GNRH Receptor

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.

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.

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

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

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

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

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

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

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

(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.

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.

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.

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

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

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).

Histrelin acetate is a nonapeptide analog of gonadotropin-releasing hormone (GnRH) with added potency. It acts on particular cells of the pituitary gland called gonadotropes when present in the bloodstream. Histrelin stimulates these cells to release luteinizing hormone and follicle-stimulating hormone. Thus it is considered a gonadotropin-releasing hormone agonist or GnRH agonist.

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

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

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.

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.

AG 045572 is a potent GnRH receptor antagonist that inhibits the GnRH receptor in humans and rats with Ki values of 6.0 nM and 3.8 nM, respectively.AG 045572 is metabolized by CYP3A and inhibits testosterone.

Leuprolide Acetate (53714-56-0 free base) (Leuprorelin acetate) is an agonist at pituitary GnRH receptors. Leuprolide Acetate (53714-56-0 free base) is a gonadotropin-releasing hormone (GnRH) analog used to treat a wide range of sex hormone-related disorders including advanced prostatic cancer, endometriosis, and precocious puberty. Leuprolide Acetate (53714-56-0 free base) acts primarily on the anterior pituitary, inducing a transient early rise in gonadotrophin release. With continued use, Leuprolide Acetate (53714-56-0 free base) causes pituitary desensitization and or down-regulation, leading to suppressed circulating levels of gonadotrophins and sex hormones.By interrupting the normal pulsatile stimulation of, and thus desensitizing, the GnRH receptors, it indirectly downregulates the secretion of gonadotropins luteinizing hormone (LH) and follicle-stimulating hormone (FSH), leading to hypogonadism and thus a dramatic reduction in estradiol and testosterone levels in both sexes.

Phoenixin-14 (PNX-14), an active endogenous isoform, induces an anxiolytic effect by activating the AHA GnRH system in mice and protects against ischemia/reperfusion-induced cytotoxicity in microglia [1] [2].

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

GnRH-R antagonist 1 (Compound 21a), is an orally active, membrane-permeable agent with a high binding affinity (IC50=0.57 nM) and potent in vitro antagonistic efficacy (IC50=2.18 nM). It is utilized in research focused on advanced prostate cancer and the prevention of premature LH surges [1].

Luteinizing hormone-releasing hormone (LHRH) is a neuropeptide produced in the hypothalamus that plays a pivotal role in regulating reproduction and has applications in cancer research [1].