Article ID Journal Published Year Pages File Type
10835677 Peptides 2012 12 Pages PDF
Abstract
► Netupitant behaves in vitro as a highly potent and selective NK1 receptor antagonist. ► In bioassay washout experiments, Netupitant displayed persistent (up to 5 h) antagonist effects. ► Netupitant antagonizes nociceptive responses to intrathecal substance P in mice. ► Netupitant prevents foot tapping induced by a NK1 agonist in gerbils showing long lasting effects. ► Netupitant is as a brain penetrant, orally active, potent and selective NK1 antagonist.
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