GnRH-I
目录号 : GC34264
GnRH-I一种能够调节促性腺激素释放的神经肽，用于调控生殖系统的生理功能。
Sample solution is provided at 25 µL, 10mM.
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GnRH-I is a neuropeptide capable of regulating the release of gonadotropins, used to modulate the physiological functions of the reproductive system[1]. GnRH-I stimulates the anterior pituitary to release gonadotropins, thereby regulating the synthesis and secretion of gonadal hormones and maintaining reproductive endocrine balance[2]. GnRH-I can be used to study the regulatory mechanisms of the hypothalamic-pituitary-gonadal (HPG) axis and its role in reproductive-related diseases[3]. GnRH-I may also play a significant role in the growth of ovarian tumors[4].
In vitro, GnRH-I (3nM) stimulation of gonadotropin cells from neonatal rat pituitary for 3 hours significantly promotes the secretion of luteinizing hormone (LH) and follicle-stimulating hormone (FSH). This process depends on the activation of intracellular calcium signaling and cyclic nucleotide signaling pathways[5]. Treatment of human extravillous cytotrophoblasts (EVTs) with GnRH-I (0.1–100nM) for 24 hours significantly upregulates the mRNA and protein expression levels of urokinase-type plasminogen activator (uPA), while downregulating the expression of plasminogen activator inhibitor-1 (PAI-1). This enhances extracellular matrix degradation capacity, thereby promoting the invasive potential of trophoblast cells during early pregnancy[6].
In vivo, a single intravenous bolus of GnRH-I (0.01–10μg/kg body weight) administered to female rhesus monkeys aged 8–12 months and 21–23 months significantly promotes the release of plasma luteinizing hormone (LH), with younger individuals showing greater sensitivity[7].
References:
[1] Cheng CK, Leung PC. Molecular biology of gonadotropin-releasing hormone (GnRH)-I, GnRH-II, and their receptors in humans. Endocr Rev. 2005 Apr;26(2):283-306.
[2] Leung PC, Cheng CK, Zhu XM. Multi-factorial role of GnRH-I and GnRH-II in the human ovary. Mol Cell Endocrinol. 2003 Apr 28;202(1-2):145-53.
[3] Kern J, Schilling D, Schneeweis C, et al. Identification of the unfolded protein response pathway as target for radiosensitization in pancreatic cancer. Radiother Oncol. 2024 Feb;191:110059.
[4] Kang SK, Choi KC, Yang HS, et al. Potential role of gonadotrophin-releasing hormone (GnRH)-I and GnRH-II in the ovary and ovarian cancer. Endocr Relat Cancer. 2003 Jun;10(2):169-77.
[5] Balík A, Jindřichová M, Bhattacharyya S, et al. GnRH-I and GnRH-II-induced calcium signaling and hormone secretion in neonatal rat gonadotrophs. Physiol Res. 2009;58(5):709-716.
[6] Chou CS, Zhu H, Shalev E, et al. The effects of gonadotropin-releasing hormone (GnRH) I and GnRH II on the urokinase-type plasminogen activator/plasminogen activator inhibitor system in human extravillous cytotrophoblasts in vitro. J Clin Endocrinol Metab. 2002 Dec;87(12):5594-603.
[7] Densmore VS, Urbanski HF. Relative effect of gonadotropin-releasing hormone (GnRH)-I and GnRH-II on gonadotropin release. J Clin Endocrinol Metab. 2003 May;88(5):2126-34.
GnRH-I一种能够调节促性腺激素释放的神经肽，用于调控生殖系统的生理功能[1]。GnRH-I可以刺激垂体前叶释放促性腺激素，进而调节性腺激素的合成与分泌，维持生殖内分泌平衡[2]。GnRH-I可用于研究下丘脑-垂体-性腺轴的调控机制，以及其在生殖相关疾病中的作用[3]。GnRH-I还可能在卵巢肿瘤生长中发挥重要作用[4]。
在体外，GnRH-（3nM刺激新生大鼠垂体促性腺激素细胞3小时，显著促进促黄体生成素（LH）和促卵泡激素（FSH）的分泌，该过程依赖于激活了细胞内钙信号和环核苷酸信号通路[5]。GnRH-I（0.1–100nM）处理人绒毛外细胞滋养层细胞（EVTs）24小时，显著上调尿激酶型纤溶酶原激活物（uPA）的mRNA和蛋白表达水平，同时下调纤溶酶原激活物抑制剂-1（PAI-1）的表达，增强细胞外基质降解能力，从而促进滋养层细胞在妊娠早期的侵入潜能[6]。
在体内，GnRH-I（0.01–10μg/kg体重）单次静脉推注处理8–12月龄和21–23月龄雌性恒河猴，可显著促进血浆黄体生成素（LH）的释放，且年轻个体反应更敏感[7]。
| Cell experiment [1]: | |
Cell lines | Human extravillous cytotrophoblasts (EVTs) |
Preparation Method | EVTs were cultured in DMEM supplemented with 10% fetal bovine serum at 37°C, 5% CO₂. Cells were treated with GnRH-I at concentrations ranging from 0.1 to 100nM for 24 hours. |
Reaction Conditions | 0.1–100nM; 24h |
Applications | GnRH-I significantly increased urokinase-type plasminogen activator (uPA) mRNA and protein expression in a dose-dependent manner, with maximal effects observed at 100nM. Concurrently, GnRH-I reduced plasminogen activator inhibitor-1 (PAI-1) mRNA and protein levels, altering the uPA/PAI-1 ratio to promote trophoblast invasiveness. |
| Animal experiment [2]: | |
Animal models | Rhesus monkeys (Macaca mulatta) |
Preparation Method | Monkeys were intravenously administered a single bolus injection of GnRH-I at doses of 0.01, 0.1, 1, or 10μg/kg body weight during the midluteal phase. Blood samples were collected remotely via vascular catheters at -10, 0, 10, 20, 30, 60, and 120 minutes post-injection. |
Dosage form | 0.01–10μg/kg; i.v. |
Applications | GnRH-I significantly increased plasma luteinizing hormone (LH) concentrations in a dose-dependent manner, with peak responses observed within 10 minutes. The LH release was more pronounced in young animals compared to old monkeys, indicating age-related sensitivity differences. |
References: | |
| Cas No. | SDF | ||
| Canonical SMILES | Pyr-His-Trp-Ser-Tyr-Gly-Leu-Arg-Pro-Gly-NH2 | ||
| 分子式 | C50H75N17O13 | 分子量 | 1182.32 |
| 溶解度 | Water : 50 mg/mL (42.29 mM) | 储存条件 | -20°C, protect from light |
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| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 845.8 μL | 4.229 mL | 8.4579 mL |
| 5 mM | 169.2 μL | 845.8 μL | 1.6916 mL |
| 10 mM | 84.6 μL | 422.9 μL | 845.8 μL |
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| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
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| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
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2.
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