Author/Authors :
Michelle Laci Wrobleski، نويسنده , , Gregory A. Reichard، نويسنده , , Sunil Paliwal، نويسنده , , Sapna Shah، نويسنده , , Hon-Chung Tsui، نويسنده , , Ruth A. Duffy، نويسنده , , Jean E. Lachowicz، نويسنده , , Cynthia A. Morgan، نويسنده , , Geoffrey B. Varty، نويسنده , , Neng-Yang Shih، نويسنده ,
Abstract :
A series of novel cyclobutane derivatives as potent and selective NK1 receptor antagonists is described. Several compounds in this series exhibited high in vitro binding affinity (Ki 1 nM), and potent inhibition of central NK1 receptor following oral administration. Syntheses of these compounds are also described herein.
Keywords :
NK1 antagonist , Substance P , cyclobutane , CNS penetration , Oral in vivo activity
