RS-127445|5-HT2B receptor antagonist|DC Chemicasl

RS-127445|5-HT2B receptor antagonist|DC Chemicasl

RS-127445 is a potent and selective antagonist at the serotonin 5-HT2B receptor, with around 1000x selectivity over the closely related 5-HT2A and 5-HT2C receptors.

Product Name: RS-127445 |Catalog Number:  DC8334 | cas: 199864-87-4 | Other names: RS-127445,RS 127445,RS127445,RS127,445,RS 127,445,RS-127,445 | Chemical name：4-(4-fluoro-1-naphthyl)-6-isopropylpyrimidin-2-amine | Molecule Formula: C17H16FN3.HCl | MW: 317.8

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 research and scientific purpose only, not for human use.