RS-127445 (C007B-258565)

InformationRS-127445 (MT500) is a selective5-HT2Breceptor antagonist withpKiof 9.5 andpIC50of 10.4, exhibits >1000-fold selectivity against other 5-HT receptors.Targets5-HT2B ; 5-HT2B 10.4(pIC50); 9.5(pKi)In vitroRS-127445 is a novel high affinity, selective 5-HT2B receptor antagonist devoid of detectable intrinsic activity. RS-127445 is found to have nM affinity and 1000 fold selectivity for the 5-HT2B receptor. RS-127445 is thus among the highest affinity, most selective 5- HT2B receptor ligands. RS-127445 potently blocks the 5-HT evoked increase in inositol phosphate formation and blocks the 5-HT evoked increases in intracellular calcium concentrations with a potency 1000 times greater than that of yohimbine. In vivoRS-127445 is readily absorbed with no obvious dose or route-dependent limitations and rapidly absorbed following both oral and intraperitoneal administration with peak plasma concentrations being achieved within 15 min of dosing. RS-127445 concentration in the plasma are proportional to the administered dose. RS-127445 administrated at dose of 5 mg/kg with approximately 60% of an intraperitoneal dose and 14% of the oral dose is bioavailable. RS-127445 concentration in the plasma is predicted to fully saturate accessible 5-HT2B receptors can be readily achieved and maintained in the rat. RS-127445 administered at 1 to 10 mg/kg with oral significantly inhibits visceral hypersensitivity up to 35 to 74% provoked by restraint stress. Oral RS-127445 produces a significant suppression of TNBS-induced visceral hypersensitivity (15 to 62% inhibition at 3 to 30 mg/ kg), although RS-127445 has no significant effect on the visceral nociceptive threshold of native rats. RS-127445 administrated orally with 1 to 30 mg/kg also dose -dependently reduce the restraint stress-induced defecation in native and TNBS-treated rats. RS-127445 inhibits colonic motility and defecation.Cell Research(from reference)Cell lines：HEK-293 cells expressing the human 5-HT2B receptor Concentrations：10 μM Incubation Time：20 min. Specification: 0.97 Molecular Formula: C17H16FN3 Molecular Weight: 281.34 PubChem CID: 196968 Isomeric SMILES: CC(C)C1=NC(=NC(=C1)C2=CC=C(C3=CC=CC=C32)F)N Related Documents: https://ald-pub-files.oss-cn-shanghai.aliyuncs.com/aladdinsci/pdp/sds/1/R412793-SCI_71ff505256e662ba84ca157e2e308828.pdf