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].
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].
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].
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].
[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].
Deslorelin is a GnRH agonist. Deslorelin implants can be used as an alternative to dopamine agonists to induce fertil eoestrus in the bitch in anoestrus. The deslorelin implant can be used successfully in the queen for oestrus inhibition. Deslorelin acetate did not significantly affect the spontaneous contraction amplitude but caused a decrease in the frequency in the dorsal and ventral parts of the bladder.
Goserelin(ICI 118630) 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.
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.
Buserelin (INN) Acetate is a gonadotropin-releasing hormone agonist (GnRH agonist).target: GnRHIn vivo: Buserelin treatment reduced the number of neurons along the entire gastrointestinal tract, with increased relative numbers of CRF-immunoreactive submucosal and myenteric neurons in colon (p < 0.05 and p < 0.01, respectively).[1]Compared with controls, buserelin treatment caused loss of myenteric neurons in the ileum and colon (P<0.01), a thinner circular muscle layer in ileum (P<0.05) and longitudinal muscle layer in colon (P<0.05). Long term follow up of buserelin induced enteric neuropathy reveals reduced body weight, loss of myenteric neurons, thinning of muscle layers, and increased numbers of eosinophils and T lymphocytes in the gastrointestinal tract.[2] A marked enteric neuronal loss with modest effects on GI function is found after buserelin treatment. Increased feces fat content is suggested an early sign of dysfunction.[3]
A novel potent gonadotrophin releasing hormone (GnRH) antagonist.
(D-Ser(tBu)6,D-Leu7,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].
Ozarelix (D-63153) is a GnRH antagonist. Ozarelix induces cell apoptosis and arrests cell in G2/M phase. Ozarelix can be used in the research of prostate cancer[1].
Abarelix is a potent gonadotrophin-releasing hormone (GnRH) antagonist, used for prostate cancer treatment.
MI 1544 is a LHRH antagonist.
(D-Ser4,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].
Gonadorelin acetate is a man-made protein that is like a hormone in the body called gonadotropin-releasing hormone (GnRH). Target: GNRH ReceptorGonadorelin acetate is a synthetic decapeptide prepared using solid phase peptide synthesis. GnRH is responsible for the release of follicle stimulating hormone and leutinizing hormone from the anterior pitutitary.