RS-127445 199864-87-3

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Molecular Weight:

281.33 RS-127445 is a selective 5-HT2B receptor antagonist with pKi of 9.5 and pIC50 of 10.4, exhibits >1000-fold selectivity against other 5-HT receptors.

Biological Activity

RS-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.


RS-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 achieved 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.

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Product Categories : Neuronal Signaling > 5-HT Receptor Inhibitor