gonadotropin-releasing

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。

(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)。

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

Human follicular gonadotropin releasing peptide (hF-GRP)是一种刺激垂体分泌促黄体激素(LH)及促卵泡激素(FSH)的激素类多肽，其作用可在体外实现。

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。

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。

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。

Histrelin (Supprelin LA) 是促性腺激素释放激素 (GnRH) 的九肽类似物，具有增加的效力。它被认为是 GnRH 激动剂。 Histrelin 用于治疗对激素敏感的男性前列腺癌和女性子宫肌瘤。

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

Linzagolix choline 是一种可口服的非肽类的促性腺激素释放激素（GnRH）拮抗剂。可用于研究子宫肌瘤和子宫内膜异位症相关疼痛。

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。

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

Folligen is a novel gonadotropin-releasing hormone analog against DMBA-induced tumours in the rat.

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).

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。

17α,20β-Dihydroxy-4-pregnen-3-one (17α,20β-DHP) is an endogenous, maturation-inducing steroid that stimulates oocyte maturation in females of several teleost species. For example, 1 μg ml of 17α,20β-DHP applied to Persian sturgeon oocytes has been shown to effectively induce germinal vesicle breakdown, an essential step during oocyte maturation.1 Gonadotropin-releasing hormone and the gonadotropins, follicle-stimulating hormone and luteinizing hormone, have been shown to stimulate the production of 17α,20β-DHP either in vivo or in vitro.[2] 17α,20β-DHP has also been reported to influence spermiation by stimulating milt production when administered at 5 mg kg to various male teleosts.[1]

Goserelin acetate（醋酸戈舍瑞林）是一种天然的十肽，是一种GnRH（gonadotropin releasing hormone）激动剂，能够减少性激素（睾酮和雌激素）的产生从而用于治疗前列腺癌、乳腺癌和子宫内膜异位症。

Cetrorelix diacetate (NS-75A) 是GnRH 受体的强效拮抗剂(IC50:1.21 nM)。

Nafarelin is a gonadotropin-releasing hormone agonist (GnRH agonist) which acts as an analog of GnRH. Nafarelin increases the release of FSH and LH by the anterior pituitary, which in turn leads to an increase of estrogen progesterone. When administered, Nafarelin has the purpose of causing increase estrogen that will negatively feed back upon hypothalamus to decrease GnRH ( negative feedback loop ) Through negative feedback, Nafarelin causes a decrease in pituitary secretion of gonadotropins luteinizing hormone (LH) and follicle stimulating hormone (FSH). Nafarelin may be used in the treatment of estrogen-dependent conditions (such as endometriosis or uterine fibroids), to treat central precocious puberty, and to control ovarian stimulation in IVF. It is normally delivered via a nasal spray. Nafarelin acetate is marketed by Searle (now part of Pfizer) under the brand name Synarel.

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.

Fertirelin acetate is a gonadotropin-releasing hormone (GnRH) agonist.