gnrh receptor

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.

Dimethandrolone Undecanoate (DMAU) is a novel orally available androgen with progestational activity and is a potential male contraceptive compound.

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.

Fluorogestone acetate shows high potency with a short duration of activity and is physiologically similar to progesterone. FGA is approximately 20-25 times more potent than progesterone.

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

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.

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

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) .

(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.

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

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.

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.

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.

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

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.

GnRH antagonist 2 is a GnRH receptor antagonist used in endocrine disease research.

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).

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

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).

Ozarelix is a fourth generation GnRH antagonist, induces apoptosis in hormone refractory androgen receptor negative prostate cancer cells modulating expression and activity of death receptors. Mechanistically, LHRH antagonists exert rapid inhibition of luteinizing hormone and follicle stimulating hormone with an accompanying rapid decrease in sex hormones and would therefore be expected to be effective in a variety of hormonally dependent disease states including ovarian cancer, prostate cancer, BPH, infertility, uterine myoma and endometriosis. BPH is a non-cancerous enlargement of the prostate that is caused by testosterone. Unlike LHRH agonists, ozarelix has the potential to reduce testosterone just enough to reduce both prostate size and symptoms without the severe side effects associated with a reduction in testosterone.

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

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].