Gonadotropin releasing hormone receptor

Human growth hormone-releasing factor acetate is a hypothalamic polypeptide and stimulates GH production and release by binding to the GHRH Receptor (GHRHR) on cells in the anterior pituitary[1].

Luteinizing Hormone Releasing Hormone (LH-RH), synthesized in the hypothalamus, is a pituitary hormone that plays a crucial role in controlling reproductive function.

Thyrotropin-Releasing Hormone (TRH), Free Acid (TRH-OH), induces various thyroidal and non-thyroidal effects, most notably the feedback regulation of thyroid hormone levels.

Human Growth Hormone-Releasing Factor TFA, also known as Growth Hormone-Releasing Factor Human TFA, is a hypothalamic polypeptide that promotes the production and release of growth hormone (GH) through its interaction with the Growth Hormone-Releasing Hormone Receptor (GHRHR) on anterior pituitary cells [1].

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].

Human growth hormone-releasing factor stimulates GH production and release by binding to the GHRH Receptor (GHRHR) on cells in the anterior pituitary.Growth hormone-releasing hormone is a hormone produced in the hypothalamus. The main role of growth hormo

Growth hormone releasing peptide ia a natual product ,and has anti-inflammatory effects, due to its inhibitory effect on PKC-induced activation of p38, JNK and NF-κB, possibly by targeting to MKP-1 and PP2A.

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.

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

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

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

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).

Ganirelix Acetate is a gonadotropin-releasing hormone (GnRH) receptor antagonist

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

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

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

[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].

[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].

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-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).

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

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.

Agonist of the NPFF1 receptor (IC50 = 0.7 nM for inhibition of forskolin-induced cAMP production). Homolog of gonadotropin-inhibitory hormone (GnIH); inhibits activity of gonadotropin-releasing hormone (GnRH) neurons.

Phoenixin-14 TFA (PNX-14) is a blood-brain barrier (BBB)-penetrable neuropeptide with anxiolytic, cardioprotective, and neuroprotective properties. It modulates pituitary gonadotrophin release by enhancing gonadotropin-releasing hormone (GnRH) receptor mRNA expression and promotes insulin secretion. Additionally, PNX-14 TFA protects against ischemia reperfusion (IR) injury in mice and combats oxidative stress by diminishing reactive oxygen species (ROS) and elevating glutathione (GSH) levels [1] [2] [3].