| References: |
RS-127445 is a potent, selective and high affinity serotonin 5-HT2B receptor antagonist with a pIC50 of 10.4. The affinity (pKi) of RS-127445 for the 5-HT2B receptor is 9.5. RS-127445 is selective for the 5-HT2B receptor, having approximately 1000 fold selectivity over the human recombinant 5-HT2A, 5-HT2C, 5-HT5, 5-HT6 and 5-HT7 receptors, a 5-HT1A receptor in rat brain membranes, a 5-HT1B/D receptor in bovine caudate, and a monoamine uptake site in rabbit platelets. In the HEK-293 cells expressing the 5-HT2B receptor, RS-127445 potently antagonizes 5-HT-evoked formation of inositol phosphates (pKB=9.5±0.1) and 5-HT-evoked increases in intracellular calcium (pIC50=10.4±0.1). In addition, RS-127445 also blocks 5-HT-evoked contraction of rat isolated stomach fundus and (±) α-methyl-5-HT-mediated relaxation of the rat jugular vein with pA2 values of 9.5 and 9.9. In vivo, intraperitoneal administration of RS-127445 (5mg/kg) produces plasma concentrations predicted to fully saturate accessible 5-HT2B receptors for at least 4h. RS-127445 (0.1–10 µM) concentration-dependently reduces peristaltic frequency. RS-127445 (1–30 mg/kg), dose-dependently reduced faecal output, reaching significance at 10 and 30 mg/kg. For the detailed information of RS-127445, the solubility of RS-127445 in water, the solubility of RS-127445 in DMSO, the solubility of RS-127445 in PBS buffer, the animal experiment (test) of RS-127445, the cell expriment (test) of RS-127445, the in vivo, in vitro and clinical trial test of RS-127445, the EC50, IC50,and affinity,of RS-127445, For the detailed information of RS-127445, the solubility of RS-127445 in water, the solubility of RS-127445 in DMSO, the solubility of RS-127445 in PBS buffer, the animal experiment (test) of RS-127445, the cell expriment (test) of RS-127445, the in vivo, in vitro and clinical trial test of RS-127445, the EC50, IC50,and affinity,of RS-127445, Please contact DC Chemicals. |
