Characterization of RO4583298 as a novel potent dual antagonist with in vivo activity at tachykinin NK1 and NK3 receptors

摘要

BACKGROUND AND PURPOSEClinical results of osanetant and talnetant (selective-NK3 antagonists) indicate that blocking the NK3 receptor could be beneficial for the treatment of schizophrenia. The objective of this study was to characterize the in vitro and in vivo properties of a novel dual NK1/NK3 antagonist, RO4583298 (2-phenyl-N-(pyridin-3-yl)-N-methylisobutyramide derivative).