gnrhr

(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.

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

Buserelin Acetate (57982-77-1 free base) (Buserelin Acetate) is an agonist of gonadotropin-releasing hormone receptor(GnRHR).

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

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

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

Linzagolix choline is an orally available non-peptide gonadotropin-releasing hormone (GnRH) antagonist. It can be used to study pain associated with uterine fibroids and endometriosis.

Deslorelin acetate(57773-65-6 free base) is a gonadotropin releasing hormone super-agonist (GnRH agonist)

Cetrorelix diacetate (NS-75A) is is a gonadotropin-releasing hormone antagonist. It works by blocking the action of GnRH upon the pituitary, thus rapidly suppressing the production and action of luteinizing hormone (LH) and follicle-stimulating hormone (FSH).

Triptorelin is a GnRH agaonist shown to inhibit estradiol-induced cancer cell proliferationIn vivo: (1) Triptorelin can improve the pregnancy rate by 12% to 15% in ewes6 and downregulate ovarian GnRHR-I expression of female rats, especially in late-growing follicles.(2) Triptorelin immunity blocked EET and UWT, inhibited uterine growth and development and enhance the expression levels s of ESR1, LHR, and FSHR proteins. [1]. Wei S et al. Triptorelin and cetrorelix induce immune responses and affect uterine development and expressions of genes and proteins of ESR1, LHR, and FSHR of mice. Immunopharmacol Immunotoxicol. 2016 Jun;38(3):197-204.

Alarelin Acetate is a synthetic GnRH agonist which can directly inhibit proliferation and DNA synthesis of rat GSMC through GnRH receptors.

Triptorelin acetate(57773-63-4 free base) (CL 118,532) is used as a GnRH agonist. It decreases pituitary secretion of gonadotropins luteinizing hormone (LH) and follicle-stimulating hormone (FSH) by causing constant stimulation of the pituitary. Triptorelin acetate(57773-63-4 free base) may be used in the treatment of hormone-responsive cancers such as breast cancer or prostate cancer, precocious puberty, estrogen-dependent conditions, and assisted reproduction.

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

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.

Nafarelin acetate(76932-56-4 free base) (RS-94991-298) is a GnRH agonist that acts as an analog of GnRH. Nafarelin acetate(76932-56-4 free base) causes a decrease in the pituitary secretion of gonadotropins luteinizing hormone (LH) and follicle-stimulating hormone (FSH). It may be used in the treatment of estrogen-dependent conditions.

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.

Ganirelix Acetate is a gonadotropin-releasing hormone (GnRH) receptor antagonist

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

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

LGnRH-III, lamprey acetate is an evolutionarily conserved member of the GnRH family, can stimulate the secretion of gonadotropins, it stimulates the secretion of both luteinizing and follicle-stimulating hormones.

Lecirelin acetate is a synthetic GnRH (gonadotropin releasing hormone) analogue which shows a great efficacy in the treatment of bovine ovarian follicular cysts.

DCOIT, an isothiazolinone derivative, stimulates the synthesis of follicle-stimulating hormone and luteinizing hormone in the brain by activating the gonadotropin-releasing hormone receptor (GnRHR). Additionally, it interferes with G protein-coupled receptors, MAPK, and Ca 2+ signaling pathways [1].

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

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.