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.
Lecirelin is a synthetic gonadotropin-releasing hormone (GnRH) analogue. Lecirelin is widely used for the research of bovine ovarian follicular cysts[1].
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.
Relugolix is a novel, non-peptide, orally active gonadotropin-releasing hormone (GnRH) antagonist with IC50 of 0.33 nM in the presence of 40% fetal bovine serum, TAK-385 possesses higher affinity and potent antagonistic activity compared with TAK-013.target: GnRH [1]IC50: 0.33 nM [1]In vivo: In female knock-in mice, twice-daily oral administration of TAK-385 (100mg/kg) induces constant diestrous phases within the first week, decreases the uterus weight to ovariectomized levels and downregulated GnRH receptor mRNA in the pituitary after 4 weeks.[2]
Opigolix is a Gonadotropin-releasing hormone (GnRH) receptor antagonist, used for the research of endometriosis and rheumatoid arthritis.
Degarelix acetate hydrate is a competitive and reversible gonadotropin-releasing hormone receptor (GnRHR/LHRHR) antagonist. Degarelix acetate hydrate can be used for prostate cancer research[1].
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]
[D-Lys6]-LH-RH is a Luteinizing-hormone-releasing hormone (LHRH) analogue. [D-Lys6]-LH-RH acts as a GnRH receptor agonist[1].
LH-RH (4-10) is a heptapeptide, one of major degradation products of luteinising-hormone releasing hormone (LHRH) via pituitary and hypothalamus. LH-RH (4-10) produced in macrophages and type II pneumocytes[1].
Histrelin, a GnRH analogue, is a GnRH Receptor agonist. Histrelin increases serum luteinising hormone (LH), follicle stimulating hormone (FSH) and testosterone levels. Histrelin can be used in the research of prostate cancer, endometriosis[1][2][5].
A novel potent gonadotrophin releasing hormone (GnRH) antagonist.
Teverelix (EP 24332) is a GnRH antagonist. Teverelix binds competitively and reversibly to GnRH receptors, thereby suppressing the release of LH and FSH. Teverelix can be used in the research of prostatic hyperplasia, endometriosis, and prostate cancer[1][2].
(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.
Onvitrelin ucalontide ([Phor18-LHRH (338613)]) is an analogue of luteinizing hormone releasing hormone (LHRH) with antineoplastic activity. Onvitrelin ucalontide is a peptide with sequences of KFAKFAKKFAKFAKKFAKQHWSYGLRPG. Onvitrelin ucalontide effectively inhibits breast cancer, ovarian cancer and prostate cancer xenografts in mouse model[1][2].
Leuprolide is an agonist at pituitary GnRH receptors. Target: GnRH receptorLeuprorelin is a gonadotrophin-releasing hormone (GnRH) analogue used to treat a wide range of sex hormone-related disorders including advanced prostatic cancer, endometriosis and precocious puberty. Leuprorelin acts primarily on the anterior pituitary, inducing a transient early rise in gonadotrophin release. With continued use, Leuprorelin causes pituitary desensitisation and/or down-regulation, leading to suppressed circulating levels of gonadotrophins and sex hormones. [1] 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. [2]
GnRH Associated Peptide (GAP) (1-24), human is the human gonadotropin-releasing hormone-associated peptide (GAP) 1-24 fragment (hGAP-1-24). GAP is joined to the luteinizing hormone-releasing hormone (LH-RH) sequence by a 3 amino acid processing site[1].
Merigolix is a potent gonadotrophin releasing hormone (GnRH) antagonist[1].
Elagolix sodium is a human GnRH receptor (GnRHR) antagonist with an IC50 and Ki of 0.25 and 3.7 nM, respectively.
Cetrorelix Acetate is a potent gonadotropin-releasing hormone (GnRH) receptor antagonist with an IC50 of 1.21 nM. Sequence: N-acetyl-{2-Naph-Ala}-{Cl-Phe}-{3Py-Ala}-Ser-Tyr-{Cit}-Leu-Arg-Pro-Ala-NH2.
GnRH Associated Peptide (GAP) (25-53), human is the human gonadotropin-releasing hormone-associated peptide (GAP) 25-53 fragment (hGAP-25-53), can be used as immunogen to generate antiseras including MC-1, MC-2, and MC-3. GAP is joined to the luteinizing hormone-releasing hormone (LH-RH) sequence by a 3 amino acid processing site[1].
Fluorogestone acetate is a progesterone compound. Fluorogestone acetate inhibits ovulation and synchronizes the estrous cycle in cattle by inhibiting the release of luteinizing hormone (LH) from the pituitary gland[1].
Cetrorelix diacetate (SB-075 diacetate) is a potent gonadotropin-releasing hormone (GnRH) receptor antagonist with an IC50 of 1.21 nM[1].
Cetrorelix is a potent gonadotrophin-releasing hormone (GnRH) antagonist. Cetrorelix inhibits the endogenous luteinizing hormone surge during ovarian stimulation. Cetrorelix reduces cyclophosphamide induced ovarian follicular destruction in mice[1][2].
LHRH, the luteinizing hormone-releasing hormone, is a neuropeptide hypothalamic. LHRH regulates reproduction. LHRH can be used for the research of cancer[1].