产品描述:
Goserelin is a synthetic gonadotropin-releasing hormone (GNRH) agonist that binds to the GNRH receptor (GNRHR; Ki = 1.6 nM, in CHO cells expressing the human receptor).{36464} It binds to mouse pituitary αT3-1 cells and human placenta (Kds = 2 and 580 nM, respectively) and increases intracellular calcium in αT3-1 cells.{36465} Goserelin induces testosterone production in vitro within 4 h in rat Leydig cells (ED50 = 83 nM) but decreases testosterone plasma level in vivo in rats over a period of 2 to 24 weeks.{36466,36467} It inhibits tumor growth in a DU145 human prostate carcinoma mouse xenograft model when administered at a dose of 100 μg per day.{36468} Formulations containing goserelin have been used in the treatment of hormone-dependent breast and prostate cancers, as well as endometriosis and uterine fibroids.