH) agonist[1-2]. During the initial phase of administration, Alarelin Acetate stimulates the pituitary gland to release luteinizing hormone (LH) and follicle-stimulating hormone (FSH), and is utilized in research related to conditions such as endometriosis, uterine fibroids, and infertility caused by ovarian dysfunction[3-4].
In vitro, treatment of rat gastric parietal cells with Alarelin Acetate (1μM) for 24 hours, Alarelin Acetate inhibited gastric acid secretion by acting on GnRH receptors on parietal cells, and reduced gastric acid secretion by suppressing vagal nerve activity, with effects exhibiting time-dependent characteristics[5]. Treatment of rat gastric smooth muscle cells with Alarelin Acetate (1nM–10μM) for 24–48 hours, Alarelin Acetate significantly inhibited cell proliferation activity and DNA synthesis via GnRH receptors, arrested the cell cycle in the G1 phase and reduced the proportion of cells in the S phase[6].
In vivo, administration of Alarelin Acetate via a PLGA microsphere sustained-release system (35μg/kg or 200μg/kg) as a single intramuscular injection in Acipenser ruthenus(with sampling at 24, 48, and 72 hours), Alarelin Acetate effectively induced spermiation, prolonged semen collection duration, and enhanced sperm motility at the 35μg/kg dose[7]. In non-breeding season Assaf and Lacaune ewes, intramuscular injection of Alarelin Acetate (7.5μg) combined with progesterone (37.5mg) on day 0 of the experiment, Alarelin Acetate increased lambing rate, improved reproductive performance, and enhanced fertility[8].
References:
[1] Yuan F, Zhang P, Liu M, et al. Pharmacogenomic analysis of alarelin acetate-induced hepatotoxicity: a case report and literature review. Front Med (Lausanne). 2025 Sep 29;12:1634101.
[2] Chu L, Terasaki M, Mattsson CL, et al. In vivo drug discovery for increasing incretin-expressing cells identifies DYRK inhibitors that reinforce the enteroendocrine system. Cell Chem Biol. 2022 Sep 15;29(9):1368-1380.e5.
[3] Kong Y, Zhang JW. Experimental study on rat model of endometriosis treated with tamoxifen and rhizoma curcumae oil. Sichuan Da Xue Xue Bao Yi Xue Ban. 2006 Jul;37(4):596-8.
[4] Zhang K, Gao G, Zhao X, et al. The direct effects of gonadotropin-releasing hormone on proliferation of granulosa cells and development of follicles in goose. Br Poult Sci. 2020 Jun;61(3):242-250.
[5] Chen L, Sun XD, Zhao J, et al. Distribution, cloning and sequencing of GnRH, its receptor, and effects of gastric acid secretion of GnRH analogue in gastric parietal cells of rats. Life Sci. 2005 Feb 4;76(12):1351-65.
[6] Chen L, He HX, Sun XD, et al. Expression of gonadotropin-releasing hormone receptor and effect of gonadotropin-releasing hormone analogue on proliferation of cultured gastric smooth muscle cells of rats. World J Gastroenterol. 2004 Jun 15;10(12):1780-4.
[7] Podhorec P, Knowles J, Vysloužil J, et al. Induction of Spermiation in Sterlet Acipenser ruthenus by PLGA Microparticle Delivery with Sustained Alarelin Release. Animals (Basel). 2021 Nov 19;11(11):3305.
[8] Alijani A, Niasari-Naslaji A, Sayyah N, et al. Comparing CIDR with progesterone injections and eCG with human recombinant FSH for synchronizing estrous cycle in ewes. Iran J Vet Res. 2024;25(1):3-7.
Alarelin Acetate是一种合成的促性腺激素释放激素激动剂[1-2]。Alarelin Acetate在用药初期可刺激垂体释放促黄体生成素和促卵泡素，Alarelin Acetate可用于子宫内膜异位症、子宫肌瘤及卵巢功能异常引起的不孕症等相关研究[3-4]。
在体外，Alarelin Acetate（1μM）处理大鼠胃壁细胞24小时，Alarelin Acetate通过作用于壁细胞上的GnRH受体直接抑制胃酸分泌，并可能通过抑制迷走神经功能间接降低胃酸分泌，作用呈时间依赖性[5]。Alarelin Acetate（1nM-10μM）处理大鼠胃平滑肌细胞24-48小时，Alarelin Acetate通过GnRH受体显著抑制细胞增殖活力、DNA合成，同时将细胞周期阻滞在G1期并减少S期比例[6]。
在体内，Alarelin Acetate通过PLGA微球缓释系统（35μg/kg或200μg/kg）单次肌肉注射处理Acipenser ruthenus（于24、48和72小时采样），35μg/kg Alarelin Acetate可有效诱导Acipenser ruthenus排精，延长精液采集时间，并提高精子活力[7]。Alarelin Acetate（7.5μg）联合孕酮（37.5mg）在实验第0天肌肉注射处理非繁殖季节的Assaf和Lacaune母羊，Alarelin Acetate可增加母羊的产羔率、繁殖力和生育力[8]。