gonadotropin releasing hormone receptor

Relugolix (RVT-601) is an orally available, non-peptide gonadotropin-releasing hormone (GnRH or luteinizing hormone-releasing hormone (LHRH)) antagonist, with potential antineoplastic activity. Relugolix competitively binds to and blocks the GnRH receptor in the anterior pituitary gland, which both prevents GnRH binding to the GnRH receptor and inhibits the secretion and release of both luteinizing hormone (LH) and follicle stimulating hormone (FSH). In males, the inhibition of LH secretion prevents the release of testosterone from Leydig cells in the testes. Since testosterone is required to sustain prostate growth, reducing testosterone levels may inhibit hormone-dependent prostate cancer cell proliferation.

Abarelix (PPI 149) is a potent gonadotrophin-releasing hormone (GnRH) antagonist, which is used for prostate cancer treatment.

(R)-Elagolix (NBI-56418) is a short-acting, nonpeptide, GnRH antagonist with an IC50 and Ki of 0.25 and 3.7 nM, respectively. administered orally, that unlike injectable depot GnRH agonists and antagonists, produces a dose-dependent suppression of ovarian estrogen production, that is, from partial suppression at lower doses to full suppression at higher doses.

Linzagolix is a small-molecule, non-peptide, orally active gonadotropin-releasing hormone antagonist (GnRH antagonist) which is under development by Kissei Pharmaceutical and ObsEva for the treatment of uterine fibroids, endometriosis, and adenomyosis. As of December 2020, it is under review for approval for uterine fibroids, is in phase III clinical trials for endometriosis, and is in phase II clinical studies for adenomyosis.

Goserelin acetate (Fertilan) is a synthetic long-acting agonist of gonadotropin-releasing hormone, used in treatments of cancer.

Elagolix sodium (NBI-56418 sodium) is a GnRH receptor (GnRHR) antagonist ( IC50 and Ki of 0.25 and 3.7 nM, respectively).

Fertirelin, or fertirelin acetate, sold under the brand name Ovalyse, is a gonadotropin-releasing hormone agonist (GnRH agonist).

GnRH-I acetate in release of biologically active Follicle-Stimulating Hormone (FSH) and Luteinizing Hormone (LH) in the blood.

BAY-784 is a potent gonadotropin-releasing hormone receptor (GnRH-R) antagonist that exhibits strong inhibitory activity with IC50 values of 21 nM for human GnRH-R and 24 nM for rat GnRH-R, BAY-784 is widely applied in endocrine research to study GnRH signaling, reproductive hormone regulation, and therapeutic modulation of hormone-dependent physiological and pathological processes.

Opigolix, a Gonadotropin-releasing hormone receptor antagonist, treats hormone-dependent conditions by inhibiting the actions of gonadotropin-releasing hormone (GnRH).

BAY 1214784 is a selective and orally active human GnRH-R (Human Gonadotropin-Releasing Hormone Receptor) antagonist, which can effectively reduce plasma luteinizing hormone levels by up to 49% and can be used for the study of uterine fibroids.

Degarelix is a peptide and selective GnRH (human gonadotropin-releasing hormone) receptor antagonist that treats prostate cancer by lowering testosterone levels in the body.

Degarelix acetate is a competitive and reversible antagonist of gonadotropin-releasing hormone receptor (GnRHR) .

GnRH-R antagonist-2 (Compound 44c) is a gonadotropin-releasing hormone receptor (GnRH-R) antagonist, with IC50 values of 43 nM for rat and 88 nM for human GnRH-R. It is applicable in studies related to hormone-dependent diseases such as endometriosis, breast cancer, and prostate cancer^[1].

GnRH-R antagonist-3 (Compound 37) is a gonadotropin-releasing hormone receptor (GnRH-R) antagonist with IC50 values of 94 nM for rat GnRH-R and 275 nM for human GnRH-R. It is utilized in research related to hormone-dependent diseases, such as endometriosis, breast cancer, and prostate cancer^[1].

Elagolix is an orally active, highly effective, selective non-peptide antagonist of the gonadotropin-releasing hormone receptor (GnRH receptor) with a dissociation constant (KD) of 54 pM, as well as an NFAT inhibitor, and is utilized in researching endometriosis-related pain.

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).

Triptorelin ([DTrp6]-LH-RH) is an analog of gonadotropin-releasing hormone (GnRH) and a high-affinity GnRH receptor agonist that stimulates the secretion of luteinizing hormone (LH) and follicle-stimulating hormone (FSH).

Leuprorelin acetate (also known as leuprolide acetate) is a potent gonadotropin-releasing hormone (GnRH) agonist. It is widely used in hormone-sensitive conditions, including advanced prostate cancer, endometriosis, uterine fibroids, and central precocious puberty. Leuprorelin acetate is additionally applicable in endocrine research models for investigating GnRH receptor signaling dynamics, hypothalamic–pituitary axis regulation, and hormone-responsive cellular response systems in reproductive biology studies.

Cetrorelix Acetate is gonadotropin-releasing hormone (GnRH) receptor antagonist with an IC50 of 1.21 nM.

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......