Gonadorelin is a synthetic peptide analog of gonadotropin-releasing hormone (GnRH) or luteinizing hormone releasing hormone (LHRH). Gonadorelin acts as an agonist at the GnRH/LHRH receptor, inducing release of follicle-stimulating hormone (FSH) and luteinizing hormone (LH). This hormone is clinically used to treat endometriosis. Gonadorelin exhibits anti-androgen and anticancer chemotherapeutic activities. In vitro and in vivo, gonadorelin inhibits testosterone activation of androgen receptors. Additionally, gonadorelin increases proliferation of normal cells but inhibits proliferation of prostate cancer cells through a mechanism that involved activation of the ryanodine receptor and increases in intracellular Ca2+ levels.