PF-3274167

Description: Cligosiban (formerly known as PF-3274167) is a novel, potent, selective and high-affinity nonpeptide antagonist of oxytocin receptor (OTR) with Ki of 9.5 nM. PF-3274167 displayed promising in vivo pharmacokinetics and significantly improved aqueous solubility over related compounds containing a biaryl substituent. Oxytocin receptor is a G protein-coupled receptor/protein which functions as receptor for the hormone and neurotransmitter oxytocin. Oxytocin receptors are also present in the central nervous system. PF-3274167 is a high-affinity nonpeptide oxytocin receptor (OTR) antagonist, nM.

References: Bioorg Med Chem Lett. 2010 Jan 15; 20(2):516-20.J Med Chem. 2015 Mar 12; 58(5):2547-52