gonadotropin releasing hormone receptor

(R)-Elagolix (NBI-56418) 是口服具有活性的、选择性高的非肽类促性腺激素释放激素受体短期有效拮抗剂 (KD = 54 pM)。

Goserelin acetate (Fertilan) 是一种促性腺激素释放激素 (GnRH LHRH) 十肽类似物，能作为GnRH 激动剂。它可研究乳腺癌、上皮性卵巢癌和前列腺癌。

Elagolix sodium (NBI-56418 sodium) 是人GnRH 受体拮抗剂，其IC50=0.25 nM，Ki=3.7 nM。

Abarelix (PPI 149) 是一种促性腺激素释放激素 (GnRH) 拮抗剂，用于前列腺癌研究。

Linzagolix 是一种口服有活性的非多肽GnRH 拮抗剂。可用于研究子宫肌瘤、子宫腺肌症、子宫内膜异位症。

Relugolix (RVT-601) 是口服有活性的非肽性促性腺激素释放激素的拮抗剂。同 TAK-013 相比，它对人和猴子的受体具有高亲和力和强拮抗活性，它们的 IC50值分别为0.33 nM 和0.32 nM。它可用于研究性激素依赖性疾病，如子宫肌瘤、子宫内膜异位症、前列腺癌等。

Fertirelin 是 GnRH 和 LH-RH 的类似物，可用于研究牛滤泡囊肿。 它是促性腺激素释放激素激动剂。

BAY-784 is a gonadotropin-releasing hormone receptor (GnRH-R) antagonist (IC50s: 21 and 24 nM for human and rat GnRH-R).

Opigolix (ASP-1707)是一种可口服促性腺激素释放激素 (GnRH) 受体拮抗剂，可用于研究子宫内膜异位症相关疼痛、风湿性关节炎和子宫肌瘤。

Cetrorelix Acetate 是一种GnRH 受体的强效拮抗剂(IC50:1.21 nM)。

Degarelix是一种多肽和选择性的GnRH (人类促性腺激素释放激素) 受体拮抗剂，通过降低体内睾酮水平来治疗前列腺癌。

Degarelix acetate(214766-78-6 free base) 是促性腺激素释放激素受体 (GnRHR) 的竞争性可逆拮抗剂。

gonadotropin-releasing hormone (GnRH, LHRH) receptor antagonist,orally active

SKI2496 is a potent and orally bioavailableantagonist of Gonadotropin-Releasing Hormone Receptor (hGnRHR IC50 = 0.46 nM; max. LH inh. inh. (%, h)= 84%, 12h; LH inh. (24h) = 76%.). SKI2496 exhibits more selective antagonistic activity toward the human GnRH

Kisspeptin-54 is a peptide ligand of the orphan G protein-coupled receptor GPR54 (Kis = 1.81 and 1.45 nM for rat and human receptors, respectively).1 It is a 54 amino acid peptide encoded by the metastasis suppressor gene KISS-1. Kisspeptin-54 induces calcium mobilization in CHO-K1 cells expressing rat and human receptors (EC50s = 1.39 and 5.47 nM, respectively). It also induces arachidonic acid release in CHO cells expressing rat and human GPR54 in a concentration-dependent manner. Kisspeptin-54 (10-1,000 nM) inhibits insulin secretion from isolated mouse pancreatic β-cells in the presence of 2.8 mM, but not 11.1 mM, glucose.2 Kisspeptin-54 (1-5 nmol, i.c.v.) increases serum levels of luteinizing hormone (LH) and follicular stimulating hormone (FSH) in mice, an effect which is reversed by the gonadotropin releasing hormone (GNRH) antagonist acycline.3References1. Kotani, M., Detheux, M., Vandenbogaerde, A.L., et al. The metastasis suppressor gene KiSS-1 encodes kisspeptins, the natural ligands of the orphan G protein-coupled receptor GPR54. J. Biol. Chem. 276(37), 34631-34636 (2001).2. Vikman, J., and Ahrén, B. Inhibitory effect of kisspeptins on insulin secretion from isolated mouse islets. Diabetes Obes. Metab. 11(Suppl 4), 197-201 (2009).3. Gottsch, M.L., Cunningham, M.J., Smith, J.T., et al. A role for kisspeptins in the regulation of gonadotropin secretion in the mouse. Endocrinology 145(9), 4073-4077 (2004). Kisspeptin-54 is a peptide ligand of the orphan G protein-coupled receptor GPR54 (Kis = 1.81 and 1.45 nM for rat and human receptors, respectively).1 It is a 54 amino acid peptide encoded by the metastasis suppressor gene KISS-1. Kisspeptin-54 induces calcium mobilization in CHO-K1 cells expressing rat and human receptors (EC50s = 1.39 and 5.47 nM, respectively). It also induces arachidonic acid release in CHO cells expressing rat and human GPR54 in a concentration-dependent manner. Kisspeptin-54 (10-1,000 nM) inhibits insulin secretion from isolated mouse pancreatic β-cells in the presence of 2.8 mM, but not 11.1 mM, glucose.2 Kisspeptin-54 (1-5 nmol, i.c.v.) increases serum levels of luteinizing hormone (LH) and follicular stimulating hormone (FSH) in mice, an effect which is reversed by the gonadotropin releasing hormone (GNRH) antagonist acycline.3 References1. Kotani, M., Detheux, M., Vandenbogaerde, A.L., et al. The metastasis suppressor gene KiSS-1 encodes kisspeptins, the natural ligands of the orphan G protein-coupled receptor GPR54. J. Biol. Chem. 276(37), 34631-34636 (2001).2. Vikman, J., and Ahrén, B. Inhibitory effect of kisspeptins on insulin secretion from isolated mouse islets. Diabetes Obes. Metab. 11(Suppl 4), 197-201 (2009).3. Gottsch, M.L., Cunningham, M.J., Smith, J.T., et al. A role for kisspeptins in the regulation of gonadotropin secretion in the mouse. Endocrinology 145(9), 4073-4077 (2004).

