Gonadotropin-releasing hormone 1 receptor (GnRH1R)

The gonadotropin-releasing hormone 1 receptor (GnRH1R) is a seven-transmembrane G protein-coupled receptor located primarily on pituitary gonadotrope cells, as well as extrapituitary sites including reproductive and some cancer tissues[1][4][6]. It mediates the physiological actions of GnRH—a decapeptide released by the hypothalamus—that regulates the synthesis and secretion of luteinizing hormone (LH) and follicle-stimulating hormone (FSH), playing a pivotal role in the control of reproduction[4][6][7][9]. Structurally, GnRH1R is notable for lacking the cytoplasmic C-terminal tail present in most class A GPCRs, leading to unique receptor activation and ligand-binding properties[1][2][3]. Pharmacologically, both agonists and antagonists for GnRH1R are widely used in reproductive medicine, hormone-dependent cancer therapy, and the management of diseases like endometriosis and infertility[3][5][6].

Other names

GnRH receptorGnRHRLuteinizing hormone-releasing hormone receptor (LHRHR)Gonadotrophin-releasing hormone receptorType I GnRH receptor

Agonists stimulate GnRH1R, causing receptor-mediated signaling and, with continued exposure, receptor downregulation and suppression of gonadotropin secretion. Antagonists block GnRH1R, inhibiting gonadotropin release and lowering sex steroid levels.