Histrelin acetate, a GnRH analogue, is a GnRH Receptor agonist. Histrelin acetate increases serum luteinising hormone (LH), follicle stimulating hormone (FSH) and testosterone levels. Histrelin acetate can be used in the research of prostate cancer, endometriosis[1][2][5].
Leuprolide acetate is a potent gonadotropin-releasing hormone receptor agonist used for the treatment of prostate cancer, endometriosis, uterine fibroids.
Goserelin (ICI 118630) acetate is an injectable gonadotropin releasing hormone superagonist (GnRH agonist).IC50 value:Target: GnRH agonistGoserelin is used to treat hormone-sensitive cancers of the breast (in pre- and peri- menopausal women) and prostate, and some benign gynaecological disorders (endometriosis, uterine fibroids and endometrial thinning). In addition, goserelin is used in assisted reproduction and in the treatment of precocious puberty. It may also be used in the treatment of male-to-female transsexuals and is favoured above other anti-androgens in some countries, such as the UK. It is available as a 1-month depot and a long-acting 3-month depot. Goserelin stimulates the production of the sex hormones testosterone and estrogen in a non-pulsatile (non-physiological) manner.
(D-Trp6)-LHRH free acid is a luteinizing hormone-releasing hormone (LHRH) agonist[1].
Gonadoliberin (GnRH) is a synthetic GnRH. Gonadoliberin binds to GnRH receptor on the cell surface of the gonadotrope, and activates the synthesis and release of LH and FSH[1][2].
LH-RH (7-10) is a tetrapeptide, one of major degradation products of luteinising-hormone releasing hormone (LHRH) via pituitary and hypothalamus. LH-RH (7-10) produced in macrophages, type I-like and type II pneumocytes[3].
Lamprey LH-RH I is a gonadotropin-releasing hormone, elevates plasma steroid levels and stimulates ovulation in the lamprey without biological activity in other animal models[1].
(D-Tyr5,D-Ser(tBu)6,Azagly10)-LHRH is an analogue of luteinizing hormone-releasing hormone (LHRH). LHRH plays a central role in the control of reproduction by stimulating the release of pituitary luteinizing hormone (LH) and follicle-stimulating hormone (FSH)[1].
WAY-207024 (dihydrochloride) is a potent and orally active GnRH antagonist that reduces leuteinizing hormone (LH) levels in plasma[1].
Elagolix is a highly potent, selective, orally-active, short-duration, non-peptide antagonist of the gonadotropin-releasing hormone receptor (GnRHR) (KD = 54 pM).Target: GnRHin vitro: Elagolix is a short-acting, nonpeptide, GnRH antagonist, 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 is regarded as the frontrunner of a new class of GnRH inhibitors that have been denoted as second-generation, due to their non-peptide nature and oral bioavailability.
(Des-Gly10,D-Ala6,Pro-NHEt9)-LHRH (salmon) is a GnRH analog that induces ovulation and/or spawning in farmed fish[1].
Nafarelin is a gonadotropin-releasing hormone (GnRH) agonist that stimulates secretion of luteinizing hormone (LH) and follicle-stimulating hormone (FSH). Sequence: {Glp}-His-Trp-Ser-Tyr-{2-Naph-Ala}-Leu-Arg-Pro-Gly-NH2.
Acyline , a GnRH peptide analogue, is a GnRH antagonist that inhibits gonadotropin and testosterone (T) levels[1].
FSH receptor-binding inhibitor fragment(bi-10) is a potent FSH antagonist. FSH receptor-binding inhibitor fragment(bi-10) blocks the binding of FSH to FSHR, and alteres FSH action at the receptor level. FSH receptor-binding inhibitor fragment(bi-10) results in the suppression of ovulation and causes follicular atresia of mice. FSH receptor-binding inhibitor fragment(bi-10) has the potential for utilizing to restrain the carcinogenesis of ovarian cancer by down-regulating overexpression of FSHR and ERβ in the ovaries[1].
Phoenixin-14 (PNX-14) is one of the endogenous active isoform, and generates anxiolytic effect via the activation of the AHA GnRH system in mice. Phoenixin-14 inhibits ischemia/reperfusion-induced cytotoxicity in microglia[1][2].
GnRH Associated Peptide (GAP) (1-13), human is an amino acid peptide fragment derived from GnRH. GAP can increase the secretion of luteinizing hormone (LH) and follicle-stimulating hormone (FSH) in rat anterior pituitary cells. GAP also inhibit the secretion of prolactin[1].
Alarelin acetate is a synthetic GnRH agonist.
Triptorelin acetate is a Gonadotropin-releasing hormone (GnRH) receptor agonist[1].
Antide (D-21074) is a potent LHRH antagonist. Antide also can be used for the research of prostatic cancer.
Bim 21009 is an inhibitor of gonadorelin.
Degarelix is a competitive and reversible gonadotropin-releasing hormone receptor (GnRHR) antagonist.
sGnRH-A is a salmon gonadotropin-releasing hormone (GnRH) analogue that stimulates growth hormone secretion and can also be used as an inducer of ovulation by artificial insemination[1][2].
NBI-42902 is an orally active, potent functional and competitive antagonist of GnRH receptor with an IC50 value of 0.79 nM, a Ki value of 0.56 nM, respectively. NBI-42902 inhibits GnRH-stimulated inositol phosphate (IP) accumulation, Ca2+ flux, and ERK1/2 activation. NBI-42902 inhibits serum luteinizing hormone (LH) in castrated male macaques. NBI-42902 can be used for research on sex-hormone-related diseases[1].
Kisspeptin 13 is a GPR54 and GnRH receptor activator, an endogenous active isoform. Kisspeptin 13 enhances memory and can be used in Alzheimer's disease research[1].
(Des-Gly10,D-Ala6,Pro-NHEt9)-LHRH (Surfagon, Mwt 1167.34 Da) is an agonist of gonadotropin-releasing hormone (GnRH). (Des-Gly10,D-Ala6,Pro-NHEt9)-LHRH can be used as an internal standard for the LC-MS analysis of leuprorelide acetate. (Des-Gly10,D-Ala6,Pro-NHEt9)-LHRH has potential applications in biochemical analysis and fertility[1][2][3].
Kisspeptin-54(human) (Metastin(human)) is an endogenous ligand for kisspeptin receptor (KISS1, GPR54). Kisspeptin-54(human) binds to rat and human GPR54 receptors with Ki values of 1.81 nM and 1.45 nM, respectively. Kisspeptin-54(human) hinders tumor metastasis and stimulates gonadotropin secretion[1][2].
[D-Glp1,D-Phe2,D-Trp3,6]-LH-RH is a Luteinizing-hormone-releasing hormone (LHRH) analogue. [D-Glp1,D-Phe2,D-Trp3,6]-LH-RH acts as a GnRH receptor antagonist[1].
Ganirelix acetate (Ganirest) is an injectable competitive gonadotropin-releasing hormone (GnRH) antagonist. Ganirelix acetate directly competes against the endogenous molecule for receptor binding, and causes a rapid reduction in estradiol levels. Ganirelix acetate can be used for researching ovarian hyperstimulation syndrome (OHSS)[1].
BAY-784 is a gonadotropin releasing hormone receptor (GnRH-R) antagonist probe with IC50s of 21 and 24 nM for human and rat GnRH-R, respectively[1].
AG-045572 is a GnRH receptor antagonist with Kis of 6.0 nM and 3.8 nM for human and rat GnRH receptor, respectively. AG-045572 is metabolized by CYP3A and ressuppresses testosterone[1].