RS-127445

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Chemical Information

Product name：RS-127445	Purity：98% min
CAS NO：199864-87-4	Solubility：DMSO : ≥ 31 mg/mL (97.55 mM)
Molecular Formula：C₁₇H₁₇ClFN₃	Package：Package according to customer requirements
Molecular Weight：317.788	Storage：Store at -20℃

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Remarks

RS-127445 is a selective; high affinity; orally bioavailable serotonin 5-HT2B receptor antagonist. RS-127445 was found to have nanomolar affinity for the 5-HT2B receptor (pKi = 9.5+/-0.1) and 1,000 fold selectivity for this receptor as compared to numerous other receptor and ion channel binding sites. RS-127445 potently antagonized 5-HT-evoked formation of inositol phosphates (pK(B) = 9.5+/-0.1) and 5-HT-evoked increases in intracellular calcium (pIC50 = 10.4+/-0.1). RS-127445 also blocked 5-HT-evoked contraction of rat isolated stomach fundus (pA2 = 9.5+/-1.1) and (+/-)alpha-methyl-5-HT-mediated relaxation of the rat jugular vein (pA2 = 9.9+/-0.3).

5-HT Receptor Inhibitors Related Products:

Asenapine Maleate; WAY-100635 Maleate; WAY-100635 maleate salt; Vortioxetine; Vortioxetine hydrobromide; Blonanserin; Intepirdine; Sertraline HCl; Lamotrigine; Azasetron hydrochloride; Iloperidone

References

[1]. Bonhaus DW, et al. RS-127445: a selective, high affinity, orally bioavailable 5-HT2B receptor antagonist. Br J Pharmacol. 1999 Jul;127(5):1075-82.

[2]. Bassil AK, et al. Inhibition of colonic motility and defecation by RS-127445 suggests an involvement of the 5-HT2B receptor in rodent large bowel physiology. Br J Pharmacol. 2009 Sep;158(1):252-8