gonadotropin-releasing

Human Follicular Gonadotropin Releasing Peptide (hF-GRP) is a hormonal peptide that, in vitro, can induce the secretion of pituitary luteinizing hormone (LH) and follicle-stimulating hormone (FSH) [1] [2].

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

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

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

LH-RH II (chicken), a structural variant of mammalian luteinizing hormone-releasing hormone (LHRH) found in the hypothalamus of the domestic hen, exists as one of two forms of LHRH that enhance gonadotropin release in domestic chickens [1] [2].

Lamprey LH-RH I, a gonadotropin-releasing hormone, effectively increases plasma steroid levels and induces ovulation in lampreys, yet demonstrates no biological activity in other animal models [1].

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.

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

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

Histrelin (Supprelin LA) acetate is a nonapeptide analog of gonadotropin-releasing hormone (GnRH) with added potency. It is considered a GnRH agonist. Histrelin is used in the treatment of hormone-sensitive cancers of the prostate in men and uterine fibroids in women.

Kisspeptin-54 is a peptide ligand of the orphan G protein-coupled receptor GPR54 (Kis = 1.81 and 1.45 nM for rat and human receptors, respectively).1 It is a 54 amino acid peptide encoded by the metastasis suppressor gene KISS-1. Kisspeptin-54 induces calcium mobilization in CHO-K1 cells expressing rat and human receptors (EC50s = 1.39 and 5.47 nM, respectively). It also induces arachidonic acid release in CHO cells expressing rat and human GPR54 in a concentration-dependent manner. Kisspeptin-54 (10-1,000 nM) inhibits insulin secretion from isolated mouse pancreatic β-cells in the presence of 2.8 mM, but not 11.1 mM, glucose.2 Kisspeptin-54 (1-5 nmol, i.c.v.) increases serum levels of luteinizing hormone (LH) and follicular stimulating hormone (FSH) in mice, an effect which is reversed by the gonadotropin releasing hormone (GNRH) antagonist acycline.3References1. Kotani, M., Detheux, M., Vandenbogaerde, A.L., et al. The metastasis suppressor gene KiSS-1 encodes kisspeptins, the natural ligands of the orphan G protein-coupled receptor GPR54. J. Biol. Chem. 276(37), 34631-34636 (2001).2. Vikman, J., and Ahrén, B. Inhibitory effect of kisspeptins on insulin secretion from isolated mouse islets. Diabetes Obes. Metab. 11(Suppl 4), 197-201 (2009).3. Gottsch, M.L., Cunningham, M.J., Smith, J.T., et al. A role for kisspeptins in the regulation of gonadotropin secretion in the mouse. Endocrinology 145(9), 4073-4077 (2004). Kisspeptin-54 is a peptide ligand of the orphan G protein-coupled receptor GPR54 (Kis = 1.81 and 1.45 nM for rat and human receptors, respectively).1 It is a 54 amino acid peptide encoded by the metastasis suppressor gene KISS-1. Kisspeptin-54 induces calcium mobilization in CHO-K1 cells expressing rat and human receptors (EC50s = 1.39 and 5.47 nM, respectively). It also induces arachidonic acid release in CHO cells expressing rat and human GPR54 in a concentration-dependent manner. Kisspeptin-54 (10-1,000 nM) inhibits insulin secretion from isolated mouse pancreatic β-cells in the presence of 2.8 mM, but not 11.1 mM, glucose.2 Kisspeptin-54 (1-5 nmol, i.c.v.) increases serum levels of luteinizing hormone (LH) and follicular stimulating hormone (FSH) in mice, an effect which is reversed by the gonadotropin releasing hormone (GNRH) antagonist acycline.3 References1. Kotani, M., Detheux, M., Vandenbogaerde, A.L., et al. The metastasis suppressor gene KiSS-1 encodes kisspeptins, the natural ligands of the orphan G protein-coupled receptor GPR54. J. Biol. Chem. 276(37), 34631-34636 (2001).2. Vikman, J., and Ahrén, B. Inhibitory effect of kisspeptins on insulin secretion from isolated mouse islets. Diabetes Obes. Metab. 11(Suppl 4), 197-201 (2009).3. Gottsch, M.L., Cunningham, M.J., Smith, J.T., et al. A role for kisspeptins in the regulation of gonadotropin secretion in the mouse. Endocrinology 145(9), 4073-4077 (2004).

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

Nafarelin is a gonadotropin-releasing hormone (GnRH) agonist. Nafarelin increases the release of luteinizing hormone (LH) and follicle stimulating hormone (FSH) by the anterior pituitary leading to an increase of estrogen progesterone.

Fertirelin, or fertirelin acetate, sold under the brand name Ovalyse, is a gonadotropin-releasing hormone agonist (GnRH agonist).

Des-Gly10,D-Ala6,Pro-NHEt9)-LHRH (salmon), a gonadotropin-releasing hormone (GnRH) analog, effectively induces ovulation and or spawning in farmed fish [1].

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

Kisspeptin 234 acetate(1145998-81-7 free base) is a Kisspeptin receptor (KISS1, GPR54) antagonist; a Kisspeptin-10 analogue. It inhibits the stimulation of inositol phosphate (IP) (IC50 = 7 nM) and the release of gonadotropin-releasing hormone (GnRH) by kisspeptin-10.

Goserelin is a gonadotropin-releasing hormone (GnRH LHRH) deceptide-like agent that acts as a GnRH agonist. It is suitable for hormone therapy of prostate cancer, premenopausal and perimenopausal breast cancer, endometriosis.

Gonadotropin-Releasing Hormone-Associated Peptide (GAP) (1-24), human, also known as hGAP-1-24, is the 1-24 fragment of the human GAP, which is connected to the luteinizing hormone-releasing hormone (LH-RH) through a 3 amino acid processing site [1].

Acyline is a novel GnRH antagonist found in animal studies to be a potent suppressor of circulating gonadotropin and testosterone (T) levels. Acyline inhibits basal and GnRH-stimulated serum testosterone concentrations in male dogs. Acyline prevented ovulation, but did not affect ovarian follicular development or gestational corpora lutea in the domestic cat. A single dose of the potent gonadotropin-releasing hormone antagonist acyline suppresses gonadotropins and testosterone for 2 weeks in healthy young men.

sGnRH-A, a salmon gonadotropin-releasing hormone (GnRH) analogue, promotes growth hormone secretion and serves as an ovulation inducer for artificial insemination [1] [2].

[D-Glp1,D-Phe2,D-Trp3,6]-LH-RH, a luteinizing hormone-releasing hormone (LHRH) analogue, acts as a gonadotropin-releasing hormone (GnRH) receptor antagonist [1].

[MePhe7]-Neurokinin B is a neurokinin NK-3 receptor (NK3R) agonist, exhibiting a potent agonistic activity with an IC50 value of 3 nM. It acts as a potential regulator of pulsatile gonadotropin-releasing hormone (GnRH) secretion through the activation of NK3R [1].

Neurokinin B (NKB) belongs in the family of tachykinin peptides. Neurokinin B is implicated in a variety of human functions and pathways such as the secretion of gonadotropin-releasing hormone.