GNRHR, Gonadotropin Releasing Hormone Receptor, GnRH-R, GRHR, Gonadotropin-Releasing Hormone (Type 1) Receptor 1, Leutinizing-Releasing Hormone Receptor, Type I GnRH Receptor, Luliberin Receptor, GNRHR1, LHRHR, LRHR, HH7, Receptors, LHRH, GnRH receptor, Gonadotropin-Releasing Hormone Receptor, Leutinizing Hormone Releasing Horomone Receptor


Gonadotropin-releasing hormone receptor(GNRHR)is a protein that in humans is encoded by the GNRHR gene. This gene encodes the receptor for type 1 gonadotropin-releasing hormone. This receptor is a member of the seven-transmembrane, G-protein coupled receptor (GPCR) family. It is expressed on the surface of pituitary gonadotrope cells as well as lymphocytes, breast, ovary, and prostate. Following binding of gonadotropin-releasing hormone, the receptor associates with G-proteins that activate a phosphatidylinositol-calcium second messenger system. Activation of the receptor ultimately causes the release of gonadotropic luteinizing hormone (LH) and follicle stimulating hormone (FSH). Defects in this gene are a cause of hypogonadotropic hypogonadism (HH). Alternative splicing results in multiple transcript variants encoding different isoforms. More than 18 transcription initiation sites in the 5' region and multiple polyA signals in the 3' region have been identified for this gene.

KO Status


Drug Information

Launched drugs: 10
Drugs in clinical trials: 5
Latest Research Phase: Approved

Drug Name





Clinical Trials

Alarelin Acetate


Maanshan Fengyuan Pharmaceutical Co Ltd


Relugolix/Estradiol/Norethindrone Acetate


Myovant Sciences

Leiomyoma, Menorrhagia

Degarelix Acetate

ASP-3550, FE-200486, Uglypeptide-1


Ferring Bv

Prostatic Hyperplasia, Prostatic Neoplasms, Lower Urinary Tract Symptoms, Infertility, Female

Cetrorelix Acetate

SB-75, NS 75B, SB-075, D-20761, NS-75A (acetate), NS-75B (pamoate salt), D-20453 (trifluoroacetate)


Merck Serono

Prostatic Hyperplasia, Polycystic Ovary Syndrome, Endometriosis, Endocrine System Diseases, Infertility, Female

Elagolix Sodium

ABT-620, NBI-56418


Neurocrine Biosciences

Pain, Polycystic Ovary Syndrome, Endometriosis, Leiomyoma, Menorrhagia, Uterine Hemorrhage

Triptorelin Pamoate

Debio-8206 (pamoate salt), D-Trp6-LHRH, Debio 8206 SC, (D-Trp6)-LH-RH, Debio 8206 CPP, AY-25650, BN-52014, Wy-42422, Wy-42462, BIM-21003, CL-118532


Actavis A/S

Endometriosis, Prostatic Neoplasms, Puberty, Precocious


P76B05O5V6 (UNII code), TAK-385, RVT-601


Takeda Pharmaceutical Co Ltd

Pain, Contraception, Endometriosis, Prostatic Neoplasms, Leiomyoma, Menorrhagia

Ganirelix Acetate

D-24598, RS-26306, ORG 37462, Org-37462



Endocrine System Diseases, Infertility, Female

Triptorelin Acetate



HIV Infections, Endometriosis, Prostatic Neoplasms, Leiomyoma, Myoma, Puberty, Precocious

Gonadorelin acetate



Mitsubishi Tanabe Pharma Corp

Prostatic Hyperplasia, Polycystic Ovary Syndrome, Endometriosis





Inhibition of gonadotropin-releasing hormone receptor signaling by expression of a splice variant of the human receptor

Grosse R., Schoneberg T., Schultz G., Gudermann T.,

Mol. Endocrinol. 11:1305-1318(1997)

The status, quality, and expansion of the NIH full-length cDNA project: the Mammalian Gene Collection (MGC)

The MGC Project Team,

Genome Res. 14:2121-2127(2004)

Tissue-specific pattern of variant transcripts of the human gonadotropin-releasing hormone receptor gene

Kottler M.L., Bergametti F., Carre M.C., Morice S., Decoret E., Lagarde J.P., Starzec A., Counis R.,

Eur. J. Endocrinol. 140:561-569(1999)

A family with hypogonadotropic hypogonadism and mutations in the gonadotropin-releasing hormone receptor

de Roux N., Young J., Misrahi M., Genet R., Chanson P., Schaison G., Milgrom E.,

N. Engl. J. Med. 337:1597-1602(1997)

Mutations in gonadotropin-releasing hormone receptor gene cause hypogonadotropic hypogonadism

Layman L.C., Cohen D.P., Jin M., Xie J., Li Z., Reindollar R.H., Bolbolan S., Bick D.P., Sherins R.R., Duck L.W., Musgrove L.C., Sellers J.C., Neill J.D.,

Nat. Genet. 18:14-15(1998)

The same molecular defects of the gonadotropin-releasing hormone receptor determine a variable degree of hypogonadism in affected kindred

de Roux N., Young J., Brailly-Tabard S., Misrahi M., Milgrom E., Schaison G.,

J. Clin. Endocrinol. Metab. 84:567-572(1999)

Resistance of hypogonadic patients with mutated GnRH receptor genes to pulsatile GnRH administration

Caron P., Chauvin S., Christin-Maitre S., Bennet A., Lahlou N., Counis R., Bouchard P., Kottler M.-L.,

J. Clin. Endocrinol. Metab. 84:990-996(1999)

Cloning, sequencing, and expression of human gonadotropin releasing hormone (GnRH) receptor

Kakar S.S., Musgrove L.C., Devor D.C., Sellers J.C., Neill J.D.,

Biochem. Biophys. Res. Commun. 189:289-295(1992)

Cloning and characterization of the human GnRH receptor

Chi L., Zhou W., Prikhozhan A., Flanagan C.A., Davidson J.S., Golembo M., Illing N., Millar R.P., Sealfon S.C.,

Mol. Cell. Endocrinol. 91:R1-R6(1993)

The nucleotide sequences of human GnRH receptors in breast and ovarian tumors are identical with that found in pituitary

Kakar S.S., Grizzle W.E., Neill J.D.,

Mol. Cell. Endocrinol. 106:145-149(1994)