Abarelix;183552-38-7

ABARELIX is a gonadotropin-releasing hormone (GnRH) antagonist. First by the United States Praecis Pharmaceuticals research and development, has been in Europe for the treatment of prostate cancer Phase III clinical trials. Underway in the United States for the treatment of endometriosis clinical trial. Have used the drug, code-named R-3827 and PPI-l490.
In vitro experiments showed that, ABARELIX of luteinizing hormone-releasing hormone (LHRH) receptor with high affinity (KD = 1nmol / L), a LHRH antagonist completely. LHRH receptor binding with the drug can block D-His6-GNRH excitement role. Rat peritoneal macrophages in vitro experiments also show that this compound has a weak histamine-releasing activity, EC50 was 100mg/ml. In addition, ABARELIX soluble in water. All results are proved, ABARELIX generated in the block has a potential effect of sex hormones.