Abarelix acetate is a synthetic third generation gonadotropin-releasing hormone receptor (GnRHR) antagonist. It increases histamine release from rat peritoneal mast cells in vitro and from a human skin model ex vivo. In vivo, abarelix decreases plasma luteinizing hormone (LH) levels six hours post-treatment in castrated rats, with levels returning to baseline within 24 hours.3 Abarelix (2 mg kg) also transiently decreases plasma testosterone levels in intact rats, with levels returning to baseline within seven days post-treatment. Formulations containing abarelix have previously been used in the treatment of advanced prostate cancer.

Dicetrorelix pamoate is a synthetic decapeptide with gonadotropin-releasing hormone (GnRH) antagonistic activity. GnRH induces the production and release of luteinizing hormone (LH) and follicle stimulating hormone (FSH) from the gonadotrophic cells of the anterior pituitary. Due to a positive estradiol (E2) feedback at midcycle, GnRH liberation is enhanced resulting in an LH-surge. This LH-surge induces the ovulation of the dominant follicle, resumption of oocyte meiosis and subsequently luteinization as indicated by rising progesterone levels. Cetrorelix competes with natural GnRH for binding to membrane receptors on pituitary cells and thus controls the release of LH and FSH in a dose-dependent manner. Cetrorelix binds to the gonadotropin releasing hormone receptor and acts as a potent inhibitor of gonadotropin secretion. It competes with natural GnRH for binding to membrane receptors on pituitary cells and thus controls the release of LH and FSH in a dose-dependent manner......

Zoptarelin doxorubicin, also known as AEZS-108, is an LHRH agonist. Zoptarelin doxorubicin is a peptide agonist of the gonadotropin releasing hormone-1 receptor (GnRH-1R) that is conjugated to the anthracycline antibiotic doxorubicin with potential antineoplastic activity. Zoptarelin doxorubicin binds to GnRH-1Rs, which may be highly expressed on endometrial and ovarian tumor cell membrane surfaces, and is internalized. Once inside the cell, the doxorubicin moiety of this agent intercalates into DNA and inhibits the topoisomerase II activity, which may result in the inhibition of tumor cell DNA replication and tumor cell proliferation

BAY 1214784是一种针对人促性腺激素释放激素受体(hGnRH-R)的高效、选择性口服活性拮抗剂，属于螺二氢吲哚衍生物化合物。该化合物能显著降低血浆促黄体激素水平，最高可达49%，同时显示出较低的药代动力学变异性和良好的耐受性，表现出研究子宫肌瘤的潜力。

[D-Glp1,D-Phe2,D-Trp3,6]-LH-RH 是一种黄体激素释放激素 (LHRH) 类似物，可作为 GnRH 受体拮抗剂。

[D-Ala6]-LH-RH，一种黄体激素释放激素(LHRH)模拟物，充当GnRH受体的激动剂。

[MePhe7]-Neurokinin B为NK-3受体(NK3R)激动剂，具有3 nM的IC50值。通过激活神经激肽3受体，[MePhe7]-Neurokinin B能够调节脉冲促性腺激素释放激素(GnRH)的分泌，成为调控该过程的潜在调节剂。

Phoenixin-14 (PNX-14) TFA 是具抗焦虑、心脏保护及神经保护效果的穿透大脑屏障神经肽。它通过上调GnRH受体mRNA调控垂体促性腺激素分泌，并促进胰岛素释放。此外，Phoenixin-14 TFA保护小鼠免受缺血 再灌注(IR)伤害，通过降低ROS、提高GSH减缓氧化应激。

DCOIT是一种典型的异噻唑啉酮，能激活促性腺激素释放激素受体(GnRHR)在大脑中引发卵泡刺激素和黄体生成素的合成。此外，DCOIT干扰了G蛋白偶联受体、MAPK和Ca2+信号传递途径。