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Introduction: Gonadotropin-releasing hormone (GnRH), the first key hormone of the reproductive system, is synthesized in the hypothalamus and stimulates pituitary luteinizing hormone (LH) and follicle-stimulating hormone (FSH) synthesis and release. The neurohormone GnRH binds to a seven transmembrane domain receptor (1–4). The cloned cDNA encodes a 327 amino acid receptor protein which lacks the common cytoplasmic carboxy terminal domain. The availability of the receptor cDNA will open a new vista for elucidation of receptor structure, ligand binding sites and development of peptide and nonpeptide agonists and antagonists. The GnRH receptor is expressed exclusively on pituitary gonadotrophs (about 5–10% of pituitary cells) which consist of 60% multihormonal cells (LH+FSH), 18% LH- and 22% FSH-containing cells (5). Occupancy of 20% of GnRH receptors is sufficient to evoke about 80% of the biological response (6). GnRH receptor complexes form aggregrates and internalization occurs in small vesicles which may transfer GnRH to the lysosome
